Conformationally locked thiosugars as potent α-mannosidase inhibitors: synthesis, biochemical and docking studies

Sivapriya, K. ; Hariharaputran, S. ; Suhas, V. L. ; Chandra, N. ; Chandrasekaran, S. (2007) Conformationally locked thiosugars as potent α-mannosidase inhibitors: synthesis, biochemical and docking studies Bioorganic & Medicinal Chemistry, 15 (17). pp. 5659-5665. ISSN 0968-0896

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Official URL: http://dx.doi.org/10.1016/j.bmc.2007.06.011

Related URL: http://dx.doi.org/10.1016/j.bmc.2007.06.011

Abstract

A series of thiosugar derivatives (thiolevomannosans) derived from mannose were synthesized and their inhibitory activity was tested against α-mannosidase (jack bean). These inhibitors were found to be more potent than the well-known inhibitors like kifunensine and deoxymannojirimycin based on docking and biochemical studies. The sulfone derivative 10 was shown to be the best inhibitor of α-mannosidase with the Ki value of 350 nM.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Thiosugars; Inhibition; α-mannosidase; Docking Studies
ID Code:7240
Deposited On:25 Oct 2010 12:04
Last Modified:28 May 2011 09:44

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