Synthesis and antihypertensive activities of 1,4-dihydropyridine-5-phosphonate derivatives. II
| Autor: | Iwao Morita, Masahiro Kise, Masami Tsuda, Shinichi Tada, Katsutoshi Kunimoto, Kiyoshi Kimura |
|---|---|
| Rok vydání: | 1987 |
| Předmět: |
Male
Dihydropyridines Chemical Phenomena Stereochemistry Nicardipine chemistry.chemical_element Calcium Pharmacology chemistry.chemical_compound Organophosphorus Compounds Nifedipine Rats Inbred SHR Drug Discovery medicine Animals Structure–activity relationship Antihypertensive Agents Dihydropyridine Rats Inbred Strains Biological activity General Chemistry General Medicine Phosphonate Rats Chemistry Blood pressure chemistry medicine.drug |
| Zdroj: | Chemical and Pharmaceutical Bulletin. 35:4144-4154 |
| ISSN: | 1347-5223 0009-2363 |
| DOI: | 10.1248/cpb.35.4144 |
| Popis: | A series of 1, 4-dihydropyridine-5-cyclic phosphonate derivatives, designed as analogues of 1, 4- dihydropyridine-3, 5-dicarboxylate calcium antagonists, was synthesized and examined for antihypertensive activity. Several compounds were proved to have activities superior or comparable to that of nifedipine in lowering blood pressure in normotensive and spontaneously hypertensive rats (SHR). Among these compounds, methyl 2, 6-dimethyl-5- (2-oxo-1, 3, 2-dioxaphosphorinan-2-yl) -4- (2-nitrophenyl) -1, 4-dihydropyridine-3-carboxylate (31, DHP-218) was approximately 7 times more active than nifedipine in SHR and was selected for further development and clinical evaluation. The structure-activity relationships are discussed. |
| Databáze: | OpenAIRE |
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