Oxadiazole-carbonylaminothioureas as SIRT1 and SIRT2 Inhibitors

A new inhibitor for human sirtuin type proteins 1 and 2 (SIRT1 and SIRT2) was discovered through virtual database screening in search of new scaffolds. A series of compounds was synthesized based on the hit compound (3-[[3-(4-tert-butylphenyl)1,2,4-oxadiazole-5-carbonyl]amino]-1-[3-(trifluoromethyl)...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2008-08, Vol.51 (15), p.4377-4380
Main Authors: Huhtiniemi, Tero, Suuronen, Tiina, Rinne, Valtteri M, Wittekindt, Carsten, Lahtela-Kakkonen, Maija, Jarho, Elina, Wallén, Erik A. A, Salminen, Antero, Poso, Antti, Leppänen, Jukka
Format: Article
Language:English
Subjects:
Biological and medical sciences
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Humans
Medical sciences
Miscellaneous
Models, Molecular
Molecular Structure
Oxadiazoles - chemistry
Oxadiazoles - pharmacology
Pharmacology. Drug treatments
Semicarbazides - chemical synthesis
Semicarbazides - chemistry
Semicarbazides - pharmacology
Sirtuin 1
Sirtuin 2
Sirtuins - antagonists & inhibitors
Sirtuins - chemistry
Sirtuins - metabolism
Structure-Activity Relationship
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Summary:A new inhibitor for human sirtuin type proteins 1 and 2 (SIRT1 and SIRT2) was discovered through virtual database screening in search of new scaffolds. A series of compounds was synthesized based on the hit compound (3-[[3-(4-tert-butylphenyl)1,2,4-oxadiazole-5-carbonyl]amino]-1-[3-(trifluoromethyl)phenyl]thiourea). The most potent compound in the series was nearly as potent as the reference compound (6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide).
ISSN:0022-2623
1520-4804
DOI:10.1021/jm800639h