Literature DB >> 21752642

Diversity oriented design of various hydrazides and their in vitro evaluation against Mycobacterium tuberculosis H37Rv strains.

Atul Manvar1, Abhay Bavishi, Ashish Radadiya, Jignesh Patel, Vipul Vora, Narshih Dodia, Kena Rawal, Anamik Shah.   

Abstract

Control and prevention of tuberculosis is a major challenge, as one-third of the world's population is infected with Mycobacterium tuberculosis. The resurgence of tuberculosis and the emergence of multidrug-resistance strains of mycobacteria, necessitate the search for new class of antimycobacterial agents. As a part of investigation of new antitubercular agents in this laboratory, we describe the syntheses of various hydrazides of comarins, quinolones and pyrroles and screening against M. tuberculosis (Mtb) H37(Rv) by using rifampin as a standard drug. Among the designed molecules, the most prominent compounds 2a-g, 4a and 9a showed >90% GI at MIC<6.25 μg/mL. Finally, these studies suggests that compounds 2a-g, 4a and 9a may serve as promising lead scaffolds for further generation of new anti-TB agents.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21752642     DOI: 10.1016/j.bmcl.2011.06.074

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


  9 in total

1.  Bis-spirochromanones as potent inhibitors of Mycobacterium tuberculosis: synthesis and biological evaluation.

Authors:  Ashok Dongamanti; Vikas Kumar Aamate; Mohan Gandhi Devulapally; Srinivas Gundu; Saikrishna Balabadra; Vijjulatha Manga; Perumal Yogeeswari; Dharmarajan Sriram; Sridhar Balasubramanian
Journal:  Mol Divers       Date:  2017-08-24       Impact factor: 2.943

2.  Coumarin-carbazole based functionalized pyrazolines: synthesis, characterization, anticancer investigation and molecular docking.

Authors:  Mrugesh Patel; Nilesh Pandey; Jignesh Timaniya; Paranjay Parikh; Alex Chauhan; Neeraj Jain; Kaushal Patel
Journal:  RSC Adv       Date:  2021-08-13       Impact factor: 4.036

3.  Indole-fused spirochromenes as potential anti-tubercular agents: design, synthesis and in vitro evaluation.

Authors:  Ashok Dogamanti; Pamula Chiranjeevi; Vikas Kumar Aamate; Siva Krishna Vagolu; Dharmarajan Sriram; Sridhar Balasubramanian; Madderla Sarasija
Journal:  Mol Divers       Date:  2020-05-30       Impact factor: 2.943

4.  An expeditious iodine-catalyzed synthesis of 3-pyrrole-substituted 2-azetidinones.

Authors:  Debasish Bandyopadhyay; Jessica Cruz; Ram N Yadav; Bimal K Banik Banik
Journal:  Molecules       Date:  2012-09-28       Impact factor: 4.411

Review 5.  Promising Lead Compounds in the Development of Potential Clinical Drug Candidate for Drug-Resistant Tuberculosis.

Authors:  Saad Alghamdi; Shaheed Ur Rehman; Nashwa Talaat Shesha; Hani Faidah; Muhammad Khurram; Sabi Ur Rehman
Journal:  Molecules       Date:  2020-12-02       Impact factor: 4.411

6.  Synthesis and structure-activity relationship of coumarins as potent Mcl-1 inhibitors for cancer treatment.

Authors:  Yang-Liu Xia; Jing-Jing Wang; Shi-Yang Li; Yong Liu; Frank J Gonzalez; Ping Wang; Guang-Bo Ge
Journal:  Bioorg Med Chem       Date:  2020-11-07       Impact factor: 3.641

7.  A Coumarin-Based Analogue of Thiacetazone as Dual Covalent Inhibitor and Potential Fluorescent Label of HadA in Mycobacterium tuberculosis.

Authors:  Asma Farjallah; Laurent R Chiarelli; Martin Forbak; Giulia Degiacomi; Mathieu Danel; Fernanda Goncalves; Chantal Carayon; Cendrine Seguin; Marco Fumagalli; Monika Záhorszká; Elodie Vega; Souhir Abid; Anna Grzegorzewicz; Mary Jackson; Antonio Peixoto; Jana Korduláková; Maria Rosalia Pasca; Christian Lherbet; Stefan Chassaing
Journal:  ACS Infect Dis       Date:  2021-02-22       Impact factor: 5.084

8.  Combined in Vitro and in Silico Studies for the Anticholinesterase Activity and Pharmacokinetics of Coumarinyl Thiazoles and Oxadiazoles.

Authors:  Aliya Ibrar; Ajmal Khan; Majid Ali; Rizwana Sarwar; Saifullah Mehsud; Umar Farooq; Syed M A Halimi; Imtiaz Khan; Ahmed Al-Harrasi
Journal:  Front Chem       Date:  2018-03-26       Impact factor: 5.221

9.  Synthesis and Structure Insights of Two Novel Broad-Spectrum Antibacterial Candidates Based on (E)-N'-[(Heteroaryl)methylene]adamantane-1-carbohydrazides.

Authors:  Lamya H Al-Wahaibi; Natalia Alvarez; Olivier Blacque; Nicolás Veiga; Aamal A Al-Mutairi; Ali A El-Emam
Journal:  Molecules       Date:  2020-04-22       Impact factor: 4.411

  9 in total

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