2. Academic Validation
  3. Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives

Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives

  • Eur J Med Chem. 2017 May 26:132:333-340. doi: 10.1016/j.ejmech.2017.03.065.
Yogita K Abhale 1,  Amit V Sasane 2,  Abhijit P Chavan 2,  Saddam Husen Shekh 2,  Keshav K Deshmukh 1,  Sujit Bhansali 3,  Laxman Nawale 3,  Dhiman Sarkar 3,  Pravin C Mhaske 4
Affiliations

Affiliations

  • 1 Post-Graduate Department of Chemistry and Research Centre, S. N. Arts, D. J. M. Commerce and B. N. S. Science College, College Road, Sangamner, District Ahmednagar, 422 605, India(1).
  • 2 Post Graduate Department of Chemistry, S. P. Mandali's Sir Parashurambhau College, Tilak Road, Pune 411 030, India(1).
  • 3 CombiChemBio Resource Centre, CSIR-National Chemical Laboratory, Pune 411 008, India.
  • 4 Post Graduate Department of Chemistry, S. P. Mandali's Sir Parashurambhau College, Tilak Road, Pune 411 030, India(1). Electronic address: mhaskepc18@gmail.com.
PMID: 28411559 DOI: 10.1016/j.ejmech.2017.03.065
Abstract

In the present study a series of 4-methyl-2-aryl-5-(2-aryl/benzyl thiazol-4-yl) oxazole (4a-v) have been synthesized and evaluated for their preliminary antitubercular, antimicrobial and cytotoxicity activity. Among all the synthesized compounds, 4v reported comparable activity against dormant M. tuberculosis H37Ra and M. bovis BCG strains with respect to standard drug rifampicin. The active compounds from the antitubercular study were further tested for anti-proliferative activity against HeLa, A549 and PANC-1 cell lines using MTT assay and showed no significant cytotoxic activity at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential Antibacterial activities with MIC range of 2.1-26.8 μg/mL. High potency, lower cytotoxicity and promising antimycobacterial activity suggested that these compounds could serve as good leads for further optimisation and development.

Keywords

Antitubercular activity; Cytotoxicity; Oxazole; Thiazole.

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