797756-92-4Relevant academic research and scientific papers
CYCLOBUTANE- AND AZETIDINE-CONTAINING MONO AND SPIROCYCLIC COMPOUNDS AS ALPHA V INTEGRIN INHIBITORS
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Page/Page column 296-298, (2018/05/27)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to αv- containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of av-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
Kinetic resolution of tropic acid ethyl ester and its derivatives by lipase PS
Atuu, Mary Rose,Mahmood, Syed J.,Laib, Frank,Hossain, M. Mahmun
, p. 3091 - 3101 (2007/10/03)
The first kinetic resolution of tropic acid ethyl ester (TAEE) with lipase PS and vinyl acetate as an acylating agent is reported. The resulting (S)-(-)-3-acetoxy tropic acid ethyl ester and (R)-(+)-tropic acid ethyl ester are produced in high yields and in excellent ee (87-94%). The method has been extended to resolve a variety of tropic acid ester derivatives. In addition, an improved method for the preparation of racemic mixtures of tropic acid ethyl ester and its derivatives from 3-hydroxy-2-phenylacrylic acid ethyl ester using NaBH4 in methanol is reported. This procedure is better than the previous ones because it is cleaner, safer and can be worked up easily. An improved method of deacylating the chiral 3-acetoxy tropic acid ethyl ester without any loss of stereochemical integrity using HCl/CH3OH is also reported.
Differential analgesic activity of the enantiomers of atropine derivatives does not correlate with their muscarinic subtype selectivity
Dei,Bartolini,Bellucci,Ghelardini,Gualtieri,Manetti,Romanelli,Scapecchi,Teodori
, p. 595 - 605 (2007/10/03)
The enantiomers of several tropic and p-substituted tropic acid esters related to atropine obtained by esterification under non-racemizing conditions after resolution of the corresponding racemic acids [(+)- and (-)-18, (+)- and (-)-19] are reported. They were tested in vitro on muscarinic subtype receptors and in vivo for their analgesic activity on mice. As in the case of the lead compound, R-(+)-hyoscyamine, these substances show enantioselectivity in analgesic tests, the eutomers being the R-(+) or R-(+)-p-substituted tropic acid derivatives. However, this property, which is a consequence of increased central release of ACh, seems unrelated to muscarinic subtype selectivity insofar as the compounds are unable to discriminate muscarinic subtype receptors. A possible explanation of these results which does not involve subtype selectivity is proposed, based on the recently developed concept of inverse agonism.
