-transparent.png){kind=logo}
The synthesis and biological characterization of some 3-carboxylate isosteres of PAF-acether structurally modified in positions 1 (ether, carbamate), 2 (acetoyl, ethoxy), and 3 (chain length and polar head group) are reported. All derivatives present antagonist activities against PAF-acether-induced effects in vitro (platelet aggregation) and in vivo (bronchoconstriction and thrombocytopenia in guinea pig and, to a lesser extent, hypotension in rat). The functional modifications presented here do not modify dramatically the potency of antagonist activities, and there is no enantioselectivity. All of the isosteres are specific PAF-acether antagonists, except the 1-carbamoyl analogue, which is also potent against acetylcholine-induced hypotension and bronchoconstriction.
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
May 1987,
Journal of medicinal chemistry,
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
December 1981,
Agents and actions,
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
January 1988,
Progress in clinical and biological research,
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
January 1992,
Chemical & pharmaceutical bulletin,
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
January 2015,
Anti-inflammatory & anti-allergy agents in medicinal chemistry,
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
November 1990,
Gut,
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
December 1982,
Agents and actions,
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
January 2021,
Oxidative medicine and cellular longevity,
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
January 1986,
Comptes rendus de l'Academie des sciences. Serie III, Sciences de la vie,
B Wichrowski, and
S Jouquey, and
C Broquet, and
F Heymans, and
J J Godfroid, and
J Fichelle, and
M Worcel
August 1984,
Journal of immunology (Baltimore, Md. : 1950),
