18212-21-0Relevant articles and documents
Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB
Li, Dongsheng,Liu, Chao,Jiang, Xinhai,Lin, Yuan,Zhang, Jing,Li, Yan,You, Xuefu,Jiang, Wei,Chen, Minghua,Xu, Yanni,Si, Shuyi
, (2020/10/21)
N-(5-Chlorobenzo[d]oxazol-2-yl)-4-methyl-1,2,3-thiadiazole-5-carboxamideox-amide has been identified as a potent inhibitor of Mtb H37Rv, with a minimum inhibitory concentration (MIC) of 0.42 μM. In this study, a series of substituted 2-acylamide-1,3-zole analogues were designed and synthesized, and their anti-Mtb activities were analyzed. In total, 17 compounds were found to be potent anti-Mtb agents, especially against the MDR- and XDR-MTB strains, with MIC values 10 μM. These analogues can inhibit both drug-sensitive and drug-resistant Mtb. Four representative compounds were selected for further profiling, and the results indicate that compound 18 is acceptably safe and has favorable pharmacokinetic (PK) properties. In addition, this compound displays potent activity against Gram-positive bacteria, with MIC values in the range of 1.48–11.86 μM. The data obtained herein suggest that promising anti-Mtb candidates may be developed via structural modification, and that further research is needed to explore other compounds.
Substituted benzo - 1, 3 - [...] compound, its preparation and use
-
Paragraph 0092; 0093; 0094, (2017/04/21)
The invention relates to a substituted benzo-1, 3-miscellaneous azole compound shown in the general formula I, and further relates to a preparation method of the compound and application to the preparation of antituberculosis drugs. The compound provided by the invention has effect not only on mycobacterium tuberculosis sensitive strains, but also on resistant strains which have drug resistance to isoniazid, rifampicin, and other traditional frontline antituberculosis drugs, and is a novel antimycobacterium tuberculosis compound.
guan Huanfa synthetic multi-nitrogen heterocyclic ring sai oxadiazole - 5 - a amidine compounds
-
Paragraph 0049, (2017/07/21)
The invention discloses an N-trisubstituted-1,2,3-thiadiazoles-5-formamidine target compound of which the general formula is TDCA. The N-trisubstituted-1,2,3-thiadiazoles-5-formamidine target compound is obtained from an M compound through a cyclization reaction. The new synthetizing method is high in yield, catalysts are easy to prepare, the catalysts are low in cost, phosphoric waste water is less, and the multi-nitrogen heterocycle thiadiazoles-5-formamidine compound is environment-friendly. (As shown in the Description).