Results 41 to 50 of about 23,799 (225)

Accelerating Primary Screening of USP8 Inhibitors from Drug Repurposing Databases with Tree‐Based Machine Learning

Advanced Intelligent Discovery, EarlyView.
This study introduces a tree‐based machine learning approach to accelerate USP8 inhibitor discovery. The best‐performing model identified 100 high‐confidence repurposable compounds, half already approved or in clinical trials, and uncovered novel scaffolds not previously studied. These findings offer a solid foundation for rapid experimental follow‐up,
Yik Kwong Ng, Sharon Ai Er Lam, Wei Chun Lim, Hannah Hui Min Toh, Shi Jun Ang   +4 more
wiley   +1 more source

Synthesis of new pyrrolidine-based organocatalysts and study of their use in the asymmetric Michael addition of aldehydes to nitroolefins

Beilstein Journal of Organic Chemistry, 2017
New pyrrolidine-based organocatalysts with a bulky substituent at C2 were synthesized from chiral imines derived from (R)-glyceraldehyde acetonide by diastereoselective allylation followed by a sequential hydrozirconation/iodination reaction.
Alejandro Castán, Ramón Badorrey, José A. Gálvez, María D. Díaz-de-Villegas   +3 more
doaj   +1 more source

Synthesis and biological evaluation of nojirimycin- and pyrrolidine-based trehalase inhibitors

Beilstein Journal of Organic Chemistry, 2012
A small set of nojirimycin- and pyrrolidine-based iminosugar derivatives has been synthesized and evaluated as potential inhibitors of porcine and insect trehalases.
Davide Bini, Francesca Cardona, Matilde Forcella, Camilla Parmeggiani, Paolo Parenti, Francesco Nicotra, Laura Cipolla   +6 more
doaj   +1 more source

Rh(II)/Pd(0) Dual Catalysis: Carbenoid N-H Insertion/Allylation Cascade Reaction to Construct Highly Functionalized and Polysubstituted Pyrrolidines

Molecules
In the category of drugs approved by the U.S. FDA, pyrrolidine is the most frequently used core of five-membered nonaromatic heterocycles containing nitrogen.
Maocheng Tang, Xianyan Jiao, Deping He, Ji-Xing Zhao, Ping Liu, Chun-Tian Li   +5 more
doaj   +1 more source

A Straightforward Route to Enantiopure Pyrrolizidines and Indolizidines by Cycloaddition to Pyrroline N-Oxides Derived from the Chiral Pool

Molecules, 1998
Enantiomerically pure, five membered cyclic nitrones, easily obtained in large amounts from protected hydroxyacids and aminoacids such as D- and L-tartaric, L-malic, and L-aspartic acids, give cycloaddition reactions with a good diastereocontrol.
Alberto Brandi, Valentina Fedi, Franca M. Cordero, Stefano Cicchi, Andrea Goti   +4 more
doaj   +1 more source

Convenient access to pyrrolidin-3-ylphosphonic acids and tetrahydro-2H-pyran-3-ylphosphonates with multiple contiguous stereocenters from nonracemic adducts of a Ni(II)-catalyzed Michael reaction

Beilstein Journal of Organic Chemistry, 2020
A new synthetic strategy toward nonracemic phosphoryl-substituted pyrrolidines and tetrahydropyranes with three and five contiguous stereocenters is presented.
Alexander N. Reznikov, Dmitry S. Nikerov, Anastasiya E. Sibiryakova, Victor B. Rybakov, Evgeniy V. Golovin, Yuri N. Klimochkin   +5 more
doaj   +1 more source

ELECTROCHEMICAL REDUCTION OF 2,2,5,5-TETRAMETHYLPYRROLINE DERIVATIVES TO CORRESPONDING PYRROLIDINES

Advanced Engineering Research, 2012
The reduction technique of 2,2,5,5-tetramethylpyrroline compounds to pyrrolidines on sodium amalgam preformed under the electrolysis of sodium hydroxide solution is described.
Irina Y. Zhukova, Igor S. Kashparov, Darya S. Garbuznyak   +2 more
doaj  

Skeletal contraction: A novel strategy to access multisubstituted cyclobutane

Green Synthesis and Catalysis, 2022
The polysubstituted and spirocyclic cyclobutanes were efficiently constructed by the utilization of a novel skeletal contraction strategy which only took one-step synthesis from the readily accessible pyrrolidines.
Chunfa Xu, V.U. Bhaskara Rao, Fen-Er Chen   +2 more
doaj   +1 more source

ELECTROCHEMICAL REDUCTION OF 2,2,5,5-TETRAMETHYLPYRROLINE DERIVATIVES TO CORRESPONDING PYRROLIDINES

Вестник Донского государственного технического университета, 2018
The reduction technique of 2,2,5,5-tetramethylpyrroline compounds to pyrrolidines on sodium amalgam preformed under the electrolysis of sodium hydroxide solution is described.
Irina Y. Zhukova, Igor S. Kashparov, Darya S. Garbuznyak   +2 more
doaj  

Carbohydrate-auxiliary assisted preparation of enantiopure 1,2-oxazine derivatives and aminopolyols

Beilstein Journal of Organic Chemistry, 2012
An approach to enantiopure hydroxylated 2H-1,2-oxazine derivatives is presented utilizing the [3 + 3] cyclisation of lithiated alkoxyallenes and an L-erythrose-derived N-glycosyl nitrone as precursors.
Marcin Jasiński, Dieter Lentz, Hans-Ulrich Reissig   +2 more
doaj   +1 more source