Literature DB >> 21657948

Design, synthesis and SAR exploration of hybrid 4-chlorophenylthiazolyl-s-triazine as potential antimicrobial agents.

Prashant Gahtori1, Surajit K Ghosh.   

Abstract

Two novel series of hybrid class 4-chlorophenylthiazole-s-triazine were synthesized via nucleophilic substitution of 2,4,6-trichloro-1,3,5-triazine with distinguished alkenyl/alkyl/aryl/hetero alkyl-aryl amino and mercapto nucleophiles under nitrogen atmosphere. We identified that the spectrums of antibacterial activity of all tested compounds reveal promising and significant inhibition of gram-positive and gram-negative micro-organisms and the most active compounds, 31d and 32d, were found to be non-toxic in preliminary cytotoxicity assay. We also report that the Molinspiration and Osiris Property Explorer calculations have found a new lead 32d, which binds preferentially to the nuclear receptor to exhibit antibacterial potency.

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Year:  2011        PMID: 21657948     DOI: 10.3109/14756366.2011.587418

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN: 1475-6366            Impact factor:   5.051


  5 in total

Review 1.  Recent development of leucyl-tRNA synthetase inhibitors as antimicrobial agents.

Authors:  Panpan Zhang; Shutao Ma
Journal:  Medchemcomm       Date:  2019-05-27       Impact factor: 3.597

2.  Synthesis of novel star-shaped molecules based on a 1,3,5-triazine core linked to different heterocyclic systems as novel hybrid molecules.

Authors:  Hadeer M Diab; Mostafa E Salem; Ismail A Abdelhamid; Ahmed H M Elwahy
Journal:  RSC Adv       Date:  2020-12-14       Impact factor: 4.036

3.  Hybrid phenylthiazole and 1,3,5-triazine target cytosolic leucyl-tRNA synthetase for antifungal action as revealed by molecular docking studies.

Authors:  Udaya Pratap Singh; Hans Raj Bhat; Prashant Gahtori; Ramendra K Singh
Journal:  In Silico Pharmacol       Date:  2013-02-12

4.  Utilisation of Home Laundry Effluent (HLE) as a catalyst for expeditious one-pot aqueous phase synthesis of highly functionalised 4-thiazolidinones.

Authors:  Udaya Pratap Singh; Hans Raj Bhat; Mukesh Kumar Kumawat; Ramendra K Singh
Journal:  Springerplus       Date:  2013-09-16

5.  Design and Synthesis of New 1,3,5-Trisubstituted Triazines for the Treatment of Cancer and Inflammation.

Authors:  Boulos Zacharie; Shaun D Abbott; Jean-Simon Duceppe; Lyne Gagnon; Brigitte Grouix; Lilianne Geerts; Liette Gervais; François Sarra-Bournet; Valérie Perron; Nicole Wilb; Christopher L Penney; Pierre Laurin
Journal:  ChemistryOpen       Date:  2018-09-21       Impact factor: 2.911

  5 in total

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