Synthesis, platelet anti-aggregating activity and anti-inflammatory activity of a series of beta-aminoxypropionic acids.
This paper reports the platelet anti-aggregating activity induced by arachidonic acid (AA) and by adenosine-diphosphate (ADP), together with the anti-inflammatory activity evaluated by the carrageenan-induced rat paw edema method, of a series of beta-aminoxypropionic acids which were projected and synthesised as analogues of non-steroidal anti-inflammatory drugs with an arylacetic structure B, in which the aromatic group is substituted by a methyleneaminoxymethylic moiety. Some of the beta-aminoxypropionic acids were evaluated for their capacity to inhibit the cyclooxygenase enzyme by measuring the malondialdehyde (MDA) produced by incubation of sodium arachidonate with platelet-rich plasma (PRP).
Macchia
M
M
Dipartimento di Scienze Farmaceutiche, Università di Pisa.
Orlandini
E
E
Rossello
A
A
Bertini
S
S
Soldani
G
G
Baldacci
M
M
Gervasi
G
G
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011422:Propionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D010975:Platelet Aggregation Inhibitors; D011422:Propionates