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Abstract

The synthesis of benzimidazoles derivative involves subsequent synthesis of 4-(2-chloro-ethoxy)-benzaldehyde, 4 methyl benzaldehyde followed by benzimidazoles derivative by reaction between amines derivatives and ophenylenediamine in dimethyl farmamide (DMF) as solvent in the presence of iodine as a catalyst. Iodine is a commercial and environmentally benign catalyst. The yield of all benzimidazole derivatives was found to be in the range of 75-94%. The purity of the compounds was ascertained by melting point and TLC. The synthesized compounds were characterized by using IR, 1 H NMR, and MASS spectral data together with elemental analysis. The synthesized benzimidazole compounds were screened for analgesic and anticonvulsant activity in albino rat (100-200gm) by using Writhing test and maximal electroshock (MES). Out of all compound studied only PS-3, PS-4, PS-5 and PS-6 showed significant analgesic activities and response against MES test.

Synthesis, Antibacterial, and Anti HepG2 Cell Line Human Hepatocyte Carcinoma Activity of Some New Potentially Benzimidazole-5-(Aryldiazenyl)Thiazole Derivatives

“…The promising therapeutic potential of benzimidazole derivatives could be traced back to 1944and Woolley, who speculated that benzimidazole could act similar to purines to elicit some biological responses [1]. The optimization of substituents around the benzimidazole nucleus resulted in many drugs with useful therapeutic activities such asmethyl (5-benzoyl-1 H -benzimidazol-2-yl)carbamate (mebendazole) as parasitic worm infestations, ( RS )-2-([3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl)-1 H -benzo[d]imidazole (lansoprazole) and ( RS )-6-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl)methylsulfinyl]-1 H -benzo[d]imidazole (pantoprazole) as proton pump inhibitors; 1-[(4-fluorophenyl)methyl]- N -[1-[2-(4-methoxyphenyl)ethyl]-4-piperidyl]benzoimidazol-2-amine (astemizole) as antihistaminic[2]; triazole-thiazol derivatives as analgesic [3,4,5,6]; 2-[2-(4-chlorophenyl)-1,3-benzoxazol-5-yl]propanoic acid (benoxaprofen) as anti-inflammatory [4,5,6,7]; methyl [5-(propylthio)-1 H -benzoimidazol-2-yl]carbamate (albendazole) as antimicrobials [8,9,10]; 1-(isopropylsulfonyl)-6-(1-phenylprop-1-en-1-yl)-1 H -benzo[d]imidazol-2-amine (enviradine) as antiviral [11,12]; antitubercular [13,14]; 4-(1 H -1,3-benzodiazol-2-yl)-1,3-thiazole(thiabendazole) as antihelmenthic [15,16,17,18]; picoline-imidazoles as anticonvulsant [19,20];4-[5-[bis(2-chloroethyl)amino]-1-methylbenzimidazol-2-yl]butanoic acid (bendamustine) as anticancer [21,22,23]; 5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methanesulfinyl]-1 H -benzimidazole (omeprazole) as antiulcer [24,25]; angiotension-II receptor antagonists [26]; 2-ethoxy-1-([4-[2-(2 H -1,2,3,4-tetrazol-5-yl)phenyl]phenyl]methyl)-1 H -1,3-benzodiazole-7-carboxylic acid (candesarten) as antihypertensive [27]; alkynyl benzimidazoles as modulators of metabotropic glutamate receptors [3,16,17,18,24,28,29,30]; and N -ribosyl-dimethyl benzimidazole as an axial ligand for cobalt in vitamins […”