Synthesis and Antihypertensive Activity of 1,4-Dihydropyridine Derivatives with a 4-(Disubstituted Phenyl) Ring and an Aminoalyl Ester Group: Highly Potent and Long-Lasting Calcium Antagonists
| Autor: | Yoshiaki Okamiya, Hideo Kanno, Tatsuyuki Naruchi, Kiyotaka Sunakawa, Hisao Yamaguchi, Toru Takeshita |
|---|---|
| Rok vydání: | 1992 |
| Předmět: |
Male
chemistry.chemical_classification Long lasting Dihydropyridines Chemistry Stereochemistry 1 4 dihydropyridine derivatives Nicardipine Nitro compound chemistry.chemical_element General Chemistry General Medicine Calcium Calcium Channel Blockers Ring (chemistry) Rats Structure-Activity Relationship Spontaneously hypertensive rat Rats Inbred SHR Drug Discovery medicine Animals Rats Wistar Antihypertensive Agents medicine.drug |
| Zdroj: | Chemical and Pharmaceutical Bulletin. 40:2049-2054 |
| ISSN: | 1347-5223 0009-2363 |
| DOI: | 10.1248/cpb.40.2049 |
| Popis: | New 1, 4-dihydropyridine derivatives bearing a 4-(disubstituted phenyl) ring and an aminoethyl ester or an amino-2, 2-dimethylpropyl 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·HCI (TC-81) showed highly potent and long-lasting activity and was selected as a candidate for further pharmacological investigations. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|