Literature DB >> 25534154

Design, Synthesis, and Biological Evaluation of 1,4-dihydropyridine Derivatives as Potent Antitubercular Agents.

Nisheeth C Desai1, Amit R Trivedi1, Hardik C Somani1, Kandarp A Bhatt1.   

Abstract

A series of novel 1,4-dihydropyridine-3,5-dicarbamoyl derivatives bearing an imidazole nucleus at C-4 position were synthesized in excellent yields via multicomponent Hantzsch reaction. The newly synthesized compounds were characterized by IR, (1) H NMR, (13) C NMR, and mass spectroscopy. The synthesized compounds 3a-p were screened for antitubercular activity. Among all the screened compounds, compounds 3j and 3m showed most prominent activity against Mycobacterium tuberculosis with minimum inhibitory concentration of 0.02 μg/mL and SI > 500, making it more potent than first-line antitubercular drug isoniazid. In addition, these compounds displayed relatively low cytotoxicity.
© 2014 John Wiley & Sons A/S.

Entities:  

Keywords:  1,4-Dihydropyridines; Mycobacterium tuberculosis; antimycobacterial activity; imididazoles; tuberculosis

Mesh:

Substances:

Year:  2015        PMID: 25534154     DOI: 10.1111/cbdd.12502

Source DB:  PubMed          Journal:  Chem Biol Drug Des        ISSN: 1747-0277            Impact factor:   2.817


  5 in total

1.  1,4-Dihydropyridine as a Promising Scaffold for Novel Antimicrobials Against Helicobacter pylori.

Authors:  Andrés González; Javier Casado; Miyase Gözde Gündüz; Brisa Santos; Adrián Velázquez-Campoy; Cristina Sarasa-Buisan; María F Fillat; Milagrosa Montes; Elena Piazuelo; Ángel Lanas
Journal:  Front Microbiol       Date:  2022-05-25       Impact factor: 6.064

2.  Ionic Liquid Solvation versus Catalysis: Computational Insight from a Multisubstituted Imidazole Synthesis in [Et2NH2][HSO4].

Authors:  Yusif Abdullayev; Vagif Abbasov; Lucas C Ducati; Avtandil Talybov; Jochen Autschbach
Journal:  ChemistryOpen       Date:  2016-08-17       Impact factor: 2.911

3.  Facile one-pot four-component synthesis of 3,4-dihydro-2-pyridone derivatives: novel urease inhibitor scaffold.

Authors:  Arash Modarres Hakimi; Negar Lashgari; Shabnam Mahernia; Ghodsi Mohammadi Ziarani; Massoud Amanlou
Journal:  Res Pharm Sci       Date:  2017-10

4.  Design, synthesis and evaluation of cytotoxic, antimicrobial, and anti-HIV-1 activities of new 1,2,3,4-tetrahydropyrimidine derivatives.

Authors:  Nima Razzaghi-Asl; Mahsa Kamrani-Moghadam; Behzad Farhangi; Rouhollah Vahabpour; Rezvan Zabihollahi; Saghi Sepehri
Journal:  Res Pharm Sci       Date:  2019-03-08

5.  Four-Component Fusion Protocol with NiO/ZrO2 as a Robust Recyclable Catalyst for Novel 1,4-Dihydropyridines.

Authors:  Sandeep V H S Bhaskaruni; Suresh Maddila; Werner E van Zyl; Sreekantha B Jonnalagadda
Journal:  ACS Omega       Date:  2019-12-05
  5 in total

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