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Literature DB >> 23960775

Synthesis, SAR and antibacterial activity of hybrid chloro, dichloro-phenylthiazolyl-s-triazines.

Prashant Gahtori¹, Surajit Kumar Ghosh, Brijesh Singh, Udaya Pratap Singh, Hans Raj Bhat, Archana Uppal.

Abstract

A series of hybrid novel chloro (1a-9a) and dichloro (10b-18b) phenylthiazolyl-s-triazine were synthesized and subsequently subjected to their antibacterial activity against three gram positive viz. Lactobacillus casei (NCIM-2651); Bacillus cereus (NCIM-2458); Staphylococcus aureus (NCIM-2120) and three gram negative viz Salmonella typhimurium (NCIM-2501); Escherichia coli (NCIM-2065); Klebsiella aerogenes (NCIM-2098). The SAR studies around the lead compound revealed that introduction of electron withdrawing groups and amino (-NH-) and mercapto (-S-) linker bridge seemed more promising towards antibacterial activity. Moreover, the virtual Molinspiration screenings are in compliance with Ghose's rule.

Entities: Chemical

Keywords: Amines; Broth dilution assay; Linker bridge; MIC; s-Triazines

Year: 2011 PMID： 23960775 PMCID： PMC3745068 DOI： 10.1016/j.jsps.2011.05.003

Source DB: PubMed Journal: Saudi Pharm J ISSN： 1319-0164 Impact factor: 4.330

12 in total

1. Discovery of new 1,3,5-triazine scaffolds with potent activity against Mycobacterium tuberculosis H37Rv.

Authors: Naresh Sunduru; Leena Gupta; Vinita Chaturvedi; Richa Dwivedi; Sudhir Sinha; Prem M S Chauhan
Journal: Eur J Med Chem Date: 2010-04-20 Impact factor: 6.514

Review 2. Antibiotic discovery in the twenty-first century: current trends and future perspectives.

Authors: Stefano Donadio; Sonia Maffioli; Paolo Monciardini; Margherita Sosio; Daniela Jabes
Journal: J Antibiot (Tokyo) Date: 2010-06-16 Impact factor: 2.649

3. EUCAST Definitive Document E.DEF 3.1, June 2000: Determination of minimum inhibitory concentrations (MICs) of antibacterial agents by agar dilution.

Authors:
Journal: Clin Microbiol Infect Date: 2000-09 Impact factor: 8.067

2. 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

2 in total

Synthesis, SAR and antibacterial activity of hybrid chloro, dichloro-phenylthiazolyl-s-triazines.

1. Discovery of new 1,3,5-triazine scaffolds with potent activity against Mycobacterium tuberculosis H37Rv.

Review 2. Antibiotic discovery in the twenty-first century: current trends and future perspectives.

3. EUCAST Definitive Document E.DEF 3.1, June 2000: Determination of minimum inhibitory concentrations (MICs) of antibacterial agents by agar dilution.

4. Synthesis and antibacterial activity of various substituted s-triazines.

5. Structure-activity relationships of novel antibacterial translation inhibitors: 3,5-diamino-piperidinyl triazines.

6. Synthetic antibacterials. I. Nitrofurylvinyl-s-triazine derivatives.

7. 4-anilinoquinoline triazines: a novel class of hybrid antimalarial agents.

8. Synthesis and Antibacterial Assessment of N-[4-(4-substituted phenyl)-1,3-thiazol-2-yl]-1,3,5-triazin-2-amine.

9. Synthesis, structure and anticancer activity of novel alkenyl-1,3,5-triazine derivatives.

10. Synthesis, antimalarial activity and cytotoxicity of 4-aminoquinoline-triazine conjugates.

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

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