Source:http://linkedlifedata.com/resource/pubmed/id/15780625
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
|
pubmed:dateCreated |
2005-3-22
|
pubmed:abstractText |
A series of novel 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones 7 were synthesized by the cyclization of 2-hydrazino-3-phenylquinazolin-4(3H)-one 6 with various one carbon donors. The starting material 2-hydrazino-3-phenylquinazolin-4(3H)-one 6, was synthesized from aniline 1 by a novel innovative route. When tested for their in vivo H(1)-antihistaminic activity on conscious guinea pigs all the test compounds protected the animals from histamine induced bronchospasm significantly, whereas the compound 1-methyl-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-one 7b (percentage protection 70.7%) was found to be equipotent with the reference standard chlorpheniramine maleate (percentage protection 71%). These compounds show negligible sedation ( approximately 5%) when compared to the reference standard (26%). Hence they could serve as prototype molecules for future development.
|
pubmed:commentsCorrections | |
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Chlorpheniramine,
http://linkedlifedata.com/resource/pubmed/chemical/Histamine H1 Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Hypnotics and Sedatives,
http://linkedlifedata.com/resource/pubmed/chemical/Quinazolines,
http://linkedlifedata.com/resource/pubmed/chemical/Triazoles
|
pubmed:status |
MEDLINE
|
pubmed:month |
Apr
|
pubmed:issn |
0960-894X
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
1
|
pubmed:volume |
15
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1877-80
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:15780625-Animals,
pubmed-meshheading:15780625-Bronchial Spasm,
pubmed-meshheading:15780625-Chlorpheniramine,
pubmed-meshheading:15780625-Cyclization,
pubmed-meshheading:15780625-Guinea Pigs,
pubmed-meshheading:15780625-Histamine H1 Antagonists,
pubmed-meshheading:15780625-Hypnotics and Sedatives,
pubmed-meshheading:15780625-Quinazolines,
pubmed-meshheading:15780625-Structure-Activity Relationship,
pubmed-meshheading:15780625-Triazoles
|
pubmed:year |
2005
|
pubmed:articleTitle |
Synthesis and pharmacological investigation of novel 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones as a new class of H1-antihistaminic agents.
|
pubmed:affiliation |
Medicinal Chemistry Laboratory, Periyar College of Pharmaceutical Sciences for Girls, Trichy 620 021, Tamilnadu, India. samy_veera@yahoo.com
|
pubmed:publicationType |
Journal Article,
Comparative Study
|