2. Academic Validation
  3. Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection

Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection

  • Eur J Med Chem. 2011 Jan;46(1):106-21. doi: 10.1016/j.ejmech.2010.10.020.
Debjani Banerjee 1,  Perumal Yogeeswari,  Pritesh Bhat,  Anisha Thomas,  Madala Srividya,  Dharmarajan Sriram
Affiliations

Affiliation

  • 1 Medicinal Chemistry & Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad-500 078, Andhra Pradesh, India.
PMID: 21093117 DOI: 10.1016/j.ejmech.2010.10.020
Abstract

A series of novel 5-substituted-1-(arylmethyl/alkylmethyl)-1H-indole-2,3-dione-3-(N-hydroxy/methoxy thiosemicarbazone) analogues were synthesized and evaluated for their anti-HIV activity and anti-tubercular activity in both log phase and starved cultures. The compound 2-(1-{[4-(4-chlorophenyl)tetrahydropyrazin-1(2H)-yl]methyl}-5-methyl-2-oxo-1,2-dihydro-3H-indol-3-yliden)-N-(methyloxy)hydrazine-1-carbothioamide (B21) displayed promising activity against the replication of HIV-1 cells (EC(50) 1.69 μM). In anti-mycobacterial screening B21 proved effective in inhibiting the growth of both log phase (MIC 3.30 μM) and starved (MIC 12.11 μM) MTB cultures. Isocitrate lyase Enzyme having momentous implication in persistent TB was shown to be inhibited by 1-cyclopropyl-6-fluoro-7-[4-{[5-methyl-3-((Z)-2-{[(methyloxy)amino]carbothioyl}hydrazono)-2-oxo-1H-indol-1(2H)-yl]methyl}tetrahydropyrazin-1(2H)-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (B30) with 63.44% inhibition at 10 mM.

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