26749-23-5Relevant academic research and scientific papers
A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors
Atobe, Masakazu,Maekawara, Naomi,Ishiguro, Noriko,Sogame, Shinya,Suenaga, Yoshihito,Kawanishi, Masashi,Suzuki, Hiroko,Jinno, Norimasa,Tanaka, Eiichi,Miyoshi, Shiro
, p. 2106 - 2110 (2013/04/24)
A series of thiazole bearing thiazolidin-4-one was discovered via high-throughput screening as non-competitive inhibitors of ADAMTS-5. Compound 31 appeared to give the best ADAMTS-5 inhibition and good selectivity over other metalloproteases.
Highly stereoselective double (R)-phenylglycinol-induced cyclocondensation reactions of symmetric aryl bis(oxoacids)
Amat, Mercedes,Arroniz, Carlos,Molins, Elies,Escolano, Carmen,Bosch, Joan
experimental part, p. 2175 - 2184 (2011/05/08)
The double cyclocondensation of symmetric pyridyl bis(oxoacids) 2b and 3b with (R)-phenylglycinol stereoselectively gave access to bis-phenylglycinol- derived oxazolopyrrolidine 9 and oxazolopiperidone 10, respectively. Application of the stereocontrolled
Chemoenzymatic and yeast-catalysed synthesis of diastereomeric ethyl γ-phenyl and γ-(n-pyridyl)paraconates
Forzato, Cristina,Furlan, Giada,Nitti, Patrizia,Pitacco, Giuliana,Valentin, Ennio,Zangrando, Ennio,Buzzini, Pietro,Goretti, Marta,Turchetti, Benedetta
, p. 2026 - 2036 (2008/12/23)
The synthesis of γ-phenyl and γ-(n-pyridyl)paraconates was accomplished by chemical reduction of their respective ketodiester precursors followed by cyclisation of the resulting hydroxy diester intermediates. The cis- and trans-lactones thus obtained were separated and separately subjected to enzymatic hydrolysis with HLAP. The cis-lactonic esters had enantiomeric excesses ranging from 94% to 99%, while for the trans-isomers the ee's ranged from 80% to 93%. The same ketodiester precursors were subjected to reduction with a series of yeasts. The absolute configuration of trans-(-)-2-pyridyl paraconic acid was assigned by means of X-ray analysis of its hydrobromide salt, while the absolute configurations of the other lactones were determined via analysis of their respective CD curves.
Studies on non-thiazolidinedione antidiabetic Agents. 2. Novel oxyiminoalkanoic acid derivatives as potent glucose and lipid lowering agents
Imoto, Hiroshi,Sugiyama, Yasuo,Kimura, Hiroyuki,Momose, Yu
, p. 138 - 151 (2007/10/03)
We previously reported that (Z)-2-{4-[(5-methyl-2-phenyl-1,3-oxazol-4-yl) methoxy]benzyloxyimino}-2-(4-phenoxyphenyl)acetic acid (3) showed potent glucose and lipid lowering effects in genetically obese and diabetic mice, KKA y. This compound a
Oxyiminoalkanoic acid derivatives with hypoglycemic and hypolipidemic activity
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, (2008/06/13)
This invention provides a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.
The Stereoselective Synthesis of 2-Alkyl γ-Keto Acid and Heterocyclic Ketomethylene Peptide Isostere Core Units Using Chiral Alkylation by 2-Triflyloxy Esters
Hoffman, Robert V.,Kim, Hwa-Ok
, p. 5107 - 5113 (2007/10/02)
A simple and general protocol for the enentioselective preparation of γ-keto acids and heterocyclic γ-keto acids which have an alkyl group at C-2 is reported.The alkyl group is introduced by chiral alkylation using a scalemic 2-triflyoxy ester.The alkylation takes place with inversion of configuration and is compatible with a variety of alkyl groups.This methodology is thus wellsuited for the preparation of a wide variety of ketomethylene peptide isosteres.
