Document Detail


(6-methyl-2-methylsulfanyl-4-oxo-3,4-dihydro-3-pyrimidinyl)acetic acid and related compounds exhibiting anti-inflammatory activity.
MedLine Citation:
PMID:  12369447     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Base-promoted hydrolysis of methyl or ethyl esters 1a-c gave the (6-methyl-2-methylsulfanyl-4-oxo-3,4-dihydro-3-pyrimidinyl)- and (5-ethyl-6-methyl-2-methylsulfanyl-4-oxo-3,4-dihydro-3-pyrimidinyl)acetic acids 2a, b. Under the reaction of ester 1a or acid 2a with nucleophilic reagents a series of derivatives 3-7 of acid 2a were synthesized and evaluated for their anti-inflammatory activity. Most of them were found to be more active than acetylsalicylic acid, and compounds 2a, 6a, b, 7a, f were significantly more active than ibuprofen. The compounds exhibiting the best anti-inflammatory activity showed negative inotropic effect.
Authors:
V Jakubkiene; M M Burbuliene; E Udrenaite; V Garaliene; P Vainilavicius
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Die Pharmazie     Volume:  57     ISSN:  0031-7144     ISO Abbreviation:  Pharmazie     Publication Date:  2002 Sep 
Date Detail:
Created Date:  2002-10-08     Completed Date:  2002-11-05     Revised Date:  2007-01-29    
Medline Journal Info:
Nlm Unique ID:  9800766     Medline TA:  Pharmazie     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  610-3     Citation Subset:  IM    
Affiliation:
Faculty of Chemistry, Vilnius University, Lithuania. virginija.jakubkiene@chf.vu.lt
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MeSH Terms
Descriptor/Qualifier:
Acetic Acids / chemical synthesis*,  pharmacology*,  toxicity
Animals
Anti-Arrhythmia Agents / chemical synthesis,  pharmacology
Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*,  pharmacology*,  toxicity
Carrageenan
Edema / chemically induced,  prevention & control
Indicators and Reagents
Lethal Dose 50
Magnetic Resonance Spectroscopy
Male
Mice
Mice, Inbred BALB C
Myocardial Contraction
Papillary Muscles / drug effects
Pyrimidines / chemical synthesis*,  pharmacology*,  toxicity
Rats
Rats, Wistar
Chemical
Reg. No./Substance:
0/(6-methyl-2-methylsulfanyl-4-oxo-3,4-dihydro-3-pyrimidinyl)acetic acid; 0/Acetic Acids; 0/Anti-Arrhythmia Agents; 0/Anti-Inflammatory Agents, Non-Steroidal; 0/Indicators and Reagents; 0/Pyrimidines; 9000-07-1/Carrageenan

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