Karampuri , S and Bag , P and Yasmin , S and Chouhan , D.K and Bal , C and Mitra , D. and Chattopadhyay , C. (2012) Structure based molecular design, synthesis and biological evaluation of a-pyrone analogs as anti-HSV agent. Bioorganic & Medicinal Chemistry Letters, 22. pp. 6261-6266.

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Abstract

Several options for treating Herpes Simplex Virus type 1 and type 2 are available. However, non-specific inhibition and drug resistance warrants the discovery of new anti-herpetic compounds with better therapeutic profile or different mode of action. The non-nucleoside inhibitors of HSV DNA polymerase target the site that is less important for the binding of a natural nucleoside or nucleoside inhibitors. In the present study, we have explored the possibility to find a new lead molecule based on a-pyrone analogs as non-nucleoside inhibitors using structure based modeling approach. The designed molecules were synthesized and evaluated for anti-HSV activity using MTT assay. The compound 5h with EC50 7.4 lg/ml and CC50 52.5 lg/ml was moderately active against HSV when compared to acyclovir. A plaque reduction assay was also carried out and results reveal that 5h is more effective against HSV-1 with better selective index of 12.8 than against HSV-2 (SI = 3.6). The synthesized compounds were also evaluated for anti-HIV activity, but none were active.

Item Type:	Article
Subjects:	Cell Biology
Depositing User:	Mr. Rameshwar Nema
Date Deposited:	08 Apr 2015 11:26
Last Modified:	02 Jul 2015 09:12
URI:	http://nccs.sciencecentral.in/id/eprint/18

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