Kanno H, Yamaguchi H, Okamiya Y, Sunakawa K, Takeshita T, Naruchi T
Teijin Institute for Bio-Medical Research, Tokyo, Japan.
Chem Pharm Bull (Tokyo). 1992 Aug;40(8):2049-54. doi: 10.1248/cpb.40.2049.
New 1,4-dihydropyridine derivatives bearing a 4-(disubstituted phenyl) ring and an aminoethyl ester or an amino-2,2-dimethyl-propyl ester were synthesized and their antihypertensive activities were examined in normotensive rats and spontaneously hypertensive rats. The effects of phenyl substituents and ester groups on the antihypertensive activity are discussed. Several compounds showed a more potent antihypertensive activity than nicardipine and most compounds had a longer duration of action. Among them, 7B.HCl (TC-81) showed highly potent and long-lasting activity and was selected as a candidate for further pharmacological investigations.
合成了带有4-（二取代苯基）环以及氨基乙酯或氨基-2,2-二甲基丙酯的新型1,4-二氢吡啶衍生物，并在正常血压大鼠和自发性高血压大鼠中检测了它们的抗高血压活性。讨论了苯基取代基和酯基对抗高血压活性的影响。几种化合物显示出比尼卡地平更强的抗高血压活性，并且大多数化合物具有更长的作用持续时间。其中，7B.HCl（TC-81）表现出高效且持久的活性，并被选为进一步药理研究的候选物。
