Design and syntheses of 1, 6-naphthalene derivatives as selective HCMV protease inhibitors

…, D Grinberg, B Feld, FJ Moy, J O'Connell

Index: Gopalsamy, Ariamala; Lim, Kitae; Ellingboe, John W.; Mitsner, Boris; Nikitenko, Antonia; Upeslacis, Janis; Mansour, Tarek S.; Olson, Matthew W.; Bebernitz, Geraldine A.; Grinberg, Diane; Feld, Boris; Moy, Franklin J.; O'Connell, John Journal of Medicinal Chemistry, 2004 , vol. 47, # 8 p. 1893 - 1899

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Citation Number: 22

Abstract

Through high throughput screening of various libraries, substituted styryl naphthalene 6 was identified as an HCMV protease inhibitor. Optimization of various regions of the lead molecule using parallel synthesis resulted in 1, 6-substituted naphthalenes 19d-i. These compounds displayed good potency and were selective over elastase, trypsin, and chymotrypsin. The optimization approach on lead compound 6 in three different regions of ...