| (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 |
Related Documents
:
|
17193237 - Synthesis and pharmacological evaluation of some dual-acting amino-alcohol ester deriva... 21196377 - Tryptophan metabolism in animals: important roles in nutrition and health. 15018307 - Propionibacterium acnes lipase in seborrheic dermatitis and other skin diseases and uns... 6891217 - Non-steroidal anti-inflammatories--xii. mode of action of anti-inflammatory methane sul... 11270327 - Stereoselectivity of the folate transporter in rabbit small intestine: studies with ame... 12179967 - Phospholipid signalling in plant defence. |
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 |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| 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 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Bis(lactone)-annulated 4H-pyranes and 1,4-dihydropyridines from 3,3'-(nitrobenzlidene)-bistetronic a...
Next Document: Methoxychalcones and methoxyflavanones in analytical studies.