Press J B, McNally J J, Sanfilippo P J, Addo M F, Loughney D, Giardino E, Katz L B, Falotico R, Haertlein B J
R.W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477-0776.
Bioorg Med Chem. 1993 Dec;1(6):423-35. doi: 10.1016/s0968-0896(00)82153-7.
The syntheses and antihypertensive activity of the thieno[3,4-b]pyran and thieno[2,3-b]pyran isosteres of the potassium channel opener (PCO) RWJ 26629 (+/- 2a) are reported. While the unsubstituted thiophene derivatives were active at 20 mg/kg, introduction of a strong electron withdrawing group in the 2-position of the thieno[3,2-b] series increased potency. Similar substitution on the thieno[3,4-b] series significantly lowered potency. Compounds 26 and 30 are approximately 5-fold more potent than the prototypic PCO cromakalim (+/- 1).
报道了钾通道开放剂（PCO）RWJ 26629（±2a）的噻吩并[3,4-b]吡喃和噻吩并[2,3-b]吡喃电子等排体的合成及其降压活性。未取代的噻吩衍生物在20mg/kg时具有活性，在噻吩并[3,2-b]系列的2-位引入强吸电子基团可提高活性。噻吩并[3,4-b]系列上的类似取代显著降低了活性。化合物26和30的活性约为原型PCO克罗卡林（±1）的5倍。
