Synthesis and antihypertensive activity of N-(alkyl/alkenyl/aryl)-N-heterocyclic ureas and thioureas
| Autor: | Chutima Matayatsuk, William O. Foye, Opa Vajragupta, Lek Ruangreangyingyod, Yuvadee Wongkrajang, Aungkana Pathomsakul |
|---|---|
| Rok vydání: | 1996 |
| Předmět: |
Male
Time Factors Stereochemistry Pharmaceutical Science Blood Pressure chemistry.chemical_compound Pyridine Prazosin medicine Potency Animals Urea Rats Wistar Alkyl Antihypertensive Agents chemistry.chemical_classification Dose-Response Relationship Drug Chemistry Quinoline Thiourea Rats Heterocyclic compound Rabbits medicine.drug |
| Zdroj: | Scopus-Elsevier |
| ISSN: | 0022-3549 |
| Popis: | A variety of N-(alkyl/alkenyl/aryl-N-heterocyclic ureas and thioureas were synthesized as potential antihypertensives. The selected heterocyclic nuclei were the 6-substituted quinoline and the pyridine. Eleven synthesized compounds and seven related compounds in the series were evaluated orally at a dose of 100 mg/kg in conscious deoxycorticosterone acetate/saline-treated hypertensive rats by the tail-cuff method. Seventeen out of the eighteen tested compounds possessed significant antihypertensive activity (p < 0.05). 1-n-Propyl-3-[2'-(6-methoxy)quinolyl]urea (9), showing 29.1% reduction in systolic blood pressure, was the most active compound in the series. Two other compounds producing a fall in systolic blood pressure of the same magnitude were 1-allyl-3-[2'-(6-methyl)quinolyl]thiourea (4) and 1-n-propyl-3-[(2'-pyridyl)methyl]urea (17). Compound 17 with rapid onset caused significant relaxation (p < 0.01) of isolated rabbit femoral artery and guinea pig atrium but had no effect on heart rate. However, none of these exhibited higher potency than prazosin (5 mg/kg). The potency, onset, and duration of action improved when the heterocyclic nucleus was pyridine. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text