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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
1995-12-19
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pubmed:abstractText |
Various 2-aminothiazoles (2a-s and 3a-g) and 2-thiazolecarboxamides (4a-h), possessing a nitrogenous basic moiety at the C-2 position of the thiazole ring, were prepared and tested for anti-anoxic (AA) activity in mice. Among them, N-[2-(4-morpholinyl)ethyl]-4-(3-trifluoromethylphenyl)-2- thiazolecarboxamide hydrochloride (4e, FR108143) (minimum effective doses of 3.2 mg/kg i.p. and 10 mg/kg p.o., respectively) exhibited more potent AA activity than either FK360 or compound 1, each of which has a nitrogenous basic moiety at the C-5 position. The structure-activity relationships with regard to AA activity of this series of compounds are discussed, and the three-dimensional electrostatic potentials (3D-MEP) around the basic nitrogen atom of FK360 and the thiazole derivative (4e) are compared.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0009-2363
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
43
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
1497-504
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:7586073-Animals,
pubmed-meshheading:7586073-Chemistry, Physical,
pubmed-meshheading:7586073-Hypoxia, Brain,
pubmed-meshheading:7586073-Lethal Dose 50,
pubmed-meshheading:7586073-Lipid Peroxidation,
pubmed-meshheading:7586073-Male,
pubmed-meshheading:7586073-Mice,
pubmed-meshheading:7586073-Mice, Inbred ICR,
pubmed-meshheading:7586073-Mitochondria,
pubmed-meshheading:7586073-Physicochemical Phenomena,
pubmed-meshheading:7586073-Pyrimidines,
pubmed-meshheading:7586073-Rats,
pubmed-meshheading:7586073-Rats, Wistar,
pubmed-meshheading:7586073-Structure-Activity Relationship,
pubmed-meshheading:7586073-Thiazoles
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pubmed:year |
1995
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pubmed:articleTitle |
Studies on cerebral protective agents. VIII. Synthesis of 2-aminothiazoles and 2-thiazolecarboxamides with anti-anoxic activity.
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pubmed:affiliation |
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro
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