One-Pot Green Synthesis and Biological Evaluation of Dimedone-Coupled 2,3-Dihydrofuran Derivatives to Divulge Their Inhibition Potential against Staphylococcal Thioredoxin Reductase Enzyme

被引：0

作者：

Shukla, Manjari ^{[1
]}

Mali, Ghanshyam ^{[2
]}

Sharma, Supriya ^{[2
]}

Maji, Sushobhan ^{[1
]}

Yadav, Vinay Kumar ^{[1
]}

Mishra, Amit ^{[1
]}

Erande, Rohan D. ^{[2
]}

Bhattacharyya, Sudipta ^{[1
]}

机构：

[1] Indian Inst Technol, Dept Biosci & Bioengn, Jodhpur 342037, Rajasthan, India

[2] Indian Inst Technol, Dept Chem, Jodhpur 342037, Rajasthan, India

来源：

ACS OMEGA | 2024年 / 9卷 / 43期

关键词：

4-COMPONENT SYNTHESIS;

D O I：

10.1021/acsomega.4c04325

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

New therapeutic leads are in global demand against multiple drug-resistant Staphylococcus aureus, as presently there is no drug of choice left to treat this pathogen. In the present work, we have designed, synthesized, and in vitro validated dimedone-coupled 2,3-dihydrofuran (DDHF)-based inhibitor scaffolds against Staphylococcal thioredoxin reductase (SaTR), a pivotal drug target enzyme of Gram-positive pathogens. Accordingly, a green multicomponent method that is both efficient and one pot has been optimized to synthesize DDHF derivatives. The synthesized DDHF derivatives were found to inhibit a purified SaTR enzyme. The best inhibitor derivative, DDHF20, inhibits SaTR as a competitive inhibitor for the NADPH binding site at low micromolar concentrations. DDHF20-capped silver nanoparticles are synthesized and characterized, and their bactericidal property has been checked in vitro. Furthermore, detailed in silico-based structure-guided functional studies have been carried out to uncover the plausible mode of action of DDHF20 as a potential anti-Staphylococcal therapeutic lead.

引用

页码：43414 / 43425

页数：12

共 4 条

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