New Cytochrome P-450 Ligands Based on Urea Derivatives
| Parent link: | Pharmaceutical Chemistry Journal Vol. 39, iss. 1.— 2005.— [P. 18-21] |
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| Other Authors: | , , , , , , |
| Summary: | Title screen Cytochrome P-450 (CYPIIB1 isoform) ligands were constructed de novo on the basis of QSAR models derived using the frontal polygon (FP) method. The following compounds were designed and synthesized: 2-phenyl-6-benzyl-2,4,6,8-tetraazabicyclo[3.3.0]octane-3,7-dione, N-acetyl-N?-(1-phenylethyl)urea, and (1-phenyl-3-methylbutyl)urea. Their interaction with phenobarbital-induced microsomes isolated from rat liver was studied spectrophotometrically. The dissociation constants Ks of the enzyme - substrate complexes measured are in good agreement with the values predicted using the QSAR models. The results show that the FP method has a high potential for designing biologically active compounds. Режим доступа: по договору с организацией-держателем ресурса |
| Published: |
2005
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| Subjects: | |
| Online Access: | http://dx.doi.org/10.1007/s11094-005-0071-6 |
| Format: | Electronic Book Chapter |
| KOHA link: | https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=654378 |