rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
10
|
pubmed:dateCreated |
1998-5-28
|
pubmed:abstractText |
A series of [[(heterocyclyl)ethoxy]benzyl]-2,4-thiazolidinediones have been synthesized by the condensation of corresponding aldehyde 1 and 2,4-thiazolidinedione followed by hydrogenation. Both unsaturated thiazolidinedione 2 and its saturated counterpart 3 have shown antihyperglycemic activity. Many of these compounds have shown superior euglycemic and hypolipidemic activity compared to troglitazone (CS 045). The indole analogue DRF-2189 (3g) was found to be a very potent insulin sensitizer, comparable to BRL-49653 in genetically obese C57BL/6J-ob/ob and 57BL/KsJ-db/db mice. Pharmacokinetic and tissue distribution studies conducted on BRL-49653 and DRF-2189 (3g) indicate that these drugs are well-distributed in target tissues. On the basis of euglycemic activity as well as enhanced selectivity against reduction of triglycerides in plasma, DRF-2189 (3g) has been selected for further evaluation.
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pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0022-2623
|
pubmed:author |
pubmed-author:BhushanVV,
pubmed-author:ChakrabartyBB,
pubmed-author:JajooH KHK,
pubmed-author:LohrayB BBB,
pubmed-author:MadhavanG RGR,
pubmed-author:MamidiR NRN,
pubmed-author:MuraliNN,
pubmed-author:RajagopalanRR,
pubmed-author:RajeshB MBM,
pubmed-author:RaoB PBP,
pubmed-author:RaoK NKN,
pubmed-author:ReddyA KAK,
pubmed-author:ReddyP GPG,
pubmed-author:SubramanianRR,
pubmed-author:VikramadithyanR KRK
|
pubmed:issnType |
Print
|
pubmed:day |
7
|
pubmed:volume |
41
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1619-30
|
pubmed:dateRevised |
2010-11-18
|
pubmed:meshHeading |
pubmed-meshheading:9572887-Animals,
pubmed-meshheading:9572887-Blood Glucose,
pubmed-meshheading:9572887-Drug Evaluation, Preclinical,
pubmed-meshheading:9572887-Hypoglycemic Agents,
pubmed-meshheading:9572887-Hypolipidemic Agents,
pubmed-meshheading:9572887-Indoles,
pubmed-meshheading:9572887-Male,
pubmed-meshheading:9572887-Mice,
pubmed-meshheading:9572887-Mice, Inbred C57BL,
pubmed-meshheading:9572887-Rats,
pubmed-meshheading:9572887-Rats, Wistar,
pubmed-meshheading:9572887-Structure-Activity Relationship,
pubmed-meshheading:9572887-Thiazoles,
pubmed-meshheading:9572887-Thiazolidinediones,
pubmed-meshheading:9572887-Tissue Distribution,
pubmed-meshheading:9572887-Triglycerides
|
pubmed:year |
1998
|
pubmed:articleTitle |
Novel euglycemic and hypolipidemic agents. 1.
|
pubmed:affiliation |
Medicinal and Organic Chemistry, Pharmacology, and Clinical Research, Dr. Reddy's Research Foundation, Bollaram Road, Miyapur Hyderabad 500 050, India.
|
pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
|