Kumar Arun, Katiyar Sanjay Babu, Gupta Suman, Chauhan Prem M S
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India.
Eur J Med Chem. 2006 Jan;41(1):106-13. doi: 10.1016/j.ejmech.2005.09.007. Epub 2005 Dec 13.
A series of triazino tetrahydroisoquinolines (3-5) and beta-carboline derivatives (15-27) have been synthesized as novel antileishmanial agents. Among them, compounds 15, 16 and 25 have shown 78.0%, 78.6% and 68.0% in vivo inhibition against Leishmania donovani at a dose of 50 mg kg(-1) x 5 days, respectively, while compounds 3 and 18 exhibited 55.6% and 53.3% in vivo inhibitions, respectively, against L. donovani at a dose of 50 mg kg(-1) x 5 days.
一系列三嗪并四氢异喹啉（3 - 5）和β-咔啉衍生物（15 - 27）已被合成为新型抗利什曼原虫剂。其中，化合物15、16和25在剂量为50 mg kg⁻¹×5天时，对杜氏利什曼原虫的体内抑制率分别为78.0%、78.6%和68.0%，而化合物3和18在剂量为50 mg kg⁻¹×5天时，对杜氏利什曼原虫的体内抑制率分别为55.6%和53.3%。
