rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
8
|
pubmed:dateCreated |
2006-4-13
|
pubmed:abstractText |
In a preliminary work, we reported two NO-sartans, possessing the characteristics of an AT(1) antagonist and a "slow NO donor", obtained by adding NO-donor side chains to losartan 1. The NO release from an NO-sartan should be modulated in order to strengthen the antihypertensive activity of the native drug and to ensure additional effects, such as the antiplatelet and anti-ischemic ones. To obtain a collection of prototypical NO-sartans, showing different rates of NO release, new NO-donor moieties have been linked to 1 or its active metabolite 2 (EXP 3174). Almost all the synthesized compounds exhibited both AT(1)-antagonist and NO-mediated vasorelaxing properties, with a wide range of NO-releasing rates. Further pharmacological investigation on compound 4a showed that it possessed antihypertensive and cardiac antihypertrophic effects similar to those of the reference AT(1)-blocking or ACE-inhibiting drugs. Furthermore, the additional anti-ischemic cardio-protective properties and antiplatelet effects of 4a have been preliminarily investigated.
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pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Apr
|
pubmed:issn |
0022-2623
|
pubmed:author |
pubmed-author:BalsamoAldoA,
pubmed-author:BreschiMaria CMC,
pubmed-author:CalderoneVincenzoV,
pubmed-author:DigiacomoMariaM,
pubmed-author:MacchiaMarcoM,
pubmed-author:MartelliAlmaA,
pubmed-author:MartinottiEnricaE,
pubmed-author:MinutoloFilippoF,
pubmed-author:RapposelliSimonaS,
pubmed-author:RosselloArmandoA,
pubmed-author:TestaiLaraL
|
pubmed:issnType |
Print
|
pubmed:day |
20
|
pubmed:volume |
49
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2628-39
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:16610806-Angiotensin II Type 1 Receptor Blockers,
pubmed-meshheading:16610806-Animals,
pubmed-meshheading:16610806-Antihypertensive Agents,
pubmed-meshheading:16610806-Drug Design,
pubmed-meshheading:16610806-Drug Evaluation, Preclinical,
pubmed-meshheading:16610806-Hypertension,
pubmed-meshheading:16610806-Losartan,
pubmed-meshheading:16610806-Male,
pubmed-meshheading:16610806-Molecular Structure,
pubmed-meshheading:16610806-Rats,
pubmed-meshheading:16610806-Rats, Wistar,
pubmed-meshheading:16610806-Receptor, Angiotensin, Type 1,
pubmed-meshheading:16610806-Structure-Activity Relationship,
pubmed-meshheading:16610806-Time Factors
|
pubmed:year |
2006
|
pubmed:articleTitle |
New NO-releasing pharmacodynamic hybrids of losartan and its active metabolite: design, synthesis, and biopharmacological properties.
|
pubmed:affiliation |
Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
|
pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|