Synthesis, antifungal and antioxidant screening of some novel benzimidazole derivatives

Abstract

Some novel benzimidazole derivatives were synthesized and their in vitro effects on rat liver microsomal NADPHdependent lipid peroxidation (LP) level, ethoxyresorufin O-deethylase (EROD) and antifungal activities were determined. A significant decrease in male rat liver microsomal LP level was noted by compounds 4c (52%), 4e (58%) and 4h (43%) at 10 23 M concentration. Compounds 4c (100.0%), 4h (100.0%), 5c (98.0%) and 5h (100.0%) inhibited the microsomal ethoxyresorufin O-deethylase (EROD) enzyme activity better than that of the specific inhibitor caffeine (85%). Among these compounds, only compounds 4b and 4h exhibited moderate activity against C.albicans whereas the others had weak effects.

Structure activity relationship (SAR) study of benzimidazole scaffold for different biological activities: A mini-review

“…Even some of the derivatives of benzimidazole have been clinically approved as summarized in Fig.1, like albendazole, mebendazole, thiabendazole as antihelmintics; omeprazole, lansoprazole, pantoprazole as proton pump inhibitors; astemizole as antihistaminic; enviradine as antiviral; candesarten cilexitil and telmisartan as antihypertensives and many lead compounds in a wide range of other therapeutic areas. Reported literature have shown the various substituted derivatives of benzimidazole nucleus exhibiting remarkable biological activity as antitumor/antiproliferative/anticancer activity [3][4][5][6][7][8][9][10][11][12][13][14], antimicrobial including anti-HIV [15][16][17][18][19], antioxidant [20][21][22][23] and cysticidal activities [24]. …”

Structural, spectral, thermal and biological studies on (Z)-N-benzoyl-N′-(2-oxo-2-(phenylamino)acetyl)carbamohydrazonothioic acid (H2PABT) and its Cd(II), Hg(II), Zn(II) and U(VI)O22+ complexes

“…This type of substituted thiosemicarbazides is an important class of intermediate used for the synthesis of five membered nitrogen-sulfur or nitrogen-oxygen heterocyclic compounds [1][2][3]. The chemistry of thiosemicarbazide complexes has received much attention owing to their medicinal properties [4,5] and their biological effects which include anti-inflammatory [6], antimycobacterial [7], antimicrobial [8], and antifungal [9]. In continuation of our previous work [11][12][13] ,we report herein the synthesis of Cd(II), Hg(II), Zn(II) and U(VI)O 2 2+ complexes derived from ligand namely, (Z)-N-benzoyl-N'-(2-oxo-2-(phenylamino)acetyl)carbamohydrazono-thioic acid (H 2 PABT).…”

Synthesis, antimicrobial and antiviral activity of substituted benzimidazoles

“…Numerous biological activities and functions have been described for benzimidazole nucleus viz. antihypertensive [9], antifungal [10], antioxidant [11], antiviral [12] and topoisomerase inhibitory [13] activities. Literature reports revealed that the benzimidazole derivatives also possessed antiviral activity against various strains of pathogenic viruses viz.…”