Bioevaluation of quinoline‐4‐carbonyl derivatives of piperazinyl‐benzothiazinones as promising antimycobacterial agents

SK Sahoo, SNR Gajula, MN Ahmad, G Kaul… - Archiv der …, 2022 - Wiley Online Library
The quinoline moiety remains a privileged antitubercular (anti‐TB) pharmacophore,
whereas 8‐nitrobenzothiazinones are emerging potent antimycobacterial agents with two …

Exploration of isoxazole‐carboxylic acid methyl ester based 2‐substituted quinoline derivatives as promising antitubercular agents

S Kumar Sahoo, M Naiyaz Ahmad, G Kaul… - Chemistry & …, 2022 - Wiley Online Library
In pursuit of potent anti‐TB agents active against drug resistant tuberculosis (DR‐TB), herein
we report synthesis and bio‐evaluation of a new series of isoxazole‐carboxylic acid methyl …

New quinoline–urea–benzothiazole hybrids as promising antitubercular agents: synthesis, in vitro antitubercular activity, cytotoxicity studies, and in silico ADME …

R Moodley, C Mashaba, GH Rakodi, NB Ncube… - Pharmaceuticals, 2022 - mdpi.com
A series of 25 new benzothiazole–urea–quinoline hybrid compounds were synthesized
successfully via a three-step synthetic sequence involving an amidation coupling reaction as …

Synthesis of novel morpholine, thiomorpholine and N-substituted piperazine coupled 2-(thiophen-2-yl) dihydroquinolines as potent inhibitors of Mycobacterium …

SK Marvadi, VS Krishna, D Sriram… - European Journal of …, 2019 - Elsevier
A series of novel morpholine, thiomorpholine and N-substituted piperazine coupled 2-
(thiophen-2-yl) dihydroquinolines 7a–p was designed and synthesized from 2-acetyl …

Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines

CRM Asquith, N Fleck, CD Torrice, DJ Crona… - Bioorganic & medicinal …, 2019 - Elsevier
We screened a series of 4-anilinoquinolines and 4-anilinoquinazolines and identified novel
inhibitors of Mycobacterium tuberculosis (Mtb). The focused 4-anilinoquinoline/quinazoline …

Design, synthesis and antitubercular activity of novel N-(amino) piperazinyl benzothiazinones with improved safety

A Wang, N Du, H Song, Y Zhang, X Zhong, J Wu… - European Journal of …, 2023 - Elsevier
Tuberculosis (TB), caused by Mycobacterium tuberculosis (MTB) remains a major global
health problem and new therapeutic antitubercular agents are urgent needed. Among the …

Design, synthesis and biological activity of N-(amino) piperazine-containing benzothiazinones against Mycobacterium tuberculosis

A Wang, S Xu, Y Chai, G Xia, B Wang, K Lv… - European Journal of …, 2021 - Elsevier
A series of novel benzothiazinone derivatives containing a N-(amino) piperazine moiety,
based on the structure of WAP-1902 discovered in our lab, were designed and synthesized …

Identification of benzothiazinones containing 2-benzyl-2, 7-diazaspiro [3.5] nonane moieties as new antitubercular agents

A Wang, C Ma, Y Chai, X Liu, K Lv, L Fu, B Wang… - European Journal of …, 2020 - Elsevier
A series of new benzothiazinone derivatives containing a symmetric 2-benzyl-2, 7-
diazaspiro [3.5] nonane moiety, based on the structure of LK02 discovered in our lab, were …

Identification of novel benzothiopyranones with ester and amide motifs derived from active metabolite as promising leads against Mycobacterium tuberculosis

P Li, B Wang, L Fu, K Guo, C Ma, B Wang, Z Lin… - European Journal of …, 2021 - Elsevier
We reported three distinct series of novel benzothiopyranones, derived from an active
metabolite (M-1) of anti-TB agent 6b. These small molecules were evaluated for their …

Recent advances of 2-Quinolone-based derivatives as anti-tubercular agents

X Liu, J Deng, Z Xu, ZS Lv - Anti-Infective Agents, 2018 - ingentaconnect.com
The WHO has estimated that one-fourth of the world's population harbor a latent infection by
MTB, and around 100-200 million individuals eventually develop an active TB. To make …