2. Academic Validation
  3. Microwave assisted one-pot synthesis of highly potent novel isoniazid analogues

Microwave assisted one-pot synthesis of highly potent novel isoniazid analogues

  • Bioorg Med Chem Lett. 2011 Apr 1;21(7):2125-8. doi: 10.1016/j.bmcl.2011.01.122.
Thimmappa H Manjashetty 1,  Perumal Yogeeswari,  Dharmarajan Sriram
Affiliations

Affiliation

  • 1 Medicinal Chemistry and Antimycobacterial Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, India.
PMID: 21320779 DOI: 10.1016/j.bmcl.2011.01.122
Abstract

A series of novel isoniazid (INH) analogues were synthesized by microwave assisted one pot reaction of INH, various benzaldehydes and dimedone in water with catalytic amount of DBSA. The synthesized compounds were evaluated for their anti-TB activity against Mycobacterium tuberculosis H37Rv (MTB) and multi-drug resistant Mycobacterium tuberculosis (MDR-TB). Among the 29 compounds, compound N-[9-[2-(benzyloxy)phenyl]-3,3,6,6-tetramethyl-1,8-dioxo-2,3,4,5,6,7,8,9-octahydro-10(1H)-acridinyl]isonicotinamide (12) inhibited MTB with MIC of <0.17 μM and MDR-TB with MIC of 0.69 μM.

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