Synthesis of halogenated trimetoquinol derivatives and evaluation of their. beta.-agonist and thromboxane A2 (TXA2) antagonist activities

…, V Tantishaiyakul, A Hamada, DD Miller…

文献索引：Markovich; Tantishaiyakul; Hamada; Miller; Romstedt; Shams; Shin; Fraundorfer; Doyle; Feller Journal of Medicinal Chemistry, 1992 , vol. 35, # 3 p. 466 - 479

全文：HTML全文

被引用次数: 26

摘要

The B, &difluoro (4), 5-iodo (S), &iodo (6), and 5-trifluoromethyl (7) derivatives of trimetoquinol (TMQ, 1) have been synthesized and evaluated for their ability to stimulate b1 (guinea pig atria) and B2 (guinea pig trachea) adrenoceptors as well as for their inhibitory activity against U46619 [a thromboxane A2 (TXA,) mimetic]-mediated contraction of rat thoracic aorta and human platelet aggregation. Both 5 and 6 were considerably less ...