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Titolo:
ETHYL]-3-(2-PHENYLETHOXY)-2-PYRIDINYL]-2-PROPENOIC ACID - A HIGH-AFFINITY LEUKOTRIENE B-4 RECEPTOR ANTAGONIST WITH ORAL ANTIINFLAMMATORY ACTIVITY
Autore:
DAINES RA; CHAMBERS PA; FOLEY JJ; GRISWOLD DE; KINGSBURY WD; MARTIN LD; SCHMIDT DB; SHAM KKC; SARAU HM;
Indirizzi:
SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM,POB 1539 KING OF PRUSSIA PA 19406 SMITHKLINE BEECHAM PHARMACEUT,DEPT PHARMACOL KING OF PRUSSIA PA 19406
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 19, volume: 39, anno: 1996,
pagine: 3837 - 3841
SICI:
0022-2623(1996)39:19<3837:EA-AH>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN POLYMORPHONUCLEAR LEUKOCYTES; ARACHIDONIC-ACID; INFLAMMATION; INHIBITION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
18
Recensione:
Indirizzi per estratti:
Citazione:
R.A. Daines et al., "ETHYL]-3-(2-PHENYLETHOXY)-2-PYRIDINYL]-2-PROPENOIC ACID - A HIGH-AFFINITY LEUKOTRIENE B-4 RECEPTOR ANTAGONIST WITH ORAL ANTIINFLAMMATORY ACTIVITY", Journal of medicinal chemistry, 39(19), 1996, pp. 3837-3841

Abstract

An extensive structure-activity study based around the high-affinity leukotriene B-4 (LTB(4)) receptor antagonist SB 201146 (1) led to the identification of ethyl]-3-(2-phenylethoxy)-2-pyridinyl]-2-propenoic acid (3). This compound displays high affinity for the human neutrophilLTB(4) receptor (K-i = 0.78 nM), blocks LTB(4)-induced Ca2+ mobilization with an IC50 of 6.6 +/- 1.5 nM, and demonstrates potent oral and topical antiinflammatory activity in a murine model of dermal inflammation.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 05:16:55