Kartik M. Keertikar

The application of disubstituted vinylogous iminium salts and related synthons to the regiocontrolled preparation of unsymmetrical 2,3,4-trisubstituted pyrroles

Abstract Reactions of 2,3-disubstituted chloropropeniminium salts and related synthons with ethyl glycinate, ethyl N-methylglycinate, and ethyl N-benzylglycinate have been studied under acidic, basic and neutral conditions. Such reactions have resulted in efficient and selective methodology for the synthesis of unsymmetrical 2,3,4-trisubstituted pyrrole systems.

Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: A template-based approach.

The synthesis and hit-to-lead SAR development from a pyrazolo[1,5-a]pyrimidine-derived hit 5 to the identification of a series of potent, pan-Pim inhibitors such as 11j are described.

Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors

Using the HIV-1 protease binding mode of MK-8718 and PL-100 as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and synthesized. The resulting HIV-1 protease inhibitor containing this core showed an 60-fold increase in enzyme binding affinity and a 10-fold increase in antiviral activity relative to MK-8718.