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

…, V Tantishaiyakul, A Hamada, DD Miller…

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

Full Text: HTML

Citation Number: 26

Abstract

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 ...