ANTI-HIV AGENTS - V - SYNTHESIS, STRUCTURE AND IN-VITRO ANTI-HIV ACTIVITY OF NOVEL 1H,3H-NAPHTHO[2',3' 4,5]IMIDAZO[1,2-C]THIAZOLES/

A series of 1H,3H-naphtho[2',3':4,5]imidazo[1,2-c]thiazoles, TBZ analo gues, was prepared in order to explore the influence on anti-HIV activ ity of the spatial requirements of the hydrophobic moiety fused to imi dazothiazole system. In spite of a butterfly-like conformation evidenc ed by X-ray analysis of compound 4g, the results of in vitro screening suggest that the replacement of the benzene fused ring by the naphthy l moiety negatively influences the activity of analogous thiazolobenzi midazole derivatives, some of which are potent non-nucleoside HIV-I RT inhibitors.