INHIBITION OF HIV REVERSE TRANSCRIPTASE-CATALYZED POLYMERIZATION OF MODEL SUBSTRATES BY OLIGO-1,3-THIAZOLECARBOXAMIDE DERIVATIVES

A series of nonnatural peptides of a new type (oligo-1,3-thiazolecarbo xamides) capable of binding in the minor groove of nucleic acids were synthesized. They differ from the previously described distamycin and its analogs in containing the thiazole rather than pyrrole rings. The thiazole-containing oligopeptides, like distamycin, slightly inhibit t he polymerization reaction catalyzed by the HIV-1 reverse transcriptas e [EC 2.7.7.49] in RNA.RNA template-primer complexes. Their inhibitory effect is comparable with that of distamycin in the case of DNA.DNA s ubstrates and is two orders of magnitude higher for the RNA.RNA and DN A.RNA complexes. The plausible causes of different effects of the nonn atural peptides on polymerization with various template-primer complex es are discussed.