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| Title: | Discovery of novel antileishmanial agents in an attempt to synthesize aplysinopsin pentamidine hybrid molecule |
| Authors: | Porwal, Sharad
Chauhan, Shikha
Chauhan, P M S
Shakya, Nishi
Verma, Aditya
Gupta, Suman |
| Keywords: | pentamidine aplysinopsin
indole-3-carbaldehyde
Leishmaniasis
cutaneous leishmaniasis
mucocutaneous leishmaniasis
protozoan Leishmania |
| Issue Date: | 2009 |
| Citation: | J Med Chem. 2009, 52(19), 5793-802. |
| 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. |
| URI: | http://hdl.handle.net/123456789/580 |
| Appears in Collections: | Medicinal and Process Chemistry
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Files in This Item:
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Description |
Size | Format |
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| chauhanpms-7738-J. Med. Chem. -2009- 52- 5793–5802.pdf | | 201Kb | Adobe PDF | View/Open |
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