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Hydroxylamine Derivatives
Author(s) -
Rehse Klaus,
Shahrouri Tawfig
Publication year - 1998
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/(sici)1521-4184(199811)331:11<365::aid-ardp365>3.0.co;2-n
Subject(s) - chemistry , hydroxylamine , organic chemistry
Twelve ethoxycarbonyl or phenylsulfonyl derivatives as prodrugs of hydroxylamine or phenylhydroxylamine were prepared and tested for antiplatelet (in vitro, Born test) antithrombotic (in vivo thrombosis model), and antihypertensive (in vivo, SHR rats) effects. In the Born test N,N ‐bisphenylsulfonylhydroxylamine ( 10 ) was most active (IC 50 = 11 μmol/L). The N ‐ethoxycarbonyl‐phenylhydroxylamine ( 7 ) was the most potent antithrombotic compound. It inhibited the thrombus formation in mesenteric arterioles of rats by 39% after a single p.o. dose of 60 mg/kg. Compound 7 lacked any antihypertensive activity. It, therefore, had been possible to seperate completely the antithrombotic activities from antihypertensive properties in suitable hydroxylamine derivatives.