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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.
March 2005
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14 Reads
ACS National Meeting Book of Abstracts
March 2004
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7 Reads
ACS National Meeting Book of Abstracts
April 2003
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47 Reads
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39 Citations
Tetrahedron Letters
Tripeptides having a 3-bromobenzyl group at the C-termini and an acryloyl group at the N termini undergo efficient intramolecular Heck reactions to afford the corresponding cyclic peptides in good yields. Synthesis of two such peptides is discussed.
August 2001
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53 Reads
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97 Citations
European Journal of Medicinal Chemistry
We report here the synthesis of a series of 5-[4-[2-[substituted phthalazinones-2(or 4)yl]ethoxy]phenylmethyl]thiazolidine-2,4-diones and 5-[4-[2-[2,3-benzoxazine-4-one-2-yl]ethoxy]phenylmethyl]thiazolidine-2,4-diones and their plasma glucose and plasma triglyceride lowering activity in db/db mice. In vitro PPARgamma transactivation assay was performed in HEK 293T cells. In vitro and in vivo pharmacological studies showed that the phthalazinone analogue has better activity. PHT46 (compound 5a), the best compound in this series, showed better in vitro PPARgamma transactivation potential than troglitazone and pioglitazone. In insulin resistant db/db mice, PHT46 showed better plasma glucose and triglyceride lowering activity than the standard drugs. Pharmacokinetic study in Wistar rats showed good systemic exposure of PHT46. Subchronic toxicity study in Wistar rats did not show any treatment-related adverse effect.
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 helix-turn-helix (HTH) motif is instrumental to many DNA-binding proteins such as transcription factors that are capable of recognizing a particular DNA sequence for regulatory purposes [27]. To develop chemical probes gauging DNA-protein interactions, Iqbal et al. designed cyclic peptides bridged by a meta benzene ring such as 10 ( Figure 2A) [28]. As the final step of their synthesis, acyclic substrate 9 was treated with Pd(OAc) 2 , tri(o-tolyl)phosphine, and diisopropylethylamine in refluxing acetonitrile for 36 h. ...
April 2003
Tetrahedron 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
... The phthalazin-1(2H)-one scaffold is one valuable diazaheterocyclic scaffold due to its wide pharmacological profile [1] as well as its applications in agrochemicals [2] and functional materials. [3] In particular, the phthalazin-1(2H)-ones bearing substitutions on C4-position display potent medicinal properties as anticancer, [4] antimicrobial, [5] anti-inflammatory, [6] antihypertensive, [7] antidiabetic [8] and neuroprotective [9] agents ( Figure 1). ...
August 2001
European Journal of Medicinal Chemistry
