Synthesis of a 2,5‐diaryloxazoline as a potential platelet‐activating factor antagonist | Zendy

Peet Norton P. | Zendy; Burkhart Joseph P. | Zendy; Broersma Robert J. | Zendy; Heminger Eileen F. | Zendy

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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 .

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