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Titolo:
New carbamoylpiperidines as human platelet aggregation inhibitors
Autore:
Guo, ZM; Zheng, XZ; Thompson, W; Dugdale, M; Gollamudi, R;
Indirizzi:
Univ Tennessee, Dept Pharmaceut Sci, Memphis, TN 38163 USA Univ TennesseeMemphis TN USA 38163 Pharmaceut Sci, Memphis, TN 38163 USA Univ Tennessee, Dept Med, Memphis, TN 38163 USA Univ Tennessee Memphis TNUSA 38163 ssee, Dept Med, Memphis, TN 38163 USA
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 5, volume: 8, anno: 2000,
pagine: 1041 - 1058
SICI:
0968-0896(200005)8:5<1041:NCAHPA>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN-BLOOD PLATELETS; CHEMICAL-STRUCTURE; ANTIPLATELET NIPECOTAMIDES; INOSITOL PHOSPHATES; NITRIC-OXIDE; ALPHA,ALPHA'-BIS<3-(N,N-DIETHYLCARBAMOYL)PIPERIDINO>-P-XYLENE; PHOSPHORYLATION; PHYSIOLOGY; SEROTONIN; ENTITIES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
35
Recensione:
Indirizzi per estratti:
Indirizzo: Gollamudi, R Univ Tennessee, Dept Pharmaceut Sci, Memphis, TN 38163 USA Univ Tennessee Memphis TN USA 38163 i, Memphis, TN 38163 USA
Citazione:
Z.M. Guo et al., "New carbamoylpiperidines as human platelet aggregation inhibitors", BIO MED CH, 8(5), 2000, pp. 1041-1058

Abstract

A series of 3-carbamoylpiperidines (nipecotamides) are designed, synthesized and tested for their inhibitory action against adenosine diphosphate (ADP)-induced aggregation of human platelets. A structure-activity analysis ofthe bis(nipecotamido)aralkane type showed that a substituent on the piperidine ring should preferably be an amide and that the electronegativity of the carbonyl oxygen and the orientation of the amide group affected activities. Based on the knowledge of factors influencing platelet activation and aggregation, a nitric ester moiety which could release nitric oxide (NO) in situ, is incorporated into the nipecotamide structure. These compounds exhibit increased activity compared to those having no -ONO2 function. They also show stereoselectivity, with the meso isomer being approximately twice aspotent as the synthetic diastereomeric mixture. Replacement of the -ONO2 function with hydroxyl, ester or alkyl groups considerably diminishes aggregation-inhibitory potential. Nipecotamides are shown here to inhibit the basal and collagen-induced rise in platelet inositol trisphosphate (IP3) levels, as well as phosphoinositide turnover. A comprehensive mechanism of action is proposed taking: earlier results into consideration. (C) 2000 ElsevierScience Ltd. All rights reserved.

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Documento generato il 18/01/20 alle ore 10:37:39