- Studies on New Acidic Azoles as Glucose-Lowering Agents in Obese, Diabetic db/db Mice
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Bioisosteric substitution was used as a tool to generate several new structural alternatives to the thiazolidine-2,4-dione and tetrazole heterocycles as potential antidiabetic agents.Among the initial leads that emerged from this strategy, a family of aci
- Kees, Kenneth L.,Caggiano, Thomas J.,Steiner, Kurt E.,Fitzgerald, John J.,Kates, Michael J.,et al.
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- Coumarins as novel 17β-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer
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The synthesis and SAR studies of 3- and 4-substituted 7-hydroxycoumarins as novel 17β-HSD3 inhibitors are discussed. The most potent compounds from this series exhibited low nanomolar inhibitory activity with acceptable selectivity versus other 17β-HSD isoenzymes and nuclear receptors.
- Harada, Koichiro,Kubo, Hideki,Tomigahara, Yoshitaka,Nishioka, Kazuhiko,Takahashi, Junya,Momose, Mio,Inoue, Shinichi,Kojima, Atsuyuki
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scheme or table
p. 272 - 275
(2010/04/06)
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- Deacylative oxidation strategy for the preparation of α- functionalized carbonyls
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(Matrix Presented) α-Alkoxylation and amination of carbonyl derivatives is made possible through a unique deacylative coupling reaction that proceeds via in situ Rh-carbene formation and subsequent heteroatom-H (X-H) insertion. Reactions perform optimally
- Brodsky, Benjamin H.,Du Bois
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p. 2619 - 2621
(2007/10/03)
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- Nonpeptide endothelin antagonists: From lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids
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Random screening of compounds in endothelin receptor (ET(A) and ET(B)) binding assays led to the discovery of a new class of pyrazol-5-ol ligands. Characterization of structural features crucial for binding activities of these pyrazol-5-ols, by structure-activity-relationship (SAR) studies, allowed us to design a novel class of pyrazole-5-carboxylic acids as more potent ET antagonists. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Zhang, Jidong,Didierlaurent, Stanislas,Fortin, Michel,Lefrancois, Dominique,Uridat, Eric,Vevert, Jean Paul
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p. 1351 - 1355
(2007/10/03)
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- ALKYLATION DU TRIFLUOROACETYLACETATE D'ETHYLE METHODE GENERALE D'ACCES AUX TRIFLUOROMETHYLCETONES. 2eme PARTIE: ALKYLATIONS INDIRECTS DU TFAAE
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A versatile method of alkylation of ethyltrifluoroacetylacetate (ETFAA) allowed selective C-alkylation of ETFAA, whatever the structure of alkyl halide was, providing that the carbonyl function was masked into a dioxolan 3 or a N,N-dimethyl hydrazone 5.These last derivatives were easily alkylated and their specific deprotection led to various C-alkylated ETFAA which in turn allowed, by a simple decarbethoxylation, the preparation of the corresponding trifluoromethyl ketones in good yields.
- Aubert, Corinne,Begue, Jean-Pierre,Charpentier-Morize, Micheline,Nee, Gerard,Langlois, Bernard
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p. 377 - 394
(2007/10/02)
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- METHODE GENERALE D'ACCES AUX TRIFLUOROMETHYLCETONES. 1ere PARTIE: ALKYLATION DIRECTE DU TRIFLUOROACETYLACETATE D'ETHYLE
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Alkylation of Ethyl 4,4,4 trifluoroacetylacetate (ETFAA) 1 by alkyl halides presented some typical features.The reaction was very slow and led preferentially to O-alkylated products.However, with activated halides and under some peculiar conditions, it was possible to obtain selectively C-alkylated products 3 and 4 in good yields.
- Aubert, Corinne,Begue, Jean-Pierre,Charpentier-Morize, Micheline,Nee, Gerard,Langlois, Bernard
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p. 361 - 376
(2007/10/02)
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- Alkylation of Ethyl 4,4,4-Trifluoroacetoacetate. First Example of a Reversible O-Alkylation Process leading to C-Alkylation
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In aprotic polar solvents the ratio of O vs.C alkylation products of ethyl 4,4,4-trifluoroacetoacetate (ETFAA) can be dependent on reaction time; in hexamethylphosphoric triamide (HMPA) or acetone, the SN2 cleavage of enol ethers of ETFAA with sodium iodide was observed with concomitant formation of the sodium enolate and the corresponding iodides, and in the case of an activated iodide the mono- and di-alkylation products resulted quantitavely.
- Begue, Jean-Pierre,Charpentier-Morize, Micheline,Nee, Gerard
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