title: Microwave assisted one-pot synthesis of highly potent novel isoniazid analogues.
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.
authors.affiliation: Medicinal Chemistry and Antimycobacterial Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, India.
authors.forename: Thimmappa H
authors.initials: TH
authors.lastname: Manjashetty
authors.forename: Perumal
authors.initials: P
authors.lastname: Yogeeswari
authors.forename: Dharmarajan
authors.initials: D
authors.lastname: Sriram
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis*; D002522:Chlorocebus aethiops; D007538:Isoniazid / Q000138:chemical synthesis*; D008826:Microbial Sensitivity Tests; D008872:Microwaves; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D014709:Vero Cells
chemical_list: D000995:Antitubercular Agents; D007538:Isoniazid