Synthesis, antimicrobial evaluation, molecular docking, and drug-likeness assessment of novel phenothiazine chromene hybrid compounds

新型吩噻嗪色烯杂合化合物的合成、抗菌活性评价、分子对接和类药性评价

阅读:3

Abstract

By carefully hybridizing with scaffolds generated from chromene, pyranochromene, and cyanoacetamide, a novel class of phenothiazine-based heterocycles was created. IR, NMR, and MS investigations were used to establish the structural integrity of each molecule. Several derivatives showed considerable inhibitory activity, especially compounds 4, 7, and 10, which had MIC values ranging from 3.9 to 15.6 µg/mL against both Gram-positive and Gram-negative bacteria, according to the antimicrobial assessment. The majority of compounds met Lipinski's criteria, indicating favorable oral bioavailability, according to the drug-likeness assessment. Significant binding affinity was shown by molecular docking against Staphylococcus aureus β-lactamase (PDB: 3G7B). Compound 7 had the best docking score (-5.99 kcal/mol), followed by compound 4 (-5.86 kcal/mol), which was supported by important hydrophobic and hydrogen-bonding interactions with Asp73, Arg76, and Lys103. These findings demonstrate the possibility of phenothiazine-chromene hybrids as viable options for creating novel antimicrobial medicines that effectively combat infections that are resistant to multiple drugs.

特别声明

1、本页面内容包含部分的内容是基于公开信息的合理引用;引用内容仅为补充信息,不代表本站立场。

2、若认为本页面引用内容涉及侵权,请及时与本站联系,我们将第一时间处理。

3、其他媒体/个人如需使用本页面原创内容,需注明“来源:[生知库]”并获得授权;使用引用内容的,需自行联系原作者获得许可。

4、投稿及合作请联系:info@biocloudy.com。