Synthesis and Inhibitory Effect on Platelet Aggregation and Antihypertensive Activity of 1-Hydroxy-2,5-dihydro-1H-imidazole-2- carboxylic Acid 3-Oxides, 1,3-Dihydroxyimidazolidine-2-carboxylic Acids, and 1,4-Dihydroxy-2,3-piperazinediones

The reaction of 1,2‐hydroxylamino‐oximes 1 with pyruvic or glyoxylic acid and of 1,2‐bishydroxylamines 4 with glyoxylic acid resulted in 2,5‐dihydro‐1H‐imidazole‐2‐carboxylic acid 3‐oxides 2 and 2‐imidazolidinecarboxylic acids 5, respectively. It was found that hydroxylamino acids 2 and 1,4‐dihydrox...

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Published in:	Archiv der Pharmazie (Weinheim) Vol. 332; no. 9; pp. 305 - 308
Main Authors:	Tikhonov, Aleksei Ya, Mazhukin, Dmitrii G., Grigor′eva, Larisa N., Khlestkin, Vadim K., Voinova, Natal′ya N., Syropyatov, Boris Ya, Shirinkina, Svetlana S., Volodarsky, Leonid B.
Format:	Journal Article
Language:	English
Published:	Weinheim WILEY-VCH Verlag GmbH 01-09-1999 WILEY‐VCH Verlag GmbH Wiley-VCH
Subjects:	2,5‐dihydro‐1H‐imidazole‐2‐carboxylic acids 3-piperazinediones 4-dihydroxy-2 4‐dihydroxy‐2,3‐piperazinediones 5-dihydro-1H-imidazole-2-carboxylic acids Animals antihypertensive activity Antihypertensive Agents - chemical synthesis Antihypertensive Agents - pharmacology Blood Pressure - drug effects Carboxylic Acids - chemical synthesis Carboxylic Acids - pharmacology Carboxylic Acids - toxicity Cats Imidazoles - chemical synthesis Imidazoles - pharmacology Imidazoles - toxicity imidazolidine-2-carboxylic acids In Vitro Techniques Lethal Dose 50 Mice Piperazines - chemical synthesis Piperazines - pharmacology Piperazines - toxicity Platelet Aggregation Platelet Aggregation Inhibitors - chemical synthesis Platelet Aggregation Inhibitors - pharmacology Platelet Aggregation Inhibitors - toxicity Rabbits
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Summary:	The reaction of 1,2‐hydroxylamino‐oximes 1 with pyruvic or glyoxylic acid and of 1,2‐bishydroxylamines 4 with glyoxylic acid resulted in 2,5‐dihydro‐1H‐imidazole‐2‐carboxylic acid 3‐oxides 2 and 2‐imidazolidinecarboxylic acids 5, respectively. It was found that hydroxylamino acids 2 and 1,4‐dihydroxy‐2,3‐piperazinediones 7 showed marked inhibitory effect on platelet aggregation. 1‐Hydroxy‐2‐methyl‐1,5,6,7,8,8a‐hexahydro‐2H,4H‐cycloheptimidazole‐2‐carboxylic acid 3‐oxide 2e exhibited antihypertensive activity.
Bibliography:	istex:C8618DD145C292A892E1D06F37248F622A41E224 ark:/67375/WNG-7SF6L8B9-4 ArticleID:ARDP305
ISSN:	0365-6233 1521-4184
DOI:	10.1002/(SICI)1521-4184(19999)332:9<305::AID-ARDP305>3.0.CO;2-2