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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

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Published on: June 23, 2019

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

Thimmappa H Manjashetty¹, Perumal Yogeeswari, Dharmarajan Sriram

¹Medicinal Chemistry and Antimycobacterial Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, India.

Bioorganic & Medicinal Chemistry Letters

|February 16, 2011

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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