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August 2010
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27 Reads
ChemInform
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
May 1998
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30 Reads
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111 Citations
Journal of Medicinal Chemistry
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.
December 1997
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29 Reads
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50 Citations
Bioorganic & Medicinal Chemistry Letters
Several thiazolidinediones having indol as heterocyclic moiety have been synthesized and evaluated for euglycemic properties. A few of them have been found to be superior to troglitazone.
... With the aim to develop a more efficient synthetic process for the synthesis of highly functionalized 5-arylidene rhodanines 3a-v from the building blocks 1a-i and 2a-p, microwave irradiation was employed to shorten the reaction times in comparison to conventional heating. For the reported methods, the Knoevenagel condensations have been realized in the presence of catalyst with various solvents: sodium acetate in glacial acetic acid [48] or in ethanol [46], piperidinium benzoate in toluene [49], tetrabutylammonium bromide in water [50], and piperidine in ethanol [51], using conventional heating in an oil bath. These older protocols suffer from one or more limitations, such as requiring harsh reaction conditions, low moderate yields, cumbersome experimental process, and long reaction time. ...
December 1997
Bioorganic & Medicinal Chemistry Letters
... The substituents at carbon-2 and carbon-3 of indole significantly reduce the euglycemic and hypolipidemic actions. [16,17] Darwish KM developed, produced, and tested a unique class of thiazolidinediones (TZDs) from benzhydrol and indole for their binding affinity to two receptors: PPAR-E and FFAR1, also known as GPCR40. There are three compounds that have a high affinity for both targets. ...
May 1998
Journal of Medicinal Chemistry
