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1.
Bioorg Med Chem ; 10(7): 2283-90, 2002 Jul.
Article in English | MEDLINE | ID: mdl-11983525

ABSTRACT

In order to clarify an index which could be used as proof of the presence of hydroxyl radical, a new standard isomer distribution ratio of phenols formed from aromatic hydroxylation with [(4-bromophenyl)diazenyl](phenyl)methyl hydroperoxide 4, which is a stable source of hydroxyl radical, under a new appropriate photolysis condition in the presence or absence of benzoquinones is reported. We also demonstrated the strong electrophilic properties of hydroxyl radical in reference to earlier results of electron density calculations.


Subject(s)
Hydroxyl Radical/chemistry , Chromatography, Gas , Photochemistry
2.
Bioorg Med Chem ; 10(5): 1399-415, 2002 May.
Article in English | MEDLINE | ID: mdl-11886803

ABSTRACT

The synthesis and biological activity of novel 1-phenylsulfonyl-4- phenylsulfonylaminopyrrolidine analogues are described. All compounds were produced through modification of the substituent formally corresponding to the 1,3-dioxane ring system and the omega-octenol side chain of thromboxane A(2) (TXA(2)), in reference to the structure of Daltroban. Several compounds were found to be potent TXA(2) receptor antagonists. Compound 51a was the most effective inhibitor of 9,11-epoxymethano PGH(2) (U-46619)-induced rat aortic strip contraction (IC(50)=0.48 nM).


Subject(s)
Pyrrolidines/chemical synthesis , Pyrrolidines/pharmacology , Receptors, Thromboxane/antagonists & inhibitors , Sulfonamides/chemical synthesis , Sulfonamides/pharmacology , 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid/antagonists & inhibitors , Animals , Aorta , Disease Models, Animal , Dogs , Guinea Pigs , Haplorhini , Humans , Male , Mice , Muscle Contraction/drug effects , Muscle, Smooth, Vascular/drug effects , Platelet Aggregation/drug effects , Pulmonary Embolism/drug therapy , Pulmonary Embolism/prevention & control , Pyrrolidines/chemistry , Rabbits , Rats , Structure-Activity Relationship , Sulfonamides/chemistry , Thrombosis/drug therapy , Thrombosis/prevention & control , Vasoconstrictor Agents/antagonists & inhibitors
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