Synthesis of Novel MKC‐442 Analogues with Potent Activities against HIV‐1 | Zendy

ElBrollosy Nasser R. | Zendy; Pedersen Erik B. | Zendy; Nielsen Claus | Zendy

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Synthesis of Novel MKC‐442 Analogues with Potent Activities against HIV‐1

Author(s) -

ElBrollosy Nasser R.,

Pedersen Erik B.,

Nielsen Claus

Publication year - 2003

Publication title -

archiv der pharmazie

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.468

H-Index - 61

eISSN - 1521-4184

pISSN - 0365-6233

DOI - 10.1002/ardp.200300742

Subject(s) - human immunodeficiency virus (hiv) , chemistry , structure–activity relationship , pharmacology , stereochemistry , in vitro , biochemistry , virology , biology

Bis(alken‐1‐yloxy)methanes 2 were synthesized by reacting 2‐cyclohexenol, 3‐cyclohexenylmethanol, cinnamyl alcohol and its α‐methyl analogue with dibromomethane. Condensation of 2 with 5, 6‐disubstituted uracil derivatives 1 resulted in the desired MKC‐442 analogues 3‐6 . The most active compounds, N‐1 cinnamyloxymethyl‐ and N‐1 2‐methyl‐3‐phenylallyloxymethyl substituted 5‐ethyl‐6‐(3, 5‐dimethylbenzyl)uracils ( 5b and 6b ), showed activity against wild‐type HIV‐1 in the nanomolar range, and against Y181C andY181C+K103N, mutant strains known to be resistant to MKC‐442, in the micromolar range.

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