دورية أكاديمية
SAR studies of capsazepinoid bronchodilators. Part 2: Chlorination and catechol replacement in the A-ring.
| العنوان: | SAR studies of capsazepinoid bronchodilators. Part 2: Chlorination and catechol replacement in the A-ring. |
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| المؤلفون: | Berglund M; Division of Organic Chemistry, Lund University, PO Box 124, SE-221 00 Lund, Sweden., Dalence-Guzmán MF, Skogvall S, Sterner O |
| المصدر: | Bioorganic & medicinal chemistry [Bioorg Med Chem] 2008 Mar 01; Vol. 16 (5), pp. 2513-28. Date of Electronic Publication: 2007 Nov 28. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Original Publication: Oxford : New York : Pergamon Press, c1993- |
| مواضيع طبية MeSH: | Bronchodilator Agents/*chemical synthesis , Bronchodilator Agents/*pharmacology , Capsaicin/*analogs & derivatives , Catechols/*chemistry , Chlorine Compounds/*chemical synthesis , Chlorine Compounds/*pharmacology, Bronchodilator Agents/chemistry ; Capsaicin/chemical synthesis ; Capsaicin/chemistry ; Capsaicin/pharmacology ; Chlorine Compounds/chemistry ; Humans ; Molecular Structure ; Respiration/drug effects ; Structure-Activity Relationship |
| مستخلص: | Capsazepine as well as its derivatives and analogues are general inhibitors of constriction of human small airways. From a systematic variation of the capsazepine structure, divided into four regions, SARs were established. This paper concerns the chlorination of the A-ring as well as the replacement of the catechol with bioisosteric groups. It is revealed that chlorination of the A-ring has a profound effect on activity. Moreover, di-chlorination of the 6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline structure results in a 10-fold increase in potency compared to capsazepine. |
| المشرفين على المادة: | 0 (Bronchodilator Agents) 0 (Catechols) 0 (Chlorine Compounds) LF3AJ089DQ (catechol) LFW48MY844 (capsazepine) S07O44R1ZM (Capsaicin) |
| تواريخ الأحداث: | Date Created: 20071211 Date Completed: 20080514 Latest Revision: 20131121 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1016/j.bmc.2007.11.061 |
| PMID: | 18065228 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3391 |
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| DOI: | 10.1016/j.bmc.2007.11.061 |