Discovery of novel antileishmanial agents in an attempt to synthesize aplysinopsin pentamidine hybrid molecule
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
View Archive Info| Field | Value | |
| Creator |
Porwal, Sharad
Chauhan, Shikha Chauhan, P M S Shakya, Nishi Verma, Aditya Gupta, Suman |
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| Date |
2010-09-04T06:34:36Z
2010-09-04T06:34:36Z 2009 |
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| Identifier |
J Med Chem. 2009, 52(19), 5793-802.
http://hdl.handle.net/123456789/580 |
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| Description |
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.
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| Format |
205977 bytes
application/pdf |
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| Language |
en
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| Subject |
pentamidine aplysinopsin
indole-3-carbaldehyde Leishmaniasis cutaneous leishmaniasis mucocutaneous leishmaniasis protozoan Leishmania |
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| Title |
Discovery of novel antileishmanial agents in an attempt to synthesize aplysinopsin pentamidine hybrid molecule
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| Type |
Article
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