Synthesis and Pharmacological Evaluation of N-(6-Functionalized-amino-3-pyridyl)-N'-bicycloalkyl-N'-cyanoguanidines as Antihypertensive Agents
| العنوان: | Synthesis and Pharmacological Evaluation of N-(6-Functionalized-amino-3-pyridyl)-N'-bicycloalkyl-N'-cyanoguanidines as Antihypertensive Agents |
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| المؤلفون: | T. Takemoto, Hiroshi Sakashita, Sumio Matzno, Norifumi Nakamura, T. Okada, Masahiro Eda, Kazutaka Hayashi, Chikara Fukaya, Maki Gohda |
| المصدر: | Chemical and Pharmaceutical Bulletin. 44:307-313 |
| بيانات النشر: | Pharmaceutical Society of Japan, 1996. |
| سنة النشر: | 1996 |
| مصطلحات موضوعية: | Male, Potassium Channels, Stereochemistry, Potassium, chemistry.chemical_element, Blood Pressure, In Vitro Techniques, Guanidines, Chemical synthesis, Muscle, Smooth, Vascular, Structure-Activity Relationship, chemistry.chemical_compound, Rats, Inbred SHR, Drug Discovery, Animals, Structure–activity relationship, Rats, Wistar, Diuretics, Antihypertensive Agents, Histidine, Alanine, chemistry.chemical_classification, Portal Vein, Chemistry, Pinacidil, General Chemistry, General Medicine, Rats, Amino acid, Depression, Chemical, Hypertension, Potassium channel opener |
| الوصف: | A series of amino acid conjugates of N-(6-amino-3-pyridyl)-N'-[exo-bicyclo[2.2.1]hept-2-yl]-N''- cyanoguanidine (4) were prepared and evaluated as antihypertensive agents. The parent compound 4 showed potent potassium channel-opening and antihypertensive activities, but with undesirable changes of the urinary balance of electrolytes. However, alanine and histidine congeners (9,19) reduced this undesirable side effect of 4 through improved pharmacokinetics without loss of antihypertensive activity. They also provided additional information on the structural requirements for pinacidil-type potassium channel openers. |
| تدمد: | 1347-5223 0009-2363 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5406d1be55913de17cf540daa1e179fTest https://doi.org/10.1248/cpb.44.307Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....b5406d1be55913de17cf540daa1e179f |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 13475223 00092363 |
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