1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

Bioorganic & Medicinal Chemistry - Tập 27 Số 16 - Trang 3511-3531 - 2019
Khurshed Bozorov1,2, Jiangyu Zhao2, Haji Akber Aisa2
1Institute of the Chemistry of Plant Substances, Academy of Sciences of Uzbekistan, Mirzo Ulugbek Str. 77, Tashkent, 100170, Uzbekistan
2Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, 40-1 South Beijing Rd, Urumqi, 830011, PR China

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Tài liệu tham khảo

Ahmad, 2018, Pyrrole: an insight into recent pharmacological advances with structure activity relationship, Eur J Med Chem, 157, 527, 10.1016/j.ejmech.2018.08.002

Parker, 2009, Enzymology of purine and pyrimidine antimetabolites used in the treatment of cancer, Chem Rev, 109, 2880, 10.1021/cr900028p

Bozorov, 2017, 2-Aminothiophene scaffolds: diverse biological and pharmacological attributes in medicinal chemistry, Eur J Med Chem, 140, 465, 10.1016/j.ejmech.2017.09.039

Bozorov, 2015, Recent developments regarding the use of thieno[2,3-d]pyrimidin-4-one derivatives in medicinal chemistry, with a focus on their synthesis and anticancer properties, Eur J Med Chem, 102, 552, 10.1016/j.ejmech.2015.08.018

Bozorov, 2014, Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: synthesis and in vitro biological evaluation. Part 1, Eur J Med Chem, 84, 739, 10.1016/j.ejmech.2014.07.065

Bozorov, 2017, Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and anti-influenza virus agents. Part 2, RSC Adv, 7, 31417, 10.1039/C7RA04808D

Khanam, 2015, Bioactive Benzofuran derivatives: a review, Eur J Med Chem, 97, 483, 10.1016/j.ejmech.2014.11.039

Naik, 2015, Bioactive benzofuran derivatives: moracins A-Z in medicinal chemistry, Eur J Med Chem, 90, 379, 10.1016/j.ejmech.2014.11.047

Majumdar, 2014, Acid hydrazides, potent reagents for synthesis of oxygen-, nitrogen-, and/or sulfur-containing heterocyclic rings, Chem Rev, 114, 2942, 10.1021/cr300122t

Ayati, 2016, The importance of triazole scaffold in the development of anticonvulsant agents, Eur J Med Chem, 109, 380, 10.1016/j.ejmech.2016.01.009

Briguglio, 2015, Benzotriazole: an overview on its versatile biological behavior, Eur J Med Chem, 97, 612, 10.1016/j.ejmech.2014.09.089

Abdellatif, 2018, New advances in synthesis and clinical aspects of pyrazolo[3,4-d]pyrimidine scaffolds, Bioorg Chem, 78, 341, 10.1016/j.bioorg.2018.03.032

Herr, 2002, 5-Substituted-1H-tetrazoles as carboxylic acid isosteres: medicinal chemistry and synthetic methods, Bioorg Med Chem, 10, 3379, 10.1016/S0968-0896(02)00239-0

Dymińska, 2015, Imidazopyridines as a source of biological activity and their pharmacological potentials—infrared and Raman spectroscopic evidence of their content in pharmaceuticals and plant materials, Bioorg Med Chem, 23, 6087, 10.1016/j.bmc.2015.07.045

Reports regarding the use of triazoles in the Scopus database in: www.scopus.com, 2018.

Dheer, 2017, Medicinal attributes of 1,2,3-triazoles: current developments, Bioorg Chem, 71, 30, 10.1016/j.bioorg.2017.01.010

Carmona, 2018, Harnessing pyrrolidine iminosugars into dimeric structures for the rapid discovery of divalent glycosidase inhibitors, Eur J Med Chem, 151, 765, 10.1016/j.ejmech.2018.04.008

Guo, 2018, Selective inhibitors of human neuraminidase 3, J Med Chem, 61, 1990, 10.1021/acs.jmedchem.7b01574

Gonzalez, 2018, The 4-N-acyl and 4-N-alkyl gemcitabine analogues with silicon-fluoride-acceptor: application to 18F-radiolabeling, Eur J Med Chem, 148, 314, 10.1016/j.ejmech.2018.02.017

Fjellaksel, 2018, Copper-mediated late-stage iodination and 123 I-labelling of triazole-benzimidazole bioactives, Synlett, 29, 1491, 10.1055/s-0036-1591985

Kommidi, 2018, 18F-positron emitting/trimethine cyanine-fluorescent contrast for image-guided prostate cancer management, J Med Chem, 61, 4256, 10.1021/acs.jmedchem.8b00240

Huang, 2018, Radiosynthesis and biological evaluation of 18F-labeled 4-anilinoquinazoline derivative (18F-FEA-Erlotinib) as a potential EGFR PET agent, Bioorg Med Chem Lett, 28, 1143, 10.1016/j.bmcl.2017.08.066

Valdomir, 2018, Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells, New J Chem, 42, 13784, 10.1039/C8NJ02388C

Zhou, 2018, Boronic acid inhibitors of the class A β-lactamase KPC-2, Bioorg Med Chem, 26, 2921, 10.1016/j.bmc.2018.04.055

Lopes, 2018, Hetero-Diels-Alder reactions of novel 3-triazolyl-nitrosoalkenes as an approach to functionalized 1,2,3-triazoles with antibacterial profile, Eur J Med Chem, 143, 1010, 10.1016/j.ejmech.2017.11.052

Fletcher, 2018, Antimicrobial 1,3,4-trisubstituted-1,2,3-triazolium salts, Bioorg Med Chem Lett, 28, 3320, 10.1016/j.bmcl.2018.09.011

Rezaei-Matehkolaei, 2018, In vitro antifungal activity of novel triazole efinaconazole and five comparators against dermatophyte isolates, Antimicrob Agents Chemother, 62, 10.1128/AAC.02423-17

Savanur, 2018, Click chemistry inspired design, synthesis and molecular docking studies of coumarin, quinolinone linked 1,2,3-triazoles as promising anti-microbial agents, ChemistrySelect, 3, 5296, 10.1002/slct.201800319

Tarawneh, 2018, Evaluation of triazole and isoxazole derivatives as potential anti-infective agents, Med Chem Res, 27, 1269, 10.1007/s00044-018-2146-4

Batra, 2018, Synthesis and antimalarial evaluation of [1,2,3]-triazole-tethered sulfonamide-berberine hybrids, ChemistrySelect, 3, 9790, 10.1002/slct.201801905

Rajavelu, 2018, Synthesis, optical properties, and antioxidant and anticancer activity of benzoheterazole dendrimers with triazole bridging unit, New J Chem, 42, 3282, 10.1039/C7NJ04060A

Kumar, 2018, Synthesis and in-vitro antioxidant activities of some coumarin derivatives containing 1,2,3-triazole ring, Phosphorus, Sulfur Silicon Relat Elem, 193, 294, 10.1080/10426507.2017.1417293

Santosh, 2018, Synthesis, characterization, antibacterial and antioxidant studies of some heterocyclic compounds from triazole-linked chalcone derivatives, ChemistrySelect, 3, 6338, 10.1002/slct.201800905

Liu, 2018, A general approach towards triazole-linked adenosine diphosphate ribosylated peptides and proteins, Angew Chem Int Ed, 57, 1659, 10.1002/anie.201710527

Ben Haj Salah, 2018, How are 1,2,3-triazoles accommodated in helical secondary structures?, Org Biomol Chem, 16, 3576, 10.1039/C8OB00686E

Kacprzak, 2016, Alkaloids and isoprenoids modification by copper(I)-catalyzed Huisgen 1,3-dipolar cycloaddition (click chemistry): toward new functions and molecular architectures, Chem Rev, 116, 5689, 10.1021/acs.chemrev.5b00302

Johansson, 2016, Ruthenium-catalyzed azide alkyne cycloaddition reaction: scope, mechanism, and applications, Chem Rev, 116, 14726, 10.1021/acs.chemrev.6b00466

Efimov, 2019, Recent methods for the synthesis of NH-1,2,3-triazoles (microreview), Chem Heterocycl Compd, 55, 28, 10.1007/s10593-019-02414-8

Totobenazara, 2015, New click-chemistry methods for 1,2,3-triazoles synthesis: recent advances and applications, Tetrahedron Lett, 56, 2853, 10.1016/j.tetlet.2015.03.136

Usachev, 2018, Chemistry of fluoroalkyl-substituted 1,2,3-triazoles, J Fluorine Chem, 210, 6, 10.1016/j.jfluchem.2018.02.012

Bonandi, 2017, The 1,2,3-triazole ring as a bioisostere in medicinal chemistry, Drug Discov Today, 22, 1572, 10.1016/j.drudis.2017.05.014

Rejhová, 2018, Natural compounds and combination therapy in colorectal cancer treatment, Eur J Med Chem, 144, 582, 10.1016/j.ejmech.2017.12.039

Prasad, 2018, Chapter 5 – chemosensitization by ursolic acid: a new avenue for cancer therapy, Vol 2, 99

Lal, 2018, Recent advancements in 1,4-disubstituted 1H-1,2,3-triazoles as potential anticancer agents, Anti-Cancer Agents Med Chem, 18, 21, 10.2174/1871520616666160811113531

Ding, 2018, Copper(I) oxide nanoparticles catalyzed click chemistry based synthesis of melampomagnolide B-triazole conjugates and their anti-cancer activities, Eur J Med Chem, 156, 216, 10.1016/j.ejmech.2018.06.058

Janganati, 2018, MMB triazole analogs are potent NF-κB inhibitors and anti-cancer agents against both hematological and solid tumor cells, Eur J Med Chem, 157, 562, 10.1016/j.ejmech.2018.08.010

Yu, 2018, Design, synthesis, cytotoxicity and mechanism of novel dihydroartemisinin-coumarin hybrids as potential anti-cancer agents, Eur J Med Chem, 151, 434, 10.1016/j.ejmech.2018.04.005

Ke, 2018, Synthesis and biological evaluation of novel Jiyuan Oridonin A-1,2,3-triazole-azole derivatives as antiproliferative agents, Eur J Med Chem, 157, 1249, 10.1016/j.ejmech.2018.08.056

Ke, 2018, Design, synthesis and biological mechanisms research on 1,2,3-triazole derivatives of Jiyuan Oridonin A, Bioorg Med Chem, 26, 4761, 10.1016/j.bmc.2017.11.005

Wei, 2018, Novel antitumor compound optimized from natural saponin Albiziabioside A induced caspase-dependent apoptosis and ferroptosis as a p53 activator through the mitochondrial pathway, Eur J Med Chem, 157, 759, 10.1016/j.ejmech.2018.08.036

Li, 2018, Synthesis, antitumor activity evaluation and mechanistic study of novel hederacolchiside A1 derivatives bearing an aryl triazole moiety, Biorg Med Chem, 26, 4025, 10.1016/j.bmc.2018.06.026

Wu, 2018, Synthesis and anti-proliferative activity of allogibberic acid derivatives containing 1,2,3-triazole pharmacophore, Bioorg Med Chem Lett, 28, 2543, 10.1016/j.bmcl.2018.05.038

Boratyński, 2018, Triazole biheterocycles from cinchona alkaloids: coordination and antiproliferative properties, ChemistrySelect, 3, 9368, 10.1002/slct.201801810

Abou Samra, 2018, Dual inhibitors of the pro-survival proteins Bcl-2 and Mcl-1 derived from natural compound meiogynin A, Eur J Med Chem, 148, 26, 10.1016/j.ejmech.2018.01.100

Bębenek, 2018, Novel triazoles of 3-acetylbetulin and betulone as anticancer agents, Med Chem Res, 27, 2051, 10.1007/s00044-018-2213-x

Reddy, 2018, 4β-amidotriazole linked podophyllotoxin congeners: DNA topoisomerase-IIα inhibition and potential anticancer agents for prostate cancer, Eur J Med Chem, 144, 595, 10.1016/j.ejmech.2017.12.050

Bian, 2018, Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity, Bioorg Chem, 81, 373, 10.1016/j.bioorg.2018.08.028

Gupta, 2018, Synthesis and biological evaluation of novel bavachinin analogs as anticancer agents, Eur J Med Chem, 145, 511, 10.1016/j.ejmech.2018.01.006

Safavi, 2018, Novel quinazolin-4(3H)-one linked to 1,2,3-triazoles: synthesis and anticancer activity, Chem Biol Drug Des, 92, 1373, 10.1111/cbdd.13203

Vasu, 2018, 2-((1H-1,2,3-Triazol-1-yl)methyl)-3-phenylquinazolin-4(3H)-ones: design, synthesis and evaluation as anti-cancer agents, Curr Bioact Compd, 14, 254, 10.2174/1573407213666170329131557

Le-Nhat-Thuy, 2018, Design, synthesis and evaluation of novel hybrids between 4-anilinoquinazolines and substituted triazoles as potent cytotoxic agents, Bioorg Med Chem Lett, 28, 3741, 10.1016/j.bmcl.2018.10.016

Srinivas, 2018, Design and synthesis of 1,4-substituted 1H–1,2,3-triazolo-quinazolin-4(3H)-ones by Huisgen 1,3-dipolar cycloaddition with PI3Kγ isoform selective activity, Bioorg Med Chem Lett, 28, 1005, 10.1016/j.bmcl.2018.02.032

Kettle, 2018, Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors, J Med Chem, 61, 8797, 10.1021/acs.jmedchem.8b00938

Craik, 2013, The future of peptide-based drugs, Chem Biol Drug Des, 81, 136, 10.1111/cbdd.12055

Chen, 2018, Identification of novel and selective non-peptide inhibitors targeting the polo-box domain of polo-like kinase 1, Bioorg Chem, 81, 278, 10.1016/j.bioorg.2018.08.030

Matthiesen, 2018, α-Methylation enhances the potency of isoprenoid triazole bisphosphonates as geranylgeranyl diphosphate synthase inhibitors, Bioorg Med Chem, 26, 376, 10.1016/j.bmc.2017.10.023

Cao, 2018, Novel leucine ureido derivatives as aminopeptidase N inhibitors using click chemistry, Bioorg Med Chem, 26, 3145, 10.1016/j.bmc.2018.04.041

Compain, 2018, A β-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy, Eur J Med Chem, 158, 1, 10.1016/j.ejmech.2018.08.100

Chen, 2018, Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors, Bioorg Med Chem, 26, 3958, 10.1016/j.bmc.2018.06.016

Gao, 2018, Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors, Bioorg Med Chem, 26, 2420, 10.1016/j.bmc.2018.03.045

Geng, 2018, Design, synthesis and in vitro biological evaluation of novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing a thiosemicarbazide moiety, Eur J Med Chem, 146, 147, 10.1016/j.ejmech.2018.01.031

Yamada, 2018, Synthesis, antitumor activity, and cytotoxicity of 4-substituted 1-benzyl-5-diphenylstibano-1H-1,2,3-triazoles, Bioorg Med Chem Lett, 28, 152, 10.1016/j.bmcl.2017.11.038

Gilandoust, 2018, Synthesis, characterization and cytotoxicity studies of 1,2,3-triazoles and 1,2,4-triazolo [1,5-a] pyrimidines in human breast cancer cells, Bioorg Med Chem Lett, 28, 2314, 10.1016/j.bmcl.2018.05.020

Allam, 2018, Synthesis of pyrazolo[3,4-d]pyrimidin-4(5H)-ones tethered to 1,2,3-triazoles and their evaluation as potential anticancer agents, Eur J Med Chem, 156, 43, 10.1016/j.ejmech.2018.06.055

Li, 2018, Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells, Bioorg Med Chem Lett, 28, 700, 10.1016/j.bmcl.2018.01.011

Wang, 2018, Discovery of thinopyrimidine-triazole conjugates as c-Met targeting and apoptosis inducing agents, Bioorg Chem, 77, 370, 10.1016/j.bioorg.2018.01.037

Sayeed, 2018, Imidazopyridine linked triazoles as tubulin inhibitors, effectively triggering apoptosis in lung cancer cell line, Bioorg Chem, 80, 714, 10.1016/j.bioorg.2018.07.026

Bistrović, 2018, Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer, Eur J Med Chem, 143, 1616, 10.1016/j.ejmech.2017.10.061

Borowiecki, 2018, Synthesis of novel proxyphylline derivatives with dual Anti-Candida albicans and anticancer activity, Eur J Med Chem, 150, 307, 10.1016/j.ejmech.2018.02.077

Costa, 2018, Synthesis and evaluation of the cytotoxic activity of Furanaphthoquinones tethered to 1H-1,2,3-triazoles in Caco-2, Calu-3, MDA-MB231 cells, Eur J Med Chem, 156, 524, 10.1016/j.ejmech.2018.07.018

Dadmal, 2018, Synthesis and biological evaluation of triazole and isoxazole-tagged benzothiazole/benzoxazole derivatives as potent cytotoxic agents, New J Chem, 42, 15546, 10.1039/C8NJ01249K

Kumar, 2018, Design, synthesis, anti-proliferative evaluation and docking studies of 1: H-1,2,3-triazole tethered ospemifene-isatin conjugates as selective estrogen receptor modulators, New J Chem, 42, 3703, 10.1039/C7NJ04964A

Naaz, 2018, 1,2,3-Triazole tethered Indole-3-glyoxamide derivatives as multiple inhibitors of 5-LOX, COX-2 & tubulin: their anti-proliferative & anti-inflammatory activity, Bioorg Chem, 81, 1, 10.1016/j.bioorg.2018.07.029

Schlapbach, 2018, N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity, Bioorg Med Chem Lett, 28, 2153, 10.1016/j.bmcl.2018.05.017

Wang, 2018, Exploration of 1,2,3-triazole-pyrimidine hybrids as potent reversal agents against ABCB1-mediated multidrug resistance, Eur J Med Chem, 143, 1535, 10.1016/j.ejmech.2017.10.041

Wang, 2018, Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R, Eur J Med Chem, 143, 123, 10.1016/j.ejmech.2017.11.008

Marepu, 2018, 1,2,3-Triazole fused with pyridine/pyrimidine as new template for antimicrobial agents: regioselective synthesis and identification of potent N-heteroarenes, Bioorg Med Chem Lett, 28, 3302, 10.1016/j.bmcl.2018.09.021

Szałaj, 2018, Boronic ester-linked macrocyclic lipopeptides as serine protease inhibitors targeting Escherichia coli type I signal peptidase, Eur J Med Chem, 157, 1346, 10.1016/j.ejmech.2018.08.086

Lal, 2018, Design, synthesis, characterization, antimicrobial evaluation and molecular modeling studies of some dehydroacetic acid-chalcone-1,2,3-triazole hybrids, Bioorg Chem, 77, 236, 10.1016/j.bioorg.2018.01.016

Maddili, 2018, Molecular interaction of novel benzothiazolyl triazolium analogues with calf thymus DNA and HSA-their biological investigation as potent antimicrobial agents, Eur J Med Chem, 150, 228, 10.1016/j.ejmech.2018.02.056

Mishra, 2018, Rational modification of a lead molecule: improving the antifungal activity of indole – triazole – amino acid conjugates, Eur J Med Chem, 155, 658, 10.1016/j.ejmech.2018.06.039

Yu, 2018, Structure-based design of bacterial transglycosylase inhibitors incorporating biphenyl, amine linker and 2-alkoxy-3-phosphorylpropanoate moieties, Eur J Med Chem, 150, 729, 10.1016/j.ejmech.2018.03.034

Bi, 2018, Substitution of terminal amide with 1H-1,2,3-triazole: identification of unexpected class of potent antibacterial agents, Bioorg Med Chem Lett, 28, 884, 10.1016/j.bmcl.2018.02.001

Sall, 2018, Towards smart biocide-free anti-biofilm strategies: click-based synthesis of cinnamide analogues as anti-biofilm compounds against marine bacteria, Bioorg Med Chem Lett, 28, 155, 10.1016/j.bmcl.2017.11.039

Gatadi, 2018, Synthesis of 1,2,3-triazole linked 4(3H)-Quinazolinones as potent antibacterial agents against multidrug-resistant Staphylococcus aureus, Eur J Med Chem, 157, 1056, 10.1016/j.ejmech.2018.08.070

Yadav, 2018, Synthesis, crystal structure and antimicrobial potential of some fluorinated chalcone-1,2,3-triazole conjugates, Eur J Med Chem, 155, 263, 10.1016/j.ejmech.2018.05.055

Srinivasarao, 2018, Design, synthesis and biological evaluation of triazole-containing 2-phenylindole and salicylic acid as quorum sensing inhibitors against Pseudomonas aeruginosa, ChemistrySelect, 3, 9170, 10.1002/slct.201801622

Govindaiah, 2018, Regioselective synthesis, antibacterial, molecular docking and fingerprint applications of 1-benzhydrylpiperazine derivatized 1,4-disubstituted 1,2,3-triazoles, ChemistrySelect, 3, 8111, 10.1002/slct.201801364

Kaushik, 2018, Convenient synthesis, antimalarial and antimicrobial potential of thioethereal 1,4-disubstituted 1,2,3-triazoles with ester functionality, Med Chem Res, 27, 458, 10.1007/s00044-017-2072-x

Moghimi, 2018, Synthesis, evaluation, and molecular docking studies of aryl urea-triazole-based derivatives as anti-urease agents, Arch Pharm, 351, 10.1002/ardp.201800005

Faidallah, 2018, Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates, Eur J Med Chem, 143, 1524, 10.1016/j.ejmech.2017.10.042

Yang, 2018, 1,3,5-Triazaspiro[5.5]undeca-2,4-dienes as selective Mycobacterium tuberculosis dihydrofolate reductase inhibitors with potent whole cell activity, Eur J Med Chem, 144, 262, 10.1016/j.ejmech.2017.12.017

Spain, 2018, Antitubercular bis-substituted cyclam derivatives: structure-activity relationships and in vivo studies, J Med Chem, 61, 3595, 10.1021/acs.jmedchem.7b01569

Carta, 2019, Design synthesis and antitubercular activity of 4-alkoxy-triazoloquinolones able to inhibit the M. tuberculosis DNA gyrase, Eur J Med Chem, 161, 399, 10.1016/j.ejmech.2018.10.031

Yan, 2018, Synthesis and in vitro evaluation of novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids for their anti-mycobacterial activities, Eur J Med Chem, 143, 899, 10.1016/j.ejmech.2017.11.090

Srivastava, 2018, Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole, Eur J Med Chem, 150, 268, 10.1016/j.ejmech.2018.02.067

Danne, 2018, Triazole-diindolylmethane conjugates as new antitubercular agents: synthesis, bioevaluation, and molecular docking, MedChemComm, 9, 1114, 10.1039/C8MD00055G

Ashok, 2018, 1,2,3-Triazole-fused spirochromenes as potential anti-tubercular agents: synthesis and biological evaluation, RSC Adv, 8, 16997, 10.1039/C8RA03197E

Giroud, 2018, 2H-1,2,3-triazole-based dipeptidyl nitriles: potent, selective, and trypanocidal rhodesain inhibitors by structure-based design, J Med Chem, 61, 3370, 10.1021/acs.jmedchem.7b01870

Negi, 2018, Synthesis, antiamoebic activity and docking studies of metronidazole-triazole-styryl hybrids, Eur J Med Chem, 150, 633, 10.1016/j.ejmech.2018.03.033

Zimmermann, 2018, Synthesis and SAR of new isoxazole-triazole bis-heterocyclic compounds as analogues of natural lignans with antiparasitic activity, Bioorg Med Chem, 26, 4850, 10.1016/j.bmc.2018.08.025

Zhang, 2018, Synthesis and evaluation of novel arctigenin derivatives as potential anti-Toxoplasma gondii agents, Eur J Med Chem, 158, 414, 10.1016/j.ejmech.2018.08.087

Hu, 2018, Recent development of coumarin derivatives as potential antiplasmodial and antimalarial agents, Curr Top Med Chem, 18, 114, 10.2174/1568026618666171215101158

Jarrahpour, 2018, Design, synthesis, activity evaluation and QSAR studies of novel antimalarial 1,2,3-triazolo-β-lactam derivatives, J Iran Chem Soc, 15, 1311, 10.1007/s13738-018-1330-2

Brandão, 2018, Antimalarial naphthoquinones. Synthesis via click chemistry, in vitro activity, docking to PfDHODH and SAR of lapachol-based compounds, Eur J Med Chem, 145, 191, 10.1016/j.ejmech.2017.12.051

Chopra, 2018, Pyrimidine-chloroquinoline hybrids: synthesis and antiplasmodial activity, Eur J Med Chem, 148, 39, 10.1016/j.ejmech.2018.02.021

Yadav, 2018, In vitro antiplasmodial efficacy of synthetic coumarin-triazole analogs, Eur J Med Chem, 145, 735, 10.1016/j.ejmech.2018.01.017

Thakur, 2018, Synthesis and antiplasmodial activity of glyco-conjugate hybrids of phenylhydrazono-indolinones and glycosylated 1,2,3-triazolyl-methyl-indoline-2,3-diones, Eur J Med Chem, 155, 764, 10.1016/j.ejmech.2018.06.042

Oliveira, 2018, Design, synthesis and antileishmanial activity of naphthotriazolyl-4-oxoquinolines, Curr Top Med Chem, 18, 1454, 10.2174/1568026618666181002110116

Temraz, 2018, Anti-leishmanial click modifiable thiosemicarbazones: design, synthesis, biological evaluation and in silico studies, Eur J Med Chem, 151, 585, 10.1016/j.ejmech.2018.04.003

Teixeira, 2018, Synthesis and leishmanicidal activity of eugenol derivatives bearing 1,2,3-triazole functionalities, Eur J Med Chem, 146, 274, 10.1016/j.ejmech.2018.01.046

Upadhyay, 2018, Synthesis and evaluation of novel triazolyl quinoline derivatives as potential antileishmanial agents, Eur J Med Chem, 154, 172, 10.1016/j.ejmech.2018.05.014

Maji, 2018, Potential antileishmanial activity of a triazole-based hybrid peptide against leishmania major, ChemistrySelect, 3, 10220, 10.1002/slct.201802002

Gonzaga, 2018, Identification of 1-aryl-1H-1,2,3-triazoles as potential new antiretroviral agents, Med Chem, 14, 242, 10.2174/1573406413666170906121318

Liu, 2018, Design, synthesis, and biological evaluation of new 1,2,3-triazolo-2′-deoxy-2′-fluoro- 4′-azido nucleoside derivatives as potent anti-HBV agents, Eur J Med Chem, 143, 137, 10.1016/j.ejmech.2017.11.028

Karypidou, 2018, Synthesis, biological evaluation and molecular modeling of a novel series of fused 1,2,3-triazoles as potential anti-coronavirus agents, Bioorg Med Chem Lett, 28, 3472, 10.1016/j.bmcl.2018.09.019

Yan, 2018, Synthesis of pentacyclic iminosugars with constrained butterfly-like conformation and their HIV-RT inhibitory activity, Bioorg Med Chem Lett, 28, 425, 10.1016/j.bmcl.2017.12.025

Liu, 2018, Design, synthesis, and structure-activity relationships of novel imidazo[4,5-c]pyridine derivatives as potent non-nucleoside inhibitors of hepatitis C virus NS5B, Bioorg Med Chem, 26, 2621, 10.1016/j.bmc.2018.04.029

Kaoukabi, 2018, Dihydropyrimidinone/1,2,3-triazole hybrid molecules: synthesis and anti-varicella-zoster virus (VZV) evaluation, Eur J Med Chem, 155, 772, 10.1016/j.ejmech.2018.06.028

Wu, 2018, Discovery of phenylalanine derivatives as potent HIV-1 capsid inhibitors from click chemistry-based compound library, Eur J Med Chem, 158, 478, 10.1016/j.ejmech.2018.09.029

Tian, 2018, Targeting the entrance channel of NNIBP: discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus, Eur J Med Chem, 151, 339, 10.1016/j.ejmech.2018.03.059

Saeedi, 2019, Design and synthesis of novel quinazolinone-1,2,3-triazole hybrids as new anti-diabetic agents: in vitro α-glucosidase inhibition, kinetic, and docking study, Bioorg Chem, 83, 161, 10.1016/j.bioorg.2018.10.023

Avula, 2018, Synthesis of 1H–1,2,3-triazole derivatives as new α-glucosidase inhibitors and their molecular docking studies, Bioorg Chem, 81, 98, 10.1016/j.bioorg.2018.08.008

Kumari, 2018, Synthesis, docking and ADME prediction of novel 1,2,3-triazole-tethered coumarin derivatives as potential neuroprotective agents, Res Chem Intermed, 44, 1989, 10.1007/s11164-017-3210-2

Reddy, 2018, Synthesis and biological evaluation of longanlactone analogues as neurotrophic agents, Bioorg Med Chem Lett, 28, 673, 10.1016/j.bmcl.2018.01.020

Sweeney, 2018, Riluzole-triazole hybrids as novel chemical probes for neuroprotection in amyotrophic lateral sclerosis, ACS Med Chem Lett, 9, 552, 10.1021/acsmedchemlett.8b00103

Giraudo, 2018, 4-Hydroxy-1,2,3-triazole moiety as bioisostere of the carboxylic acid function: a novel scaffold to probe the orthosteric γ-aminobutyric acid receptor binding site, Eur J Med Chem, 158, 311, 10.1016/j.ejmech.2018.08.094

Chrovian, 2018, A Dipolar cycloaddition reaction to access 6-methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines enables the discovery synthesis and preclinical profiling of a P2X7 antagonist clinical candidate, J Med Chem, 61, 207, 10.1021/acs.jmedchem.7b01279

Luo, 2018, Syntheses and in vitro evaluation of new S1PR1 compounds and initial evaluation of a lead F-18 radiotracer in rodents, Eur J Med Chem, 150, 796, 10.1016/j.ejmech.2018.03.035

Gilbertson, 2018, Synthesis and activity of functionalizable derivatives of the serotonin (5-HT) 5-HT2A receptor (5-HT2AR) antagonist M100907, Bioorg Med Chem Lett, 28, 1381, 10.1016/j.bmcl.2018.02.058

Jalili-Baleh, 2018, Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds, Eur J Med Chem, 152, 600, 10.1016/j.ejmech.2018.04.058

Jalili-Baleh, 2018, Novel 3-phenylcoumarin–lipoic acid conjugates as multi-functional agents for potential treatment of Alzheimer's disease, Bioorg Chem, 79, 223, 10.1016/j.bioorg.2018.04.030

Wang, 2018, Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: design, synthesis and biological evaluation, Eur J Med Chem, 151, 351, 10.1016/j.ejmech.2018.03.082

Wu, 2018, Design, synthesis and biological evaluation of tacrine-1,2,3-triazole derivatives as potent cholinesterase inhibitors, MedChemComm, 9, 149, 10.1039/C7MD00457E

Moussa, 2018, Novel click modifiable thioquinazolinones as anti-inflammatory agents: design, synthesis, biological evaluation and docking study, Eur J Med Chem, 144, 635, 10.1016/j.ejmech.2017.12.065

Rama Krishna, 2018, Synthesis of some novel orcinol based coumarin triazole hybrids with capabilities to inhibit RANKL-induced osteoclastogenesis through NF-κB signaling pathway, Bioorg Chem, 78, 94, 10.1016/j.bioorg.2018.03.005

Yu, 2018, Structure-guided modification of heterocyclic antagonists of the P2Y14 receptor, J Med Chem, 61, 4860, 10.1021/acs.jmedchem.8b00168

More, 2018, Acetazolamide-based [18F]-PET tracer: in vivo validation of carbonic anhydrase IX as a sole target for imaging of CA-IX expressing hypoxic solid tumors, Bioorg Med Chem Lett, 28, 915, 10.1016/j.bmcl.2018.01.060

Kumar, 2018, Design and synthesis of novel benzenesulfonamide containing 1,2,3-triazoles as potent human carbonic anhydrase isoforms I, II, IV and IX inhibitors, Eur J Med Chem, 155, 545, 10.1016/j.ejmech.2018.06.021

Vats, 2018, Synthesis of novel 4-functionalized 1,5-diaryl-1,2,3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors, Eur J Med Chem, 150, 678, 10.1016/j.ejmech.2018.03.030

Wu, 2018, Click chemistry-based discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as orally active hypoxia-inducing factor prolyl hydroxylase inhibitors with favorable safety profiles for the treatment of anemia, J Med Chem, 61, 5332, 10.1021/acs.jmedchem.8b00549

Rajan, 2018, Novel indole and triazole based hybrid molecules exhibit potent anti-adipogenic and antidyslipidemic activity by activating Wnt3a/β-catenin pathway, Eur J Med Chem, 143, 1345, 10.1016/j.ejmech.2017.10.034

Narsimha, 2018, One-pot synthesis of novel 1,2,3-triazole-pyrimido[4,5-c]isoquinoline hybrids and evaluation of their antioxidant activity, Synth Commun, 48, 1220, 10.1080/00397911.2018.1440315

Chekir, 2018, Design, synthesis and biological evaluation of novel 1,2,3-triazole linked coumarinopyrazole conjugates as potent anticholinesterase, anti-5-lipoxygenase, anti-tyrosinase and anti-cancer agents, Bioorg Chem, 80, 189, 10.1016/j.bioorg.2018.06.005

Kayet, 2018, 1,5-Disubstituted 1,2,3-triazole linked disaccharides: metal-free syntheses and screening of a new class of ribonuclease A inhibitors, Bioorg Med Chem, 26, 455, 10.1016/j.bmc.2017.12.004

Kozarski, 2018, 7-Methylguanosine monophosphate analogues with 5′-(1,2,3-triazoyl) moiety: synthesis and evaluation as the inhibitors of cNIIIB nucleotidase, Bioorg Med Chem, 26, 191, 10.1016/j.bmc.2017.11.032

Peterson, 2018, Systematic tuning of fluoro-galectin-3 interactions provides thiodigalactoside derivatives with single-digit nM affinity and high selectivity, J Med Chem, 61, 1164, 10.1021/acs.jmedchem.7b01626

Lu, 2018, Design, synthesis, and biological evaluation of novel substituted benzamide derivatives bearing a 1,2,3-triazole moiety as potent human dihydroorotate dehydrogenase inhibitors, Bioorg Chem, 76, 528, 10.1016/j.bioorg.2017.12.025

Syeda, 2018, Design, synthesis, and in vitro and in vivo evaluation of ouabain analogues as potent and selective Na, K-ATPase α4 isoform inhibitors for male contraception, J Med Chem, 61, 1800, 10.1021/acs.jmedchem.7b00925

Thomson, 2018, Development of autotaxin inhibitors: a series of zinc binding triazoles, Bioorg Med Chem Lett, 28, 2279, 10.1016/j.bmcl.2018.05.030