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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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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
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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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creator	Huhtiniemi, Tero Suuronen, Tiina Rinne, Valtteri M Wittekindt, Carsten Lahtela-Kakkonen, Maija Jarho, Elina Wallén, Erik A. A Salminen, Antero Poso, Antti Leppänen, Jukka
description	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).
doi_str_mv	10.1021/jm800639h
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source	American Chemical Society:Jisc Collections:American Chemical Society Read & Publish Agreement 2022-2024 (Reading list)
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
title	Oxadiazole-carbonylaminothioureas as SIRT1 and SIRT2 Inhibitors
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