Evaluation of some benzyl and benzylidene monosubstituted gamma-butyrolactones and tetrahydrofurans as platelet activating factor antagonist agents.
Some benzyl and benzylidene monosubstituted gamma-butyrolactones and tetrahydrofurans were applied as platelet activating factor (PAF) antagonist agents. The results indicated that, whereas all benzyl derivatives are completely inactive, benzylidene substitution is the key feature for obtaining moderate activity. Molecular modeling and molecular electrostatic potential mapping are applied in conjunction with the most recent PAF-receptor model to rationalize the results.
Coran
S A
SA
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
Giannellini
V
V
Bambagiotti-Alberti
M
M
Moriggi
E
E
Sala
R
R
Valle
G
G
D015107:4-Butyrolactone / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001593:Benzyl Compounds / Q000138:chemical synthesis / Q000378:metabolism; D018360:Crystallography, X-Ray; D005663:Furans / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008968:Molecular Conformation; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D010980:Platelet Membrane Glycoproteins / Q000378:metabolism; D011817:Rabbits; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D013329:Structure-Activity Relationship
D001593:Benzyl Compounds; D005663:Furans; D010972:Platelet Activating Factor; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor; C018674:tetrahydrofuran; D015107:4-Butyrolactone