Synthesis and biological evaluation of indolyl glyoxylamides as a new class of antileishmanial agents.
A series of indolylglyoxylamide derivatives have been synthesized and evaluated in vitro against amastigote form of Leishmania donovani. Compound 8c has been identified as the most active analog of the series with IC(50) value of 5.17μM and SI value of 31.48, and is several folds more potent than the standard drugs sodium stilbogluconate and pentamidine.
Chauhan
Shikha S
SS
Division of Medicinal and Process Chemistry, Central Drug Research Institute, CSIR, Lucknow 226001, India.
Gupta
Leena
L
Mittal
Monika
M
Vishwakarma
Preeti
P
Gupta
Suman
S
Chauhan
Prem M S
PM
D000818:Animals; D000967:Antimony Sodium Gluconate / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007893:Leishmania donovani / Q000187:drug effects*; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D010419:Pentamidine / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D002243:Carbolines; D007202:Indicators and Reagents; D010419:Pentamidine; D000967:Antimony Sodium Gluconate