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Synthesis of a 2,5‐diaryloxazoline as a potential platelet‐activating factor antagonist
Author(s) -
Peet Norton P.,
Burkhart Joseph P.,
Broersma Robert J.,
Heminger Eileen F.
Publication year - 1994
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570310229
Subject(s) - chemistry , oxazoline , antagonist , platelet activating factor , platelet , platelet aggregation , pharmacology , stereochemistry , combinatorial chemistry , receptor , biochemistry , medicine , catalysis
2,5‐Bis‐(3,4,5‐trimethoxyphenyl)‐2‐oxazoline ( 5 , MDL 100,270) was designed as a potential platelet‐activating factor (PAF) antagonist on the basis of computer modeling comparison studies with known PAF antagonists. An efficient, four‐step synthesis of oxazoline 5 was developed, starting from 3,4,5‐trimethoxybenzaldehyde ( 6 ). Oxazoline 5 was found to inhibit the PAF‐induced aggregation of human platelets with an IC 50 value of 708 μ M .