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Titolo:
NEW PYRIDAZINONE DERIVATIVES AS INHIBITORS OF PLATELET-AGGREGATION
Autore:
CORSANO S; VEZZA R; SCAPICCHI R; FORESI S; STRAPPAGHETTI G; NENCI GG; GRESELE P;
Indirizzi:
UNIV PERUGIA,INST PHARMACEUT CHEM,VIA LICEO 1 I-06123 PERUGIA ITALY UNIV PERUGIA,INST INTERNAL & VASC MED I-06126 PERUGIA ITALY
Titolo Testata:
European journal of medicinal chemistry
fascicolo: 7-8, volume: 30, anno: 1995,
pagine: 627 - 631
SICI:
0223-5234(1995)30:7-8<627:NPDAIO>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
THROMBOXANE SYNTHASE INHIBITORS; POSITIVE INOTROPIC AGENTS; CARDIOTONIC AGENTS; SYNTHETASE INHIBITION; 6-)4-(1H-IMIDAZOL-1-YL)PHENYL>-3(2H)-PYRIDAZINONES; PHOSPHODIESTERASE; INVITRO; FORMS;
Keywords:
ANTIPLATELET AGENT; HUMAN BLOOD PLATELETS; 3(2H)-PYRIDAZINONE DERIVATIVE; THROMBOXANE SYNTHASE INHIBITION;
Tipo documento:
Note
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
20
Recensione:
Indirizzi per estratti:
Citazione:
S. Corsano et al., "NEW PYRIDAZINONE DERIVATIVES AS INHIBITORS OF PLATELET-AGGREGATION", European journal of medicinal chemistry, 30(7-8), 1995, pp. 627-631

Abstract

The synthesis and evaluation of the biological activity of a series of 3(2H)-pyridazinone derivatives is reported. We assessed the in vitroactivity of these compounds on aggregation and production of thromboxane A(2) and prostaglandin E(2) of human platelets. In compounds 11 and 14 the 3-phenylpropyl group is hr-linked to the 2 position of the pyridazinone ring of 6-(1H-imidazole-1-yl)-3(2H)-pyridazinone 3 or -[4-(1H-imidazole-1-yl)-phenyl]-3(2H)-pyridazinone 4, respectively. These compounds inhibited platelet aggregation induced by arachidonic acid, ADP and collagen, and simultaneously suppressed the synthesis of TxA(2)and increased the production of PGE(2). These results characterize compounds 11 and 14 as thromboxane synthase inhibitors. However, the inhibition of platelet aggregation induced by U46619 and of the first wave of ADP-induced aggregation, which is not normally observed with thromboxane synthase inhibitors, suggests additional mechanisms of action for our compounds. On the basis of structural similarities with compounds described previously, these are possibly related to a phosphodiesterase inhibitory activity.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/09/20 alle ore 10:56:33