N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors
IR@IIIM: CSIR-Indian Institute of Integrative Medicine, Jammu
View Archive Info| Field | Value | |
| Title |
N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors
|
|
| Creator |
Nepali, Kunal
Agarwal, Amit Sapra, Sameer Mittal, Vineet Kumar, Raj Banerjee, Uttam C. Gupta, Manish K. Satti, Naresh K. Suri, Om P. Dhar, Kanaya L. |
|
| Subject |
Chemical Sciences
|
|
| Description |
A series of forty two N-(1,3-diaryl-3-oxopropyl)amides were synthesized via an efficient, modified Dakin–West reaction and were evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Structure–activity relationship analyses have been presented. Selected active xanthine oxidase inhibitors (3r, 3s, and 3zh) were assessed in vivo to study their anti-hyperuricemic effect in potassium oxonate induced hyperuricemic mice model. Compound 3s emerged as the most potent xanthine oxidase
inhibitor (IC50 = 2.45 lM) as well as the most potent anti-hyperuricemic agent. The basis of significant
inhibition of xanthine oxidase by 3s was rationalized by its molecular docking into catalytic site of xanthine oxidase.
|
|
| Date |
2011
|
|
| Type |
Article
PeerReviewed |
|
| Format |
application/pdf
|
|
| Identifier |
http://iiim.csircentral.net/297/1/10.1016j.bmc.2011.07.039.pdf
Nepali, Kunal and Agarwal, Amit and Sapra, Sameer and Mittal, Vineet and Kumar, Raj and Banerjee, Uttam C. and Gupta, Manish K. and Satti, Naresh K. and Suri, Om P. and Dhar, Kanaya L. (2011) N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors. Bioorganic & Medicinal Chemistry, 19 (18). pp. 5569-5576. ISSN 09680896 |
|
| Relation |
http://dx.doi.org/10.1016/j.bmc.2011.07.039
http://iiim.csircentral.net/297/ |
|