60658-04-0Relevant articles and documents
Reshaping the active pocket of esterase Est816 for resolution of economically important racemates
Fan, Xinjiong,Fu, Yao,Liu, Xiaolong,Zhao, Meng
, p. 6126 - 6133 (2021/09/28)
Bacterial esterases are potential biocatalysts for the production of optically pure compounds. However, the substrate promiscuity and chiral selectivity of esterases usually have a negative correlation, which limits their commercial value. Herein, an efficient and versatile esterase (Est816) was identified as a promising catalyst for the hydrolysis of a wide range of economically important substrates with low enantioselectivity. We rationally designed several variants with up to 11-fold increased catalytic efficiency towards ethyl 2-arylpropionates, mostly retaining the initial substrate scope and enantioselectivity. These variants provided a dramatic increase in efficiency for biocatalytic applications. Based on the best variant Est816-M1, several variants with higher or inverted enantioselectivity were designed through careful analysis of the structural information and molecular docking. Two stereoselectively complementary mutants, Est816-M3 and Est816-M4, successfully overcame and even reversed the low enantioselectivity, and several 2-arylpropionic acid derivatives with highEvalues were obtained. Our results offer potential industrial biocatalysts for the preparation of structurally diverse chiral carboxylic acids and further lay the foundation for improving the catalytic efficiency and enantioselectivity of esterases.
Fabrication of organogels achieved by prodrug-based organogelators of ketoprofen
Mahire, Rahul R.,Agrawal, Deepika S.,Patil, Devanand K.,More, Dhananjay H.
, p. 33286 - 33291 (2014/08/18)
The treatment strategy of curing diseases using prodrugs of an anti-inflammatory drug is widespread. In the present study, we report on the synthesis of prodrugs of ketoprofen, consisting of a derivatization of ketoprofen and long hydrocarbon chain of fat
A NEW METHOD OF SYNTHESIS OF α-ARYLPROPIONIC ACIDS INVOLVING COPPER(I) HOMOGENEOUS CATALYSIS
Ugo, Renato,Nardi, Paola,Psaro, Rinaldo,Roberto, Dominique
, p. 511 - 514 (2007/10/02)
The synthesis of α-arylpropionic acids involving, as first step, the facile coupling af an aryl bromide and diethyl malonate in the presence of Cu(I) bromide is described.The limits of application are discussed.
