1999 multi-membered N-heterocycles

multi-membered N-heterocyclesR 0690

17 - 166Tricyclic Ureas: A New Class of HIV-1 Protease Inhibitors. — Anew class of tricyclic ureas containing a conformationally constrained proline isdesigned and synthesized involving an efficient and stereoselective intermolecularpinacol coupling [(III)→(V)] as the key step. These rigid cyclic ureas prove tobe active towards HIV-1 protease, with compound (XII) being the most potentone. — (HAN, WEI; PELLETIER, JEFFREY C.; HODGE, C. NICHOLAS;Bioorg. Med. Chem. Lett. 8 (1998) 24, 3615-3620; Dep. Chem. Phys. Sci., DuPont Merck Pharm. Co., Exp. Stn., Wilmington, DE 19880, USA; EN)

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