Synthesis and antihypertensive activity of 2,4-dioxoimidazolidin-1-yl and perhydro-2,4-dioxopyrimidin-1-yl ergoline derivatives
| Autor: | Ernesto Lamberti, Laura Chiodini, Enzo Brambilla, Daniela Ruggieri, Sergio Mantegani, Carla Caccia, Patricia Salvati, Enrico Di Salle |
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| Rok vydání: | 1998 |
| Předmět: |
Male
Chemistry Stereochemistry Dopaminergic Pharmaceutical Science Pharmacology Chemical synthesis Acute toxicity Rats Ergoline Rats Sprague-Dawley Mice Structure-Activity Relationship Oral administration Rats Inbred SHR Drug Discovery Toxicity medicine Animals Potency Structure–activity relationship Female Ergolines Antihypertensive Agents medicine.drug |
| Zdroj: | Il Farmaco. 53:293-304 |
| ISSN: | 0014-827X |
| DOI: | 10.1016/s0014-827x(98)00023-8 |
| Popis: | The synthesis and antihypertensive activity of a series of 2,4-dioxoimidazolidin-1-yl and perhydro-2,4-dioxopyrimidin-1-yl ergoline derivatives are reported. The oral antihypertensive activity was studied in spontaneously hypertensive rats (SHRs) by measuring systolic blood pressure by an indirect tail-cuff method at different times after treatment. The prolactin lowering activity (indirectly measured by the nidation test) in rats and the oral acute toxicity in mice were also studied. The results of this study revealed potent antihypertensive ergoline derivatives devoid of side-effects related to the dopaminergic stimulation and the importance of the delta 9,10 double bond for conferring high potency within these compounds. |
| Databáze: | OpenAIRE |
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