Virtual screening of synthesized thiazole derivatives for M. tuberculosis and dTDP-rhamnose inhibitors

  • Rajendra Dnyandeo Dighe K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105
  • Vinod A Bairagi K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105
  • Parag A Pathade K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105
  • Yogesh T Sonawane K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105

Abstract

To determine antimycobacterium and dTDP rhamnose inhibitor activity of the synthesized azetidinone, thiazolidinone derivatives of thiazole, we studied different derivatives for the activity. One pot synthesis of 2-amino-4-methylthiazole-5-carboxylic acid ethyl ester has been carried out and synthesized different derivative compounds. Compounds were tested for antimicrobial activity against different strains of microorganism and antitubercular activity against M. tuberculosis H37Rv. Compounds 7c, 7d, 7i, 8d, 8e, 8g and 8h, were showed antimicrobial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella typhosa using Gentamycin as standard, while 7b, 7e, 7f, 7i, 8b, 8e, 8f and 8i showed very strong antimycobacterial activity using rifampicine as a standard. Thiazole derivatives especially with carbonyl group scaffold inhibit an enzyme RmlC, which is an essential component for the biosynthesis of dTDP-rhamnose and produce good antimycobacterium and antimicrobial activity.


Keywords: Thiazole, thiazolidinone derivatives, azetidinone derivative, well diffusion method, broth microdilution assay, antitubercular activity, antimicrobial activity.

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Author Biographies

Rajendra Dnyandeo Dighe, K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105

K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105

Vinod A Bairagi, K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105

K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105

Parag A Pathade, K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105

K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105

Yogesh T Sonawane, K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105

K.B.H.S.S Trust’s Institute of Pharmacy, Tal. Malegaon, Dist. Nashik, M.S.-423105

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How to Cite
Dighe, R., Bairagi, V. A., Pathade, P. A., & Sonawane, Y. T. (2019). Virtual screening of synthesized thiazole derivatives for M. tuberculosis and dTDP-rhamnose inhibitors. Journal of Drug Delivery and Therapeutics, 9(1), 207-210. https://doi.org/10.22270/jddt.v9i1.2324