Tags

Type your tag names separated by a space and hit enter

N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors.
Bioorg Med Chem. 2011 Sep 15; 19(18):5569-76.BM

Abstract

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 (IC(50)=2.45 μM) 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.

Authors+Show Affiliations

Laboratory for Drug Design and Synthesis, Department of Pharmaceutical Chemistry, Indo-Soviet Friendship College of Pharmacy, Moga 142 001, Punjab, India.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

21862335

Citation

Nepali, Kunal, et al. "N-(1,3-Diaryl-3-oxopropyl)amides as a New Template for Xanthine Oxidase Inhibitors." Bioorganic & Medicinal Chemistry, vol. 19, no. 18, 2011, pp. 5569-76.
Nepali K, Agarwal A, Sapra S, et al. N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors. Bioorg Med Chem. 2011;19(18):5569-76.
Nepali, K., Agarwal, A., Sapra, S., Mittal, V., Kumar, R., Banerjee, U. C., Gupta, M. K., Satti, N. K., Suri, O. P., & Dhar, K. L. (2011). N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors. Bioorganic & Medicinal Chemistry, 19(18), 5569-76. https://doi.org/10.1016/j.bmc.2011.07.039
Nepali K, et al. N-(1,3-Diaryl-3-oxopropyl)amides as a New Template for Xanthine Oxidase Inhibitors. Bioorg Med Chem. 2011 Sep 15;19(18):5569-76. PubMed PMID: 21862335.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors. AU - Nepali,Kunal, AU - Agarwal,Amit, AU - Sapra,Sameer, AU - Mittal,Vineet, AU - Kumar,Raj, AU - Banerjee,Uttam C, AU - Gupta,Manish K, AU - Satti,Naresh K, AU - Suri,Om P, AU - Dhar,Kanaya L, Y1 - 2011/07/26/ PY - 2011/05/25/received PY - 2011/07/19/revised PY - 2011/07/20/accepted PY - 2011/8/25/entrez PY - 2011/8/25/pubmed PY - 2012/1/11/medline SP - 5569 EP - 76 JF - Bioorganic & medicinal chemistry JO - Bioorg. Med. Chem. VL - 19 IS - 18 N2 - 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 (IC(50)=2.45 μM) 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. SN - 1464-3391 UR - https://www.unboundmedicine.com/medline/citation/21862335/N__13_Diaryl_3_oxopropyl_amides_as_a_new_template_for_xanthine_oxidase_inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0968-0896(11)00588-8 DB - PRIME DP - Unbound Medicine ER -