Antimicrobial Activity of a New Combination System of Benzimidazole and Various Azoles

Abstract

In the present study a new series of benzimidazole derivatives bearing various (benz)azolylthio moieties were synthesized so as to investigate their antimicrobial activity. Structures of the target compounds (5a-5i) were confirmed by their IR, (1) H-NMR, ES-MS spectral data, and elemental analyses. The synthesized compounds (5a-5i) exhibited poor activity against bacterial strains. On the other hand, antifungal activity of the compounds against Candida species was very significant. Brine-Shrimp lethality assay was performed for determination of toxicity of the compounds. Compounds 5a, 5c, and 5d were evaluated as non-toxic in addition to their attractive antifungal activity. However, the other compounds (5b, e-i) in the series showed toxicity to different extents.

Heterocyclic Synthesis Via Enaminonitriles: One-Pot Synthesis of Some New Pyrazole, Pyrimidine, Pyrazolo[1,5-A]Pyrimidine and Pyrido[2,3-D]Pyrimidine Derivatives

“…It should be noted that the pyrazolo[1,5-a]pyrimidine (21) could be prepared directly fro m (9) and (19) in reflu xing pyrid ine. Attempts to synthesis pyrazolo [3,4-d]-pyrimidine (23) by the reaction of (9) with DMF-DMA failed and only the amid ines (22) were formed wh ich did not cyclize to generate the corresponding (23). All analys is of compounds (21,22,24) are consistent with the proposed structures.…”

“…Attempts to synthesis pyrazolo [3,4-d]-pyrimidine (23) by the reaction of (9) with DMF-DMA failed and only the amid ines (22) were formed wh ich did not cyclize to generate the corresponding (23). All analys is of compounds (21,22,24) are consistent with the proposed structures. The site selectivity in cycloaddition of some nitrogen amb ident nucleophiles with enaminonitrile (6) was also investigate, Thus, reaction of (6) with thiourea in reflu xing ethanol containing catalytic amount of piperid ine afforded a single product for which five isomeric cycloadducts (27), (29),(31),(33) and (35) seemed possible.…”

“…The reaction mixtu re was cooled to room temperature and poured onto ice. The aqueous solution was acidified with hydrochloric acid, forming a solid that was collected by filtration, washed with water several times and recrystallized fro m DM F as pale buff crystals to give (73%, yield) of (21) A mixture of (9) (5 mmo l) and DMFDMA (5 mmo l) in case of (22) or (11 mmo l) in case of (24) in dimethylformamide (25 ml) was stirred at reflu x for 5h., cooled to room temperature and poured onto ice/water. The formed crude solid was collected by filtration, washed with water several times and recrystallized fro m the appropriate solvent.…”

“…It was interesting to synthesis hybrids possessing biological and pharmacological activit ies due to benzimidazo le [16][17][18][19][20][21][22][23][24][25][26][27][28][29] and certain substituted pyrazoles [30][31][32][33][34][35][36][37][38][39][40][41][42][43][44] hoping that this combination may possess a potential analgesic activity along with possible anticancer effect.…”

A comprehensive review in current developments of benzothiazole-based molecules in medicinal chemistry

“…Wang and co-workers reported BTA-2-thiol derivatives and evaluated for their antiproliferative activities on HepG2 and MCF-7 cells by MTT method. Compounds (90,91) exhibited good antitumor activities against the different types of human cancer cell lines in vitro, with IC 50 values ranging from 1.1 to 8.8 mM. The SAR study reveals that chloromethyl could improve significantly the antitumor activity of this series of BTA derivatives [130].…”