SYNTHESIS OF A 2,5-DIARYLOXAZOLINE AS A POTENTIAL PLATELET-ACTIVATING-FACTOR ANTAGONIST

Authors
PEET NP BURKHART JP BROERSMA RJ HEMINGER EF
Citation
Np. Peet et al., SYNTHESIS OF A 2,5-DIARYLOXAZOLINE AS A POTENTIAL PLATELET-ACTIVATING-FACTOR ANTAGONIST, Journal of heterocyclic chemistry, 31(2), 1994, pp. 419-423
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Journal of heterocyclic chemistry → ACNP
ISSN journal
0022152X
Volume
31
Issue
2
Year of publication
1994
Pages
419 - 423
Database
ISI
SICI code
0022-152X(1994)31:2<419:SOA2AA>2.0.ZU;2-#
Abstract
2,5-Bis-(3,4,5-trimethoxyphenyl)-2-oxazoline (5, MDL 100,270) was desi gned as a potential platelet-activating factor (PAF) antagonist on the basis of computer modeling comparison studies with known PAF antagoni sts. An efficient, four-step synthesis of oxazoline 5 was developed, s tarting from 3,4,5-trimethoxybenzaldehyde (6). Oxazoline 5 was found t o inhibit the PAF-induced aggregation of human platelets with an IC50 value of 708 muM.