Author/Editor		Anderluh, Marko; Cesar, Jožko; Štefanič, Petra; Kikelj, Danijel; Janeš, Damjan; Murn, Jernej; Nadrah, Kristina; Tominc, Mojca; Addicks, Elisabeth; Giannis, Athanassios; Stegnar, Mojca; Sollner-Dolenc, Marija
Title		Design and synthesis of novel platelet fibrinogen receptor anatagonists with 2H-1,4-benzoxazine-3(4H)-one scaffold. A systematic study
Type		članek
Source		Eur J Med Chem
Vol. and No.		Letnik 40
Publication year		2005
Volume		str. 25-49
Language		eng
Abstract		New platelet glycoprotein IIb/IIIa (GP IIb/IIIa, integrin alphapibbeta3) antagoniscs were prepared on a 2H-1,4-benzoxazine-3(4H)-one scaffold. Their anti-aggregatory activities in human platelet rich plasma and their affinity towards alphapibbeta3 and alphapibbeta3 integrins were assessed. Various substitution positions and side chain variations were studied. In contrast to the generally accepted model, compounds containing ethyl esters as aspartate mimetics were in general more active than the corresponding free acids. We suggest an explanation for the observed behaviour of these new compounds.
Descriptors		PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX DRUG DESIGN PLATELET AGGREGATION INHIBITORS CHEMISTRY, PHARMACEUTICAL TECHNOLOGY, PHARMACEUTICAL