Synthesis of (substituted benzamidostyryl) lH-benzimidazoles and their screening for anti-inflammatory activity
Tóm tắt
A series of substituted (benzamidostyryl) benzimidazole (3a–r) were synthesized and evaluated for their possible anti-inflammatory and ulcerogenicity. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. Majority of the compounds were active in carrageenan-induced hind paw edema method test and compounds 3b, 3k had shown high potency after 3 and 4 h time intervals (P < 0.001) almost equipotent to the standard drug indomethacin and showed less severity index than it.
Tài liệu tham khảo
Cioli V, Putzolu S, Rossi V, Barcellona SP, Corradino C (1979) The role of direct tissue contact in the protection of gastro-intestinal ulcers by anti-inflammatory drugs in rats. Toxicol Appl Pharmacol 50:283–289
Evans D, Hicks TA, Williamson WRN, Dawson W, Meacockz SCR, Kitchen EA (1996) Synthesis of a group of lH-benzimidazoles and their screening for anti-inflammatory activity. Eur J Med Chem 31:635–642
Foks H, Pancechowska-Ksepko D, Kuzmierkiewicz W, Zwolska Z, Augustynowicz-Kopec E, Janowiec M (2006) Synthesis and tuberculostatic activity of new benzimidazole derivatives. Chem Het Comp 42:611–614
Gavalas A, Kourounakis L, Litina D, Kourounakis P (1991) Anti-inflammatory and immunomodulating effects of the novel agent γ-(2-aminoethylamino)-2-butyrothienone. Ist communication: inhibitory effects on mouse paw edema. Arzneim Forsch/Drug Res 41:423–426
Gund P, Jensen NP (1983) Nonsteroidal antiinflammatory and anti-arthritic drugs. In: Blankley J (ed) Quantitative structure activity relationships of drugs. Academic Press, New York, pp 285–326
Kazimierczuk Z, Upcroft JA, Upcroft P, Górska A, Starooeciak B, Laudy A (2002) Synthesis, antiprotozoal and antibacterial activity of nitro- and halogeno-substituted benzimidazole derivatives. Acta Biochim Pol 49:185–195
Khan SA, Mullick P, Pandit P, Kaushik D (2009) Synthesis of hydrazones derivatives of quinoxalonine-prospective antimicrobial and anti-inflammatory agents. Acta Pol Pharm Drug Res 66:169–172
Mertens A, Muller-Beckmann B, Kampe W, Holck JP, Saal WVD (1987) Nonsteriodal cardiotonics. (2-Pyridyl-6, 7-dihydro-3H, 5H pyrrolo[2,3-f]benzimidazol-6-ones, a novel class of cardiotonic agents. J Med Chem 30:1279–1289
Mullick P, Khan SA, Begum T, Verma S, Kaushik D, Alam O (2009) Synthesis of 1,2,4-triazine derivatives as potential anti-anxiety and anti-inflammatory agents. Acta Pol Pharm Drug Res 66:379–385
Nicholson RM, Murphy JR, Dearden JC (1982) J Pharm Pharmacol 34:106
Preston PN (1980) Benzimidazoles and congeneric tricyclic compounds. Part II. In: Preston PN (ed) Chemistry of heterocyclic compounds. Interscience Publication (John Wiley & Sons, Inc.), New York, pp 1–281
Tsurumi K, Kyuki K, Niwa M, Kokuba S, Fujimura H (1986) Pharmacological investigations of the new anti-inflammatory agent 2-(10, 11-dihydro-10-oxodibenzo[b, f]thiepin-2-yl)propionic acid. Ist communication: inhibitory effects on rat paw edema. Arzneim Forsch/Drug Res 36:1796–1800
Vogel HS (2002) Drug discovery and evaluation (Pharmacological assays), 2nd edn. Springer, Berlin Heidelberg, p 869
Wilheme R, Gdynia M (1972) Gastric mucosal damage induced by non-steroidal anti-inflammatory gents in rats of different ages. Pharmacology 8:32
Winter CA, Risley EA, Nuss GW (1962) Carrageenan induced edema in hind paw of rat as an assay for anti-inflammatory drugs. Proc Soc Exp Biol Med 111:544–547