Synthesis of 2-(pyrimidin-2-yl)-1-phenyl-2,3,4,9-tetrahydro-1H-beta-carbolines as antileishmanial agents.
A series of 2-(pyrimidin-2-yl)-1-phenyl-2,3,4,9-tetrahydro-1H-beta-carboline derivatives has been synthesized and evaluated for antileishmanial activity against Leishmania donovani. Compound 8 exhibited best antileishmanial activity with IC(50) value of 1.93 microg/ml against amastigotes, high selectivity index, and was more active than reference drugs sodium stilbogluconate and pentamidine.
Kumar
Ravi
R
Medicinal & Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow, India.
Khan
Shahnawaz
S
Verma
Aditya
A
Srivastava
Saumya
S
Viswakarma
Preeti
P
Gupta
Suman
S
Meena
Sanjeev
S
Singh
Neetu
N
Sarkar
Jayanta
J
Chauhan
Prem M S
PM
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002243:Carbolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D051379:Mice
D000981:Antiprotozoal Agents; D002243:Carbolines