Please use this identifier to cite or link to this item:
http://dspace.bits-pilani.ac.in:8080/jspui/xmlui/handle/123456789/3048
Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Kumar, Dalip | - |
dc.date.accessioned | 2021-10-27T04:20:42Z | - |
dc.date.available | 2021-10-27T04:20:42Z | - |
dc.date.issued | 2011-12-16 | - |
dc.identifier.uri | https://onlinelibrary.wiley.com/doi/10.1111/j.1747-0285.2011.01304.x | - |
dc.identifier.uri | http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/3048 | - |
dc.description.abstract | A series of 3,5-disubstituted-1,2,4-oxadiazoles has been prepared and evaluated for phosphodiesterase inhibition (PDE4B2). Among the prepared 3,5-disubstituted-1,2,4-oxadiazoles, compound 9a is the most potent inhibitor (PDE4B2 IC50 = 5.28 μm). Structure–activity relationship studies of 3,5-disubstituted-1,2,4-oxadiazoles revealed that substituents 3-cyclopentyloxy-4-methoxyphenyl group at 3-position and cyclic ring bearing heteroatoms at 5-position are important for activity. Molecular modeling study of the 3,5-disubstituted-1,2,4-oxadiazoles with PDE4B has shown similar interactions of 3-cyclopentyloxy-4-methoxyphenyl group; however, heteroatom ring is slightly deviating when compared to Piclamilast. 3-(3-Cyclopentyloxy-4-methoxyphenyl)-5-(piperidin-4-yl)-1,2,4-oxadiazole (9a) exhibited good analgesic and antiinflammatory activities in formalin-induced pain in mice and carrageenan-induced paw edema model in rat. | en_US |
dc.language.iso | en | en_US |
dc.publisher | Wiley | en_US |
dc.subject | Chemistry | en_US |
dc.subject | Synthesis | en_US |
dc.subject | Phosphodiesterase4B2 | en_US |
dc.title | Design and Synthesis of 3,5-Disubstituted-1,2,4-Oxadiazoles as Potent Inhibitors of Phosphodiesterase4B2 | en_US |
dc.type | Article | en_US |
Appears in Collections: | Department of Chemistry |
Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.