Literature DB >> 34392175

Mycobacterium enoyl acyl carrier protein reductase (InhA): A key target for antitubercular drug discovery.

Mayuri S Prasad1, Ritesh P Bhole2, Pramod B Khedekar3, Rupesh V Chikhale4.   

Abstract

Enoyl acyl carrier protein reductase (InhA) is a key enzyme involved in fatty acid synthesis mainly mycolic acid biosynthesis that is a part of NADH dependent acyl carrier protein reductase family. The aim of the present literature is to underline the different scaffolds or enzyme inhibitors that inhibit mycolic acid biosynthesis mainly cell wall synthesis by inhibiting enzyme InhA. Various scaffolds were identified based on the screening technologies like high throughput screening, encoded library technology, fragment-based screening. The compounds studied include indirect inhibitors (Isoniazid, Ethionamide, Prothionamide) and direct inhibitors (Triclosan/Diphenyl ethers, Pyrrolidine Carboxamides, Pyrroles, Acetamides, Thiadiazoles, Triazoles) with better efficacy against drug resistance. Out of the several scaffolds studied, pyrrolidine carboxamides were found to be the best molecules targeting InhA having good bioavailability properties and better MIC. This review provides with a detailed information, analysis, structure activity relationship and useful insight on various scaffolds as InhA inhibitors.
Copyright © 2021. Published by Elsevier Inc.

Entities:  

Keywords:  Enoyl acyl carrier protein reductase (InhA); INH-NAD adduct; Kat G; Multi-drug resistant TB; Tuberculosis

Mesh:

Substances:

Year:  2021        PMID: 34392175     DOI: 10.1016/j.bioorg.2021.105242

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  2 in total

Review 1.  Advances in Key Drug Target Identification and New Drug Development for Tuberculosis.

Authors:  Jie Mi; Wenping Gong; Xueqiong Wu
Journal:  Biomed Res Int       Date:  2022-02-25       Impact factor: 3.411

Review 2.  Overcoming Mycobacterium tuberculosis through small molecule inhibitors to break down cell wall synthesis.

Authors:  Wenbin Kuang; Haolin Zhang; Xiao Wang; Peng Yang
Journal:  Acta Pharm Sin B       Date:  2022-04-27       Impact factor: 14.903

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.