Bioevaluation of quinoline‐4‐carbonyl derivatives of piperazinyl‐benzothiazinones as promising antimycobacterial agents
The quinoline moiety remains a privileged antitubercular (anti‐TB) pharmacophore,
whereas 8‐nitrobenzothiazinones are emerging potent antimycobacterial agents with two …
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
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 …
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 …
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 …
(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 …
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 …
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 …
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 …
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 …
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 …
MTB, and around 100-200 million individuals eventually develop an active TB. To make …