19361-66-1Relevant academic research and scientific papers
PROCESS FOR PRODUCING OPTICALLY ACTIVE 3-HYDROXYPROPIONIC ESTER DERIVATIVE
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Page/Page column 10-11, (2010/02/13)
The present invention is to provide a process for simply producing an optically active 3-hydroxypropionic ester derivative useful as a medicament intermediate from an inexpensive material. More specifically, the present invention is directed to a process for producing an optically active 3-hydroxypropionic ester derivative comprising reacting an acetic ester derivative available at low cost with a base and a formic ester, thereby converting the acetic ester derivative into a 2-formylacetic ester derivative, and thereafter, stereospecifically reducing the formyl group of the derivative by use of an enzymatic source capable of stereoselectively reducing the formyl group of the derivative.
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: Modification of the methylene spacer and the P1′ side chain
Davies, Stephen J.,Ayscough, Andrew P.,Beckett, R. Paul,Bragg, Ryan A.,Clements, John M.,Doel, Sheila,Grew, Christine,Launchbury, Steven B.,Perkins, Gemma M.,Pratt, Lisa M.,Smith, Helen K.,Spavold, Zoe M.,Thomas, S. Wayne,Todd, Richard S.,Whittaker, Mark
, p. 2709 - 2713 (2007/10/03)
Structural modifications to the peptide deformylase inhibitor BB-3497 are described. In this paper, we describe the initial SAR around this lead for modifications to the methylene spacer and the P1′ side chain. Enzyme inhibition and antibacterial activity data revealed that the optimum distance between the N-formyl hydroxylamine metal binding group and the P1′ side chain is one unsubstituted methylene unit. Additionally, lipophilic P1′ side chains that closely mimic the methionine residue in the substrate provided compounds with the best microbiological profile.
Guanidinothiazoles with H2-antihistaminic activity. 12: H2-antihistamines
Trumm,Schunack
, p. 188 - 190 (2007/10/02)
In studies on H2-antihistaminics, guanidinothiazoles were prepared and tested for their H2-antihistaminic activity on the isolated guinea-pig atrium. Whereas the N,N'-disubstituted cyanoguanidines 3 and 5 possess stronger H2-activity than tiotidine, the 5
