53484-49-4Relevant academic research and scientific papers
SERINE/THREONINE KINASE INHIBITORS
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Paragraph 00398, (2015/07/16)
Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such diseases, or associated pathological conditions are disclosed.
Biocatalytic racemization of aliphatic, arylaliphatic, and aromatic α-hydroxycarboxylic acids
Glueck, Silvia M.,Pirker, Monika,Nestl, Bettina M.,Ueberbacher, Barbara T.,Larissegger-Schnell, Barbara,Csar, Katrin,Hauer, Bernhard,Stuermer, Rainer,Kroutil, Wolfgang,Faber, Kurt
, p. 4028 - 4032 (2007/10/03)
Biocatalytic racemization of a range of aliphatic, (aryl)aliphatic, and aromatic α-hydroxycarboxylic acids was accomplished by using whole resting cells of a range of Lactobacillus spp. The mild (physiological) reaction conditions ensured an essentially "clean" isomerization in the absence of side reactions, such as elimination or decomposition. Whereas straight-chain aliphatic 2-hydroxy-carboxylic acids were racemized with excellent rates (up to 85% relative to lactate), steric hindrance was observed for branched-chain analogues. Good rates were observed for aryl-alkyl derivatives, such as 3-phenyllactic acid (up to 59%) and 4-phenyl-2-hydroxybutanoic acid (up to 47%). In addition, also mandelate and its o-chloro analogue were accepted at a fair rate (45%). This biocatalytic racemization represents an important tool for the deracemization of a number of pharmaceutically important building blocks.
Fluorinated tropane alkaloids generated by directed biosynthesis in transformed root cultures of Datura stramonium
O'Hagan, David,Robins, Richard J.,Wilson, Marina,Wong, Chi W.,Berry, Marc,Zabetakis, Ioannis
, p. 2117 - 2120 (2007/10/03)
2′-, 3′- and 4′-Fluorophenyl-(RS)-lactic acids were administered to transformed root cultures of Datura stramonium to determine their abilities as substrates for incorporation into the phenyllactoyl and tropoyl ester moieties of the tropane alkaloids, littorine and hyoscyamine respectively. In the event, all of the fluorinated phenyllactates generated the corresponding fluorinated littorine and hyoscyamine analogues. The efficiency of conversion for the isomerisation of the fluorinated littorines (F-lit) to fluorinated hyoscyamines was 3′-F-lit > 4′-F-lit ? 2′-F-lit.
AMINO ACID DERIVATIVE
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, (2008/06/13)
The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity.This amino acid derivative is represented by the following general formula (I): STR1 wherein R 1 represents a hydrogen atom or an acyl group; R 2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;m and n represent each independently an integer of 0, 1 or 2 and J represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.
