Inhibition of herpes proteases and antiviral activity of 2-substituted thieno[2,3-d]oxazinones

R L Jarvest; I L Pinto; S M Ashman; C E Dabrowski; A V Fernandez; L J Jennings; P Lavery; D G Tew

doi:10.1016/s0960-894x(99)00004-9

Inhibition of herpes proteases and antiviral activity of 2-substituted thieno[2,3-d]oxazinones

Bioorg Med Chem Lett. 1999 Feb 8;9(3):443-8. doi: 10.1016/s0960-894x(99)00004-9.

Authors

R L Jarvest¹, I L Pinto, S M Ashman, C E Dabrowski, A V Fernandez, L J Jennings, P Lavery, D G Tew

Affiliation

¹ SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK. Richard_L_Jarvest@sbphrd.com

PMID: 10091699
DOI: 10.1016/s0960-894x(99)00004-9

Abstract

Cinnamyl derivatives of thieno[2,3-d]oxazinones are mechanism-based inhibitors of the HSV-2, VZV and CMV herpes proteases which demonstrate nanomolar potency. Compounds 5 and 28 inhibit protease processing in HSV-2 infected cells with a selectivity index of at least 30.

MeSH terms

Antiviral Agents / chemistry
Antiviral Agents / pharmacology*
Cell Line
Herpesviridae / enzymology*
Oxazines / chemistry
Oxazines / pharmacology*
Protease Inhibitors / chemistry
Protease Inhibitors / pharmacology*

Substances

Antiviral Agents
Oxazines
Protease Inhibitors