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Methylsulfonylpyrazolyl oxadiazoles and thiadiazoles as potent, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity
- Authors
- Seo, H.J.[Seo, H.J.]; Kim, M.J.[ Kim, M.J.]; Song, K.-S.[ Song, K.-S.]; Lee, S.-H.[ Lee, S.-H.]; Jung, M.E.[ Jung, M.E.]; Kim, M.-S.[ Kim, M.-S.]; Park, H.-J.[Park, H.-J.]; Yoo, J.[Yoo, J.]; Chang, C.-H.[ Chang, C.-H.]; Kim, J.[ Kim, J.]; Lee, J.[ Lee, J.]
- Issue Date
- 2009
- Citation
- Future Medicinal Chemistry, v.1, no.5, pp.947 - 967
- Indexed
- SCOPUS
- Journal Title
- Future Medicinal Chemistry
- Volume
- 1
- Number
- 5
- Start Page
- 947
- End Page
- 967
- ISSN
- 1756-8919
- Abstract
- Background: Since the cannabinoid receptor 1 (CB1) antagonist SR141716 (rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. Discussion: In the present study, biarylpyrazole analogues based on a sulfur-containing pyrazole core coupled with 1,3,4-oxadiazole and 1,3,4-thiadiazole were synthesized and assayed for rat CB1 receptor binding affinity. Results: The structure-activity relationship studies to optimize pyrazole substituents as well as 1,3,4-oxadiazole or 1,3,4-thiadiazole rings led to four novel CB1 antagonists with IC50 values of approximately 1 nM for the rat CB1 receptor binding. Among these derivatives, we identified trifluoromethylcyclobutyl analogues 19e and 19l as promising precandidates for the development as anti-obesity agents. © 2009 Future Science Ltd.
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Collections - Pharmacy > Department of Pharmacy > 1. Journal Articles
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