Facile Synthesis, Characterization and Antimicrobial Activity of 2-Alkanamino Benzimidazole Derivatives

Abstract

Benzimidazole derivatives are known to represent a class of medicinally important compounds which are extensively used in drug design and catalysis. A series of 2-substituted benzimidazole derivatives 10a-i was herein synthesized from the reaction of o-phenylenediamine with some amino acids using ameliorable pathway. The chemical structures of the synthesized compounds were confirmed by IR, UV, 1 H-NMR, 13 C-NMR, Mass spectral and analytical data. The compounds were investigated for their antimicrobial activity alongside gentamicin clinical standard. The results showed that this skeletal framework exhibited marked potency as antimicrobial agents. The most active compound was 1H-benzo[d]imidazol-2-yl)methanamine, 10a.

Expeditious Synthesis and Spectroscopic Characterization of 2-Methyl-3-substituted-quinazolin-4(3H)-one Derivatives

“…The C=N imino functionality was present in all compound 8a-q at the stretching vibrational frequencies at region 1588 cm -1 (as found in 8c) to 1575 cm -1 (which was common to compound 8f, 8l, 8g . The C=N reported herein was within the ranged of the C=N of benzimidazole earlier reported in our previous study 2 .…”

“…Hence, in the continuation of our effort on the synthesis of N-heterocyclic motifs 1,2,4 , we have herein achieved expeditious synthesis of 2-methyl-3-substituted quinazoline-4(3H)-one derivatives 8a-q, in a two steps technique. The first step of the synthesis in this present research work, involved the reaction of anthranilic acid with acetic anhydride according to a known procedure reported by Hassan et al 22 .…”

“…Also, most marketed drugs constitute of common structural units of heterocyclic compounds which could also be useful in the synthesis of biologically active agrochemicals 2,3 . For instance, in the pharmaceutical industry, among the top two hundred branded drugs, we have more than 75% of them which have heterocyclic fragments in their structures 4 .…”

Antibacterial Screening of New Synthesis Schiff Base having Benzimidazole Moiety

“…Benzimidazole is a versatile pharmacophore producing a different range of biological activities [2], including analgesic [3] and antiinflammatory [4][5][6]. Benzimidazole derivatives have found the application in different therapeutic areas including, antihypertensive [7], antiviral [8,9], antifungal [10][11][12], anticancer [13][14][15], antitubercular [16,17], antioxidant [18,19], antimicrobial [20][21][22][23], antibacterial [24][25][26]. Benzimidazole derivatives are highly active against several viruses such as HIV, herpes (HSV-1), RNA, influenza and human cytomegalovirus (HCMV) [27].…”

Facile synthesis of N substituted 2 3 5 dinitrophenyl benzimidazole derivatives for antimicrobial investigation

“…Benzimidazole derivatives are crucial structural scaffolds found in diverse libraries of biologically active compounds which are therapeutically useful agents in drug discovery and medicinal research [1]. Numerous compounds containing benzimidazole moieties have been reported to exhibit diverse biological and pharmacological properties which include, but not limited to, antitumor [2], anticancer [3], antimalarial [4], anti-inflammatory [5], antiepileptic [6], antitubercular [7], anti-HIV [8], antihypertensive [9], antimicrobial [10], anthelmintic [11], antioxidant [12] and anti-diabetic [13] activities.…”