24589-89-7Relevant articles and documents
Organocatalytic Synthesis of Fused Bicyclic 2,3-Dihydro-1,3,4-oxadiazoles through an Intramolecular Cascade Cyclization
Fugard, Alison J.,Thompson, Bethany K.,Slawin, Alexandra M. Z.,Taylor, James E.,Smith, Andrew D.
, p. 5824 - 5827 (2015/12/11)
Hydrazone-carboxylic acids undergo intramolecular cyclization in the presence of pivaloyl chloride, iPr2NEt, and catalytic DABCO to form a range of substituted fused tricyclic 2,3-dihydro-1,3,4-oxadiazoles in high yields.
Synthesis, characterization and biological screening of some new aryloxyacetic acid analogs
Dahiya, Rajiv,Pathak, Devender,Kaur, Ramninder
experimental part, p. 754 - 758 (2009/12/24)
A novel series of 2-(4-bromo-2-formyl-phenoxy)acetyl amino acid and peptide analogs was synthesized by the coupling of 2-(4-bromo-2-formyl-phenoxy)acetic acid with different amino acid methyl ester hydrochlorides, dipeptide and tripeptide methyl esters using dicyclohexylcarbodiimide as the coupling agent and N-methylmorpholine as the base. Structures of all the newly synthesized compounds were elucidated on basis of IR, NMR and MS spectral data as well as elemental analysis. On pharmacological screening, some peptide derivatives were found to exhibit potent bioac-tivity against gram-negative bacterium Pseudomonas aeruginosa, pathogenic fungus Candida albicans and earthworms Megascoplex konkanensis, Pontoscotex corethruses and Eudrilus sp. Dermatophytes were found to be moderately sensitive towards the newly synthesized analogs. Hydrolyzed peptide derivatives displayed better antimicrobial activity in comparison to corresponding esters.
Synthesis and aldose reductase inhibitory activity of a new series of 5- [[2-(ω-carboxyalkoxy)aryl]methylene]-4-oxo-2-thioxothiazolidine derivatives
Murata, Makoto,Fujitani, Buichi,Mizuta, Hiroyuki
, p. 1061 - 1070 (2007/10/03)
A new series of 5-[[2-(ω-carboxyalkoxy)aryl]methylene]-4-oxo-2- thioxothiazolidine derivatives was synthesized and evaluated for their potency as aldose reductase inhibitors (ARIs). Their activities were examined in terms of their inhibitory effect on rat lens aldose reductase in vitro and in terms of the preventive effect on sorbitol accumulation in the sciatic nerve of streptozotocin (STZ)-induced diabetic rats in vivo. Of these compounds, some of the naphthylmethylene thiazolidine derivatives were comparable to Zenarestat in the inhibitory potency in vitro and in vivo. In particular, compound 30 was 1.5 times more potent than Zenarestat in the in vivo activity, and had an adequate potency for clinical development.