Synthesis of New MKC‐442 Analogues Containing Alkenyl Chains or Reactive Functionalities at C‐5.

Abstract

Synthesis of New MKC-442 Analogues Containing Alkenyl Chains orReactive Functionalities at C-5.-In an effort to obtain more insight into the interaction between HIV-1 reverse transcriptase (RT) and MKC-442 analogues, a series of new compounds is synthesized and evaluated for inhibition of HIV-1 replication. The modifications include bulky alkenyl substituents at the C-5 position of the uracil ring like in (III) or in the corresponding N-alkylated derivatives (V), (IX), and (XI). Uracils, e.g. (VI) and (XII) with reactive epoxy and aldehyde functionalities at C-5 are also synthesized. Antiviral activity and cytotoxicities of the new substances are tested. -(PETERSEN, LENE; HANSEN, THOMAS H.; KHALIFA, NAGY M.; JOERGENSEN, PER T.; PEDERSEN, ERIK B.; NIELSEN, CLAUS; Monatsh. Chem. 133 (2002) 7, 1031-1043; Dep. Chem., Univ. South. Den., DK-5230 Odense, Den.; EN)