THIOPHENE SYSTEMS .15. SYNTHESIS AND ANTIHYPERTENSIVE ACTIVITY OF 7-(SUBSTITUTED BENZAMIDO)-6-HYDROXYTHIENO[3,2-B]PYRANS AS NEW POTASSIUM CHANNEL ACTIVATORS
Pj. Sanfilippo et al., THIOPHENE SYSTEMS .15. SYNTHESIS AND ANTIHYPERTENSIVE ACTIVITY OF 7-(SUBSTITUTED BENZAMIDO)-6-HYDROXYTHIENO[3,2-B]PYRANS AS NEW POTASSIUM CHANNEL ACTIVATORS, Bioorganic & medicinal chemistry letters, 3(6), 1993, pp. 1385-1388
The synthesis and antihypertensive activity of novel 7-(substituted nz
amido)-6-hydroxy-5,5-dimethylthieno[3,2-b]pyrans are described. Acetyl
substitution on the thiophene significantly increases potency of thes
e benzamides in contrast to the nitro substitution which gives the bes
t results in the 7-(cyclic amido)-6-hydroxythieno[3,2-b]pyran series.
Compound 21 is 3-fold more potent than the benzopyran cromakalim (2).