136010-67-8Relevant academic research and scientific papers
α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists
Kim, Ho Shin,Jin, Mi-Kyoung,Kang, Sang-Uk,Lim, Ju-Ok,Tran, Phuong-Thao,Hoang, Van-Hai,Ann, Jihyae,Ha, Tae-Hwan,Pearce, Larry V.,Pavlyukovets, Vladimir A.,Blumberg, Peter M.,Lee, Jeewoo
, p. 2685 - 2688 (2015/02/19)
A series of α-methylated analogues of the potent sRTX thiourea antagonists were investigated as rTRPV1 ligands in order to examine the effect of α-methylation on receptor activity. The SAR analysis indicated that activity was stereospecific with the (R)-configuration of the newly formed chiral center providing high binding affinity and potent antagonism while the configuration of the C-region was not significant.
N-HYDROXYAMIDE DERIVATIVES AND USE THEREOF
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Page/Page column 95, (2008/06/13)
The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
Enantioselective synthesis of α-hydroxylated enterolactone and analogs
Sefkow, Michael,Kelling, Alexandra,Schilde, Uwe
, p. 5101 - 5104 (2007/10/03)
A short and general synthesis of enantiomerically pure α-hydroxylated lactone lignans starting from commercially available iPr malate is presented. Key reactions are two stereoselective alkylations of malic acid derivatives. Some enhancements of the alkylation of malic acid esters and a general extension of the alkylation of dioxolanones is reported. Proof of the stereochemical outcome of the alkylation reactions is provided by X-ray diffraction analysis of α-hydroxy-α,β-dibenzyl-γ-butyrolactone, the first crystal structure of an enantiomerically pure α-hydroxylated lactone lignan.
A stereospecific synthesis of (-)-bestatin from L-malic acid
Norman,Morris
, p. 6803 - 6806 (2007/10/02)
A highly diastereospecific route to (-)-Bestatin from L-Malic Acid has been developed. This approach features a stereocontrolled alkylation of diethyl (S)-malate and proceeds through an oxazolidone via a Curtius Rearrangement.
