Literature DB >> 20149496

Synthesis of some novel 2-substituted-5-[isopropylthiazole] clubbed 1,2,4-triazole and 1,3,4-oxadiazoles as potential antimicrobial and antitubercular agents.

G V Suresh Kumar1, Y Rajendraprasad, B P Mallikarjuna, S M Chandrashekar, C Kistayya.   

Abstract

In the present study a series of 2-substituted-5-[isopropylthiazole] clubbed 1,2,4-triazole and 1,3,4-oxadiazole derivatives have been synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral analysis. Synthesized compounds were evaluated for their preliminary cytotoxicity, antimicrobial and antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth dilution assay method. Antimycobacterial activity tested against M. tuberculosis indicated that compounds 4b and 6g exhibited twofold enhanced potency than parent compound 1 and the results indicate that some of them exhibited promising activities and they deserve more consideration as potential antitubercular agents. Compound 3c, 4b and 6c exhibited good or moderate antibacterial inhibition and compounds 3h and 7c showed excellent antifungal activity. Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.

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Year:  2010        PMID: 20149496     DOI: 10.1016/j.ejmech.2010.01.045

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  15 in total

1.  High throughput screening of a library based on kinase inhibitor scaffolds against Mycobacterium tuberculosis H37Rv.

Authors:  Robert C Reynolds; Subramaniam Ananthan; Ellen Faaleolea; Judith V Hobrath; Cecil D Kwong; Clinton Maddox; Lynn Rasmussen; Melinda I Sosa; Elizabeth Thammasuvimol; E Lucile White; Wei Zhang; John A Secrist
Journal:  Tuberculosis (Edinb)       Date:  2011-06-25       Impact factor: 3.131

2.  Antimicrobial activity of 1,3,4-oxadiazole derivatives against planktonic cells and biofilm of Staphylococcus aureus.

Authors:  Zhaojun Zheng; Qingzhong Liu; Wooseong Kim; Nagendran Tharmalingam; Beth Burgwyn Fuchs; Eleftherios Mylonakis
Journal:  Future Med Chem       Date:  2018-01-15       Impact factor: 3.808

Review 3.  Evaluation of small molecule kinase inhibitors as novel antimicrobial and antibiofilm agents.

Authors:  Ashley King; Meghan S Blackledge
Journal:  Chem Biol Drug Des       Date:  2021-10-04       Impact factor: 2.817

4.  Synthesis and biological evaluation of aminonaphthols incorporated indole derivatives.

Authors:  Saundane Anand Raghunath; Kirankumar Nandibeoor Mathada
Journal:  Int J Med Chem       Date:  2014-09-10

5.  Design, Synthesis, Toxicity Estimation and Molecular Docking Studies of N-(furan-2-yl)-1-(5-substituted) phenyl-1,3,4-oxadiazol-2-yl) methanimine as Antitubercular Agents.

Authors:  B Mathew; J Suresh; Githa E Mathew; George Sonia; G K Krishnan
Journal:  Indian J Pharm Sci       Date:  2014-09       Impact factor: 0.975

6.  Synthesis and biological evaluation of aryl-oxadiazoles as inhibitors of Mycobacterium tuberculosis.

Authors:  Maria Angeles Martinez-Grau; Isabel C Gonzalez Valcarcel; Julie V Early; Richard Klaus Gessner; Candice Soares de Melo; Eva Maria Martin de la Nava; Aaron Korkegian; Yulia Ovechkina; Lindsay Flint; Anisa Gravelle; Jeff W Cramer; Prashant V Desai; Leslie J Street; Joshua Odingo; Thierry Masquelin; Kelly Chibale; Tanya Parish
Journal:  Bioorg Med Chem Lett       Date:  2018-04-13       Impact factor: 2.823

7.  Synthesis and Pharmacological Activities of Some New 5-Substituted-2-mercapto-1,3,4-oxadiazoles.

Authors:  Shobha R Desai; U Laddi; Rajani S Bennur; P A Patil; S Bennur
Journal:  Indian J Pharm Sci       Date:  2011-09       Impact factor: 0.975

8.  4-Benzyl-3-(thio-phen-2-yl)-4,5-di-hydro-1H-1,2,4-triazole-5-thione.

Authors:  Mona M Al-Shehri; Ali A El-Emam; Nasser R El-Brollosy; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-04-13

9.  Synthesis and evaluation of antiinflammatory, analgesic and ulcerogenic potential of NSAIDs bearing 1,3,4-oxadiazole scaffold.

Authors:  R R Somani; U V Bhanushali
Journal:  Indian J Pharm Sci       Date:  2011-11       Impact factor: 0.975

Review 10.  An insight on medicinal attributes of 1,2,4-triazoles.

Authors:  Ranjana Aggarwal; Garima Sumran
Journal:  Eur J Med Chem       Date:  2020-07-27       Impact factor: 6.514

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