| Autor: |
Bao-Min, Xi, Pei-Zhou, Ni, Zhen-Zhou, Jiang, Dian-Qing, Wu, Shou-Hua, Zhang, Hui-Bin, Zhang, Tao, Wang, Wen-Hua, Chen |
| Rok vydání: |
2010 |
| Předmět: |
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| Zdroj: |
Chemical biologydrug design. 76(6) |
| ISSN: |
1747-0285 |
| Popis: |
Finding effective chemotherapeutic agents for clinical use is a long-lasting goal in medicinal chemistry. In this study, we report a new class of α₁-adrenoceptor (α₁-AR) antagonists. Specifically, we describe the synthesis and the blocking activities toward α₁-AR of 7-(2-hydroxypropoxy)-3,4-dihydroisoquinolin-1(2H)-one 1 and its structurally perturbed analogs 2-11 that were designed according to the principle of bioisosterism. Their structures were identified with IR, (1) H NMR, MS, HRMS and elemental analysis. The blocking activities of compounds 1-11 were evaluated on isolated rat anococcygeus muscles. The results indicated that these compounds showed moderate to good activities. Among them, compound 1 exhibited the highest activity that was comparable to those of known α₁-AR antagonists tamsulosin and DDPH (1-(2,6-dimethylphenoxy)-2-(3,4-di- methoxyphenylethylamino)propane hydrochloride) and thus may be exploitable as a lead compound for the discovery of promising α₁-AR antagonists. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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