Scola, Paul M. published the artcileDiscovery and Early Clinical Evaluation of BMS-605339, a Potent and Orally Efficacious Tripeptidic Acylsulfonamide NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection, COA of Formula: C9H5Cl2N, the main research area is BMS 605339 tripeptidic acylsulfonamide NS3 protease inhibitor hepatitis C.
The discovery of BMS-605339 (35), a tripeptidic inhibitor of the NS3/4A enzyme, is described. This compound incorporates a cyclopropylacylsulfonamide moiety that was designed to improve the potency of carboxylic acid prototypes through the introduction of favorable nonbonding interactions within the S1′ site of the protease. The identification of 35 was enabled through the optimization and balance of critical properties including potency and pharmacokinetics (PK). This was achieved through modulation of the P2* subsite of the inhibitor which identified the isoquinoline ring system as a key template for improving PK properties with further optimization achieved through functionalization. A methoxy moiety at the C6 position of this isoquinoline ring system proved to be optimal with respect to potency and PK, thus providing the clin. compound 35 which demonstrated antiviral activity in HCV-infected patients.
Journal of Medicinal Chemistry published new progress about Antiviral agents. 70810-23-0 belongs to class isoquinoline, name is 1,5-Dichloroisoquinoline, and the molecular formula is C9H5Cl2N, COA of Formula: C9H5Cl2N.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem