Gliotoxin analogues as inhibitors of reverse transcriptase. 1. Effect of lipophilicity.
J Med Chem, 1978/8;21(8):796-9.
Ottenheijm HC, Herscheid JD, Tijhuis MW, Oosterbaan M, De Clercq E
PMID: 80449
Impact factor: 8.039
Abstract
The reaction scheme, developed for the synthesis of the gliotoxin analogue 2, was found to be of general applicability for analogues with varying substituents at N(1) and C(2). Analogues 11b-g prepared by this method are inhibitors of reverse transcriptase (RNA-directed DNA polymerase). Their inhibitory activity seems to be related to the lipophilicity of the effector molecules: the most lipophilic compound is the most active inhibitor. The techniques of reversed-phase thin-layer chromatography with silylated, precoated plates as well as reversed-phase high-performance liquid chromatography were used to measure the relative lipophilicities; both techniques gave analogous results.
MeSH terms
Anti-Bacterial Agents; Chromatography, Thin Layer; DNA-Directed DNA Polymerase; Gliotoxin; Kinetics; Lipid Metabolism; Moloney murine leukemia virus; Reverse Transcriptase Inhibitors
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