3D QSAR-based design and liquid phase combinatorial synthesis of 1,2-disubstituted benzimidazole-5-carboxylic acid and 3-substituted-5H-benzimidazo[1,2-d][1,4]benzodiazepin-6(7H)-one derivatives as anti-mycobacterial agents

Abstract

Novel benzimidazole-5-carboxylic acid and benzodiazepin-6(7H)-one derivatives as anti-mycobacterial agents.

Recent advancement in drug development of nitro(NO2)‐heterocyclic compounds as lead scaffolds for the treatment of Mycobacterium tuberculosis

“…In addition, both nitrophenyl-based triazole derivatives (17-18) displayed effects against fungi, exhibiting MIC values of 6.25 μg/ml (17) and >100.0 μg/ml (18) against A. niger and 3.12 μg/ml (17) and >100.0 μg/ml (18) against C. albicans (Goud et al, 2017) (Yadav et al, 2018). Four novel N-cinnamyl-substituted isatin analogues (8-12) (Kumar et al, 2014) (Sitwala et al, 2019). A novel m-amidophenol-based derivative (14) (Zhang et al, 2018) F I G U R E 5 New 2-aminothiazole-based nitro analogues (15-16) (Kesicki et al, 2016) F I G U R E 6 Novel nitrophenyl-based triazolyl xanthenone analogues (17-18) (Goud et al, 2017).…”

“…Sitwala et al (2019) synthetized and characterized a series of new 3‐substituted‐5 H ‐benzimidazo[1,2‐ d ][1,4]‐benzodiazepin‐6(7 H )‐one analogues that presented anti‐ Mtb activity (H 37 Rv). Among these analogues, compound ( 13 ) displayed a promising MIC value of 0.195 μM (Figure 4; Sitwala et al, 2019). A cytotoxicity assay showed that compound ( 13 ) was not cytotoxic at 10 μM against THP‐1 macrophage cells (Sitwala et al, 2019).…”

“…Among these analogues, compound ( 13 ) displayed a promising MIC value of 0.195 μM (Figure 4; Sitwala et al, 2019). A cytotoxicity assay showed that compound ( 13 ) was not cytotoxic at 10 μM against THP‐1 macrophage cells (Sitwala et al, 2019). Zhang et al (2018) displayed a series of m ‐amidophenol‐based analogues.…”

“…A new 3‐substituted‐5 H ‐benzimidazoij1,2‐ d ][1,4]‐benzodiazepin‐6(7H)‐one analogue ( 13 ) (Sitwala et al, 2019). A novel m ‐amidophenol‐based derivative ( 14 ) (Zhang et al, 2018)…”

Microwave-Assisted Copper(II)-Catalyzed Cascade Cyclization of 2-Propargylamino/Oxy-Arylaldehydes andO-Phenylenediamines: Access to Densely Functionalized Benzo[f]Imidazo[1,2-d][1,4]Oxazepines and Benzo[f]Imidazo[1,2-d][1,4]Diazepines

“…Besides, clozapine VII is a psychiatric medication, primarily used for the treatment of schizophrenia and schizoaffective disorders . Owing to the wide spectrum of biological and medicinal applications of benzoxazepines and benzodiazepines, synthetic chemists seek to develop elegant and operationally simple synthetic approaches for their syntheses. , …”