75614-54-9Relevant articles and documents
Design, synthesis and evaluation of thiazole based amides for their antitubercular and PknG inhibitory activity
Sharma, Anindra
, p. 624 - 632 (2021/09/28)
A series of thiazole based amides have been designed and synthesized by solution-phase amide coupling of 2-aminothiazole and its derivatives with naturally occurring aromatic and heteroaromatic acids in excellent yield via DIC/HOBt protocol All the compounds have been evaluated for their antitubercular activity against M. tuberculosis virulent strain M. tuberculosis H37Rv and PknG inhibitory activity in the presence and absence of the inhibitors The compounds display moderate to significant PknG inhibitory activity (9.1-15.6% inhibition at 100 μM) as compared to the standard inhibitors and very moderate in vitro antitubercular activities against M. tuberculosis virulent strain M. tuberculosis H37Rv.
Access to Amide from Aldimine via Aerobic Oxidative Carbene Catalysis and LiCl as Cooperative Lewis Acid
Wang, Guanjie,Fu, Zhenqian,Huang, Wei
supporting information, p. 3362 - 3365 (2017/07/13)
Herein, an efficient route to amides from aldimines via aza-Breslow intermediates through aerobic oxidative carbene catalysis with LiCl as a cooperative Lewis acid is described. Many of the obtained N-heteroarylamides feature biological activity. Ambient
Aerobic Copper-Mediated Domino Three-Component Approach to 2-Aminobenzothiazole Derivatives
Castanheiro, Thomas,Suffert, Jean,Gulea, Mihaela,Donnard, Morgan
supporting information, p. 2588 - 2591 (2016/06/15)
An unprecedented three-component reaction involving a 2,2′-diaminodiaryl disulfide, copper cyanide, and an electrophile is described. This transformation is based on an oxidative copper-mediated S-cyanation as a key step and involves a cyanation/cyclization/acylation domino sequence enabling a rapid and efficient synthesis of diversely substituted 2-aminobenzothiazole derivatives. Notably, this reaction proceeds via an original mechanism involving an intermolecular migration of the acyl group.