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 the molecule using parallel solution-phase synthesis and the corresponding SAR are discussed in detail.
MeSH terms
-
2-Naphthylamine / analogs & derivatives
-
2-Naphthylamine / chemical synthesis*
-
2-Naphthylamine / chemistry
-
Cytomegalovirus / chemistry*
-
Databases, Factual
-
Naphthalenes / chemical synthesis*
-
Naphthalenes / chemistry
-
Protease Inhibitors / chemical synthesis*
-
Protease Inhibitors / chemistry
-
Serine Endopeptidases / chemistry*
-
Structure-Activity Relationship
-
Sulfonamides / chemical synthesis*
-
Sulfonamides / chemistry
Substances
-
C,C,C-trifluoro-N-(5-(2-pyridin-2-ylvinyl)naphthalen-2-yl)methanesulfonamide
-
Naphthalenes
-
Protease Inhibitors
-
Sulfonamides
-
2-Naphthylamine
-
Serine Endopeptidases
-
assemblin