Discovery of novel antileishmanial agents in an attempt to synthesize aplysinopsin pentamidine hybrid molecule

Porwal, Sharad; Chauhan, Shikha; Chauhan, P M S; Shakya, Nishi; Verma, Aditya; Gupta, Suman

dc.contributor.author	Porwal, Sharad
dc.contributor.author	Chauhan, Shikha
dc.contributor.author	Chauhan, P M S
dc.contributor.author	Shakya, Nishi
dc.contributor.author	Verma, Aditya
dc.contributor.author	Gupta, Suman
dc.date.accessioned	2010-09-04T06:34:36Z
dc.date.available	2010-09-04T06:34:36Z
dc.date.issued	2009
dc.identifier.citation	J Med Chem. 2009, 52(19), 5793-802.	en
dc.identifier.uri	http://hdl.handle.net/123456789/580
dc.description.abstract	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.	en
dc.format.extent	205977 bytes
dc.format.mimetype	application/pdf
dc.language.iso	en	en
dc.subject	pentamidine aplysinopsin	en
dc.subject	indole-3-carbaldehyde	en
dc.subject	Leishmaniasis	en
dc.subject	cutaneous leishmaniasis	en
dc.subject	mucocutaneous leishmaniasis	en
dc.subject	protozoan Leishmania	en
dc.title	Discovery of novel antileishmanial agents in an attempt to synthesize aplysinopsin pentamidine hybrid molecule	en
dc.type	Article	en