TY - JOUR
T1 - Antiinflammatory, gastrosparing, and antiplatelet properties of new NO-donor esters of aspirin
AU - Cena, Clara
AU - Lolli, Marco L
AU - Lazzarato, Loretta
AU - Guaita, Elena
AU - Morini, Giuseppina
AU - Coruzzi, Gabriella
AU - McElroy, Stuart P
AU - Megson, Ian L
AU - Fruttero, Roberta
AU - Gasco, Alberto
PY - 2003
Y1 - 2003
N2 - A new series of NSAIDs in which aspirin is joined by an ester linkage to furoxan moieties, with different ability to release NO, were synthesized and tested for NO-releasing, antiinflammatory, antiaggregatory, and ulcerogenic properties. Related furazan derivatives, aspirin, its propyl ester, and its gamma-nitrooxypropyl ester were taken as references. All the products described present an antiinflammatory trend, maximized in derivatives 12, 16, and 17, they are devoid of acute gastrotoxicity, principally due to their ester nature, and show an antiplatelet activity primarily determined by their ability to release NO. They do not behave as aspirin prodrugs in human serum.
AB - A new series of NSAIDs in which aspirin is joined by an ester linkage to furoxan moieties, with different ability to release NO, were synthesized and tested for NO-releasing, antiinflammatory, antiaggregatory, and ulcerogenic properties. Related furazan derivatives, aspirin, its propyl ester, and its gamma-nitrooxypropyl ester were taken as references. All the products described present an antiinflammatory trend, maximized in derivatives 12, 16, and 17, they are devoid of acute gastrotoxicity, principally due to their ester nature, and show an antiplatelet activity primarily determined by their ability to release NO. They do not behave as aspirin prodrugs in human serum.
U2 - 10.1021/jm020969t
DO - 10.1021/jm020969t
M3 - Article
C2 - 12593655
SN - 0022-2623
VL - 46
SP - 747
EP - 754
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 5
ER -