Literature DB >> 28587823

Identification and synthesis of novel inhibitors of mycobacterium ATP synthase.

Yogesh B Surase1, Kirandeep Samby2, Sagar R Amale2, Ruchi Sood2, Kedar P Purnapatre2, Pawan K Pareek2, Biswajit Das2, Kamna Nanda2, Subodh Kumar3, Ashwani K Verma2.   

Abstract

A non-diaryl quinoline scaffold 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one was identified by screening of diverse set of compounds against M. smegmatis ATP synthase. Herein, we disclose our efforts to develop the structure activity relationship against Mycobacterium tuberculosis (Mtb.H37Rv strain) around the identified hit 1. A scaffold hopping approach was used to identify compounds 14a, 14b and 24a with improved activity against MTb.H37Rv.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  ATP synthase; Anti-tubercular; Mtb; Non-darq; TMC207

Mesh:

Substances:

Year:  2017        PMID: 28587823     DOI: 10.1016/j.bmcl.2017.05.081

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Comparing and Validating Machine Learning Models for Mycobacterium tuberculosis Drug Discovery.

Authors:  Thomas Lane; Daniel P Russo; Kimberley M Zorn; Alex M Clark; Alexandru Korotcov; Valery Tkachenko; Robert C Reynolds; Alexander L Perryman; Joel S Freundlich; Sean Ekins
Journal:  Mol Pharm       Date:  2018-04-26       Impact factor: 4.939

2.  Identification of Substituted Amino Acid Hydrazides as Novel Anti-Tubercular Agents, Using a Scaffold Hopping Approach.

Authors:  Alistair K Brown; Ahmed K B Aljohani; Fatimah M A Alsalem; Joseph L Broadhead; Jason H Gill; Yucheng Lu; Jonathan D Sellars
Journal:  Molecules       Date:  2020-05-21       Impact factor: 4.411

3.  A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line.

Authors:  Meltem Tan Uygun; Karina Amudi; İrem Doğan Turaçlı; Nurettin Menges
Journal:  Mol Divers       Date:  2021-01-02       Impact factor: 2.943

  3 in total

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