New cage dimers of 4-phenyl-1,4-dihydropyridine derivatives, useful as HIV-1 protease inhibiting anti-HIV agents and for increasing resorption and bioavailability of other anti-HIV drugs

摘要

Symmetrical cage dimers (I) of 3,5-bis-(hydroxymethyl)-4-phenyl-1,4-dihydropyridines are new. Symmetrical cage dihydropyridine dimers of formula (I) are new. R1H, alkyl, aryl, alkoxycarbonyl, aryloxycarbonyl, alkylcarbonyl or arylcarbonyl; X : H, OH, CH2OH or NH2. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Anti-HIV. MECHANISM OF ACTION : HIV-1 protease inhibitor. A symmetrical cage dimer of formula (Ia) exhibited a Ki value of 600 nM for the inhibition of HIV-1 protease.