New Cytochrome P-450 Ligands Based on Urea Derivatives; Pharmaceutical Chemistry Journal; Vol. 39, iss. 1
| Parent link: | Pharmaceutical Chemistry Journal Vol. 39, iss. 1.— 2005.— [P. 18-21] |
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| Další autoři: | , , , , , , |
| Shrnutí: | 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 |
| Jazyk: | angličtina |
| Vydáno: |
2005
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| Témata: | |
| On-line přístup: | http://dx.doi.org/10.1007/s11094-005-0071-6 |
| Médium: | xMaterials Elektronický zdroj Kapitola |
| KOHA link: | https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=654378 |
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| 200 | 1 | |a New Cytochrome P-450 Ligands Based on Urea Derivatives |f A. I. Khlebnikov [et al.] | |
| 203 | |a Text |c electronic | ||
| 300 | |a Title screen | ||
| 320 | |a [References: 19 tit.] | ||
| 330 | |a 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. | ||
| 333 | |a Режим доступа: по договору с организацией-держателем ресурса | ||
| 461 | |t Pharmaceutical Chemistry Journal | ||
| 463 | |t Vol. 39, iss. 1 |v [P. 18-21] |d 2005 | ||
| 610 | 1 | |a электронный ресурс | |
| 610 | 1 | |a труды учёных ТПУ | |
| 610 | 1 | |a мочевина | |
| 610 | 1 | |a модели | |
| 610 | 1 | |a микросомы | |
| 610 | 1 | |a печень | |
| 610 | 1 | |a биологически активные соединения | |
| 610 | 1 | |a цитохрома Р-450 | |
| 610 | 1 | |a лиганды | |
| 610 | 1 | |a моделирование | |
| 701 | 1 | |a Khlebnikov |b A. I. |c Chemist |c Professor of Tomsk Polytechnic University |f 1963- |g Andrey Ivanovich |3 (RuTPU)RU\TPU\pers\33927 |9 17500 | |
| 701 | 1 | |a Achmedshanow |b R. R. |c Fachmann auf dem Gebiet der Ökologie und Lebenssicherheit |c Professor der Polytechnischen Universität Tomsk, Doktor der biologischen Wissenschafte |f 1964- |g Rafik Rawiliewich |3 (RuTPU)RU\TPU\pers\32824 | |
| 701 | 1 | |a Naboka |b O. I. | |
| 701 | 1 | |a Bakibaev |b A. A. |c Russian chemist |c Professor of TPU, doctor of chemical sciences |f 1960- |g Abdigali Abdimanapovich |3 (RuTPU)RU\TPU\pers\27851 | |
| 701 | 1 | |a Tartynova |b M. I. | |
| 701 | 1 | |a Novozheeva |b T. P. | |
| 701 | 1 | |a Saratikov |b А. S. | |
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| 856 | 4 | |u http://dx.doi.org/10.1007/s11094-005-0071-6 | |
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