Найдено научных статей и публикаций: 1, для научной тематики: Post kala-azar dermal leishmaniasis
1.
Sharad Porwal, Shikha S. Chauhan, Prem M. S. Chauhan,* Nishi Shakya, Aditya Verma and Suman Gupta
- J. Med. Chem. , 2009
In an attempt to synthesize pentamidine-aplysinopsin hybrid molecule 25, a lead molecule 8
(containing Z-configured aplysinopsin moiety) was identified for antileishmanial activity. Optimization
of lead 8 provided 24 (containing E-configured aplysinopsin) possessing 10 times more activity and
401...
In an attempt to synthesize pentamidine-aplysinopsin hybrid molecule 25, a lead molecule 8
(containing Z-configured aplysinopsin moiety) was identified for antileishmanial activity. Optimization
of lead 8 provided 24 (containing E-configured aplysinopsin) possessing 10 times more activity and
401-fold less toxicity than the drug pentamidine in cell based assays. Synthesis of 24 was possible,
surprisingly, because of two innate reactivities of indole-3-carbaldehyde which provided it in diastereoand
regio-selectively pure form without recourse to the long reaction pathway.