Anti-tubercular activity and molecular docking studies of indolizine derivatives targeting mycobacterial InhA enzyme

Anti-tubercular activity and molecular docking studies of indolizine derivatives targeting mycobacterial InhA enzyme

A series of 1,2,3-trisubstituted indolizines (2a–2f, 3a–3d, and 4a–4c) were screened for in vitro whole-cell anti-tubercular activity against the susceptible H37Rv and multidrug-resistant (MDR) Mycobacterium tuberculosis (MTB) strains. Compounds 2b–2d, 3a–3d, and 4a–4c were active against the H37Rv-...

Full description

Bibliographic Details
Main Authors:	Katharigatta N. Venugopala, Sandeep Chandrashekharappa, Pran Kishore Deb, Christophe Tratrat, Melendhran Pillay, Deepak Chopra, Nizar A. Al-Shar’i, Wafa Hourani, Lina A. Dahabiyeh, Pobitra Borah, Rahul D. Nagdeve, Susanta K. Nayak, Basavaraj Padmashali, Mohamed A. Morsy, Bandar E. Aldhubiab, Mahesh Attimarad, Anroop B. Nair, Nagaraja Sreeharsha, Michelyne Haroun, Sheena Shashikanth, Viresh Mohanlall, Raghuprasad Mailavaram
Format:	Article
Language:	English
Published:	Taylor & Francis Group 2021-01-01
Series:	Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:	indolizine mycobacterium tuberculosis inha docking x-ray crystal structure
Online Access:	http://dx.doi.org/10.1080/14756366.2021.1919889

Similar Items

Crystallography, Molecular Modeling, and COX-2 Inhibition Studies on Indolizine Derivatives
by: Katharigatta N. Venugopala, et al.
Published: (2021-06-01)

Methyl 3-(Quinolin-2-yl)indolizine-1-carboxylate
by: Roumaissa Belguedj, et al.
Published: (2015-12-01)

Novel Series of Methyl 3-(Substituted Benzoyl)-7-Substituted-2-Phenylindolizine-1-Carboxylates as Promising Anti-Inflammatory Agents: Molecular Modeling Studies
by: Katharigatta N. Venugopala, et al.
Published: (2019-10-01)

Sydnone C-4 heteroarylation with an indolizine ring via Chichibabin indolizine synthesis
by: Florin Albota, et al.
Published: (2016-11-01)

Synthesis and electrochemical characterization of substituted indolizine carboxylates
by: Soare Maria-Laura, et al.
Published: (2013-01-01)

Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors
by: Monica-Cornelia Sardaru, et al.
Published: (2020-01-01)

Antimycobacterial activity of nitrogen heterocycles derivatives: 7-(pyridine-4-yl)-indolizine derivatives. Part VII8–12
by: Anda-Mihaela Olaru, et al.
Published: (2017-01-01)

Indolizines and Their Hetero/Benzo Derivatives in Reactions of [8+2] Cycloaddition
by: Eugene V. Babaev, et al.
Published: (2021-04-01)

Microwave-Assisted Synthesis of Fluorescent Pyrido[2,3-<i>b</i>]indolizines from Alkylpyridinium Salts and Enaminones
by: Ekaterina A. Sokolova, et al.
Published: (2020-09-01)

Chiral Methyl 7,8,9-Trichloro-6,7,8,9-tetrahydro-5-oxopyrido-[2,3-a]indolizine-10-carboxylates (OPIC)
by: Sghir Elkadiri, et al.
Published: (2003-02-01)

Selective synthesis and reactivity of indolizines
by: González Soria, María José
Published: (2019)

Novel One-Pot Green Synthesis of Indolizines Biocatalysed by Candida antarctica Lipases
by: Simon Bonte, et al.
Published: (2013-02-01)

Molecular Docking and Chemical Analysis of Alcohol Compounds (C16-C20) Bound to InhA Receptors as Mycobactericidal Candidates
by: Muhammad Iqbal Shihab, et al.
Published: (2020-05-01)

Estudo da resistência à isoniazida em Mycobacterium tuberculosis: uma caracterização estrutural e biofísica de mutações missense no gene inhA identificados a partir de isolados clínicos.
by: Pacheco, Sair Maximo Chavez
Published: (2018)

Insilico Analysis of Phytoconstituents from Allium sativum as Potential Inhibitors of Inha in Mycobacterium tuberculosis
by: Rmaraj Kannan, et al.

Whole-Cells of <i>Yarrowia lipolyti</i>ca Applied in “One Pot” Indolizine Biosynthesis
by: Andreea Veronica Botezatu (Dediu), et al.
Published: (2020-06-01)

Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor
by: María Martínez-Hoyos, et al.
Published: (2016-06-01)

Fluorescent Indolizine-b-Cyclodextrin Derivatives for the Detection of Volatile Organic Compounds
by: Sophie Fourmentin, et al.
Published: (2008-06-01)

A Novel Indolizine Derivative Induces Apoptosis Through the Mitochondria p53 Pathway in HepG2 Cells
by: Yushuang Liu, et al.
Published: (2019-07-01)

Counter Anion Effect on the Photophysical Properties of Emissive Indolizine-Cyanine Dyes in Solution and Solid State
by: Jacqueline N. Gayton, et al.
Published: (2018-11-01)

The Value of the inhA Mutation Detection in Predicting Ethionamide Resistance Using Melting Curve Technology
by: Song Y, et al.
Published: (2021-01-01)

Contribution of katG, ahpC and inhA mutations to the detection of isoniazid-resistant Mycobacterium tuberculosis isolates from Lebanon and Syria
by: F Dabboussi, et al.
Published: (2015-01-01)

Indolizines and pyrrolo[1,2-c]pyrimidines decorated with a pyrimidine and a pyridine unit respectively
by: Marcel Mirel Popa, et al.
Published: (2015-06-01)

Mutations of rpoB, katG, inhA and ahp genes in rifampicin and isoniazid-resistant Mycobacterium tuberculosis in Kyrgyz Republic
by: Jainagul Isakova, et al.
Published: (2018-03-01)

In Vitro Antimycobacterial Activity and Physicochemical Characterization of Diaryl Ether Triclosan Analogues as Potential InhA Reductase Inhibitors
by: Tarek S. Ibrahim, et al.
Published: (2020-07-01)

New InhA Inhibitors Based on Expanded Triclosan and <i>Di</i>-Triclosan Analogues to Develop a New Treatment for Tuberculosis
by: Sarentha Chetty, et al.
Published: (2021-04-01)

Mutations in rpoB and katG genes and the inhA operon in multidrug-resistant Mycobacterium tuberculosis isolates from Zambia
by: Eddie S. Solo, et al.
Published: (2020-09-01)

Computational, crystallographic studies, cytotoxicity and anti-tubercular activity of substituted 7-methoxy-indolizine analogues.
by: Katharigatta Narayanaswamy Venugopala, et al.
Published: (2019-01-01)

Virtual screeningÂde possÃveis inibidores daÂtrans-enoil-ACP-redutase deÂMycobacterium tuberculosis.
by: Sergio Xavier Barbosa AraÃjo
Published: (2013)

Crystal structure of ethyl 5′′-fluoro-2′′,3-dioxo-6′,7′,8′,8a'-tetrahydro-2′H,3H,5′H-dispiro[benzo[b]thiophene-2,1′-indolizine-3′,3′′-indoline]-2′-carboxylate
by: R. Raja, et al.
Published: (2015-03-01)

An environmentally benign cascade reaction of 1,2,3-indantriones with ethyl 2-(pyridine-2-yl)acetates for site-selective synthesis of 5H-isochromeno[4,3-b]indolizin-5-ones
by: Haodan He, et al.
Published: (2021-02-01)

FLUORESCENT N-HETEROCYCLES VIA ONE-POT TANDEM REACTIONS
by: Rodica Dinica, et al.
Published: (2009-12-01)

Facile Synthesis of Heterocycles via 2-Picolinium Bromide and Antimicrobial Activities of the Products
by: Elham S. Darwish
Published: (2008-05-01)

Investigation of the Pyridinium Ylide—Alkyne Cycloaddition as a Fluorogenic Coupling Reaction
by: Simon Bonte, et al.
Published: (2016-03-01)

KF/Al2O3 as a Recyclable Basic Catalyst for 1,3-Dipolar Cycloaddition Reaction: Synthesis of Indolizine-1-Carbonitrile Derivatives
by: Abaszadeh Mehdi, et al.
Published: (2017-07-01)

Cytotoxicity and Antimycobacterial Properties of Pyrrolo[1,2-<i>a</i>]quinoline Derivatives: Molecular Target Identification and Molecular Docking Studies
by: Katharigatta N. Venugopala, et al.
Published: (2020-05-01)

Change in prevalence and molecular characteristics of isoniazid-resistant tuberculosis over a 10-year period in China
by: Fengmin Huo, et al.
Published: (2019-08-01)

N-[2-(1H-Indol-3-yl)-1-(5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)ethyl]-4-methylbenzenesulfonamide
by: Nikil Purushotham, et al.
Published: (2018-07-01)

Identification and validation of the mode of action of the chalcone anti-mycobacterial compounds
by: B. Anagani, et al.
Published: (2020-12-01)

Computational approach to understanding the mechanism of action of isoniazid, an anti-TB drug
by: Lingaraja Jena, et al.
Published: (2014-01-01)