New Cytochrome P-450 Ligands Based on Urea Derivatives / A. I. Khlebnikov [et al.]
Уровень набора: Pharmaceutical Chemistry JournalЯзык: английский.Страна: .Резюме или реферат: 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..Примечания о наличии в документе библиографии/указателя: [References: 19 tit.].Аудитория: .Тематика: электронный ресурс | труды учёных ТПУ | мочевина | модели | микросомы | печень | биологически активные соединения | цитохрома Р-450 | лиганды | моделирование Ресурсы он-лайн:Щелкните здесь для доступа в онлайнTitle screen
[References: 19 tit.]
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.
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