[PAF-acether antagonistic pyrrolo[1,2-c]thiazoles: from RP 48740 to RP 59227].
The optimisation of the PAF antagonistic activity of RP 48740 led to the discovery of still more potent molecules of the pyrrolo[1,2-c]thiazole family: RP 52629, RP 52770 and RP 59227. The latter compound, for which a stereo-specific synthesis was developed, exhibits a very high potency as a PAF receptor antagonist.
Rhône-Poulenc Santé, Centre de Recherches de Vitry-Alfortville, Vitry-sur-Seine, France.
D
D
Lavé
C
C
James
H
H
Rajoharison
A
A
Floch
C
C
Robaut
P
P
Sedivy
D000818:Animals; D006801:Humans; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D011725:Pyridines / Q000494:pharmacology*; D013844:Thiazoles / Q000494:pharmacology*
D010972:Platelet Activating Factor; D011725:Pyridines; D013844:Thiazoles; C065022:RP 59227; C052520:3-(3-pyridinyl)-1H,3H-pyrrolo(1,2-c)thiazole-7-carboxamide
Pyrrolo[1,2-c]thiazoles antagonistes du PAF-acéther: du RP 48740 au RP 59227.