Results 81 to 90 of about 29,358 (323)

2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19 [PDF]

, 2016
We demonstrate a designed scaffold-hop approach to the discovery of 2,8-disubstituted-1,6-naphthyridine- and 4,6-disubstituted-isoquinoline-based dual CDK8/19 ligands.
Blagg, Julian, Burke, Rosemary, Busch, Michael, Clarke, Paul A., Czodrowski, Paul, Eccles, Suzanne A., Esdar, Christina, Honey, Mark A., Mallinger, Aurélie, Musil, Djordje, Poeschke, Oliver, Raynaud, Florence I., Rink, Christian, Rohdich, Felix, Schiemann, Kai, Schneider, Richard, Schwartz, Daniel, Sejberg, Jimmy, Stubbs, Mark, Urbahns, Klaus, Wienke, Dirk, Workman, Paul   +21 more
core   +5 more sources

Exploration of Fluorinated Pyrazolidine‐3,5‐Diones for Positron Emission Tomography Imaging of the P2Y12 Receptor in the Central Nervous System

ChemMedChem, EarlyView.
Fluorinated pyrazolidine‐3,5‐dione derivatives are developed with the aim to find a positron emission tomography (PET) tracer candidate for imaging of the P2Y12 receptor. All compounds show nanomolar affinity. One compound is radiolabeled with 18F and used in PET imaging studies, revealing rapid metabolism and limited brain uptake.
E. Johanna L. Stéen, Anne van der Schatte Olivier, Berend van der Wildt, Pedro Pereira, Khaled Alkayal, Leopoldo J. Gabella Carena, Robert C. Schuit, Mariska Verlaan, Wissam Beaino, Barbara A. Zarzycka, Iwan J. P. de Esch, Albert D. Windhorst   +11 more
wiley   +1 more source

Syntheses, transformations and applications of aminonaphthol derivatives prepared via modified Mannich reactions [PDF]

, 2013
A special alteration is the three-component modi fi ed Mannich reaction (mMR), in which formaldehyde is replaced by an aromatic aldehyde, the secondary amine by ammonia, and the C e H acid by an electron-rich aromatic compound such as 1- or 2 ...
Fülöp, Ferenc, Szatmári, István
core   +1 more source

Cp*Co(III) Catalyzed Site-Selective C-H Activation of Unsymmetrical O-Acyl Oximes: Synthesis of Multisubstituted Isoquinolines from Terminal and Internal Alkynes.

Angewandte Chemie, 2015
The synthesis of isoquinolines by site-selective C-H activation of O-acyl oximes with a Cp*Co(III) catalyst is described. In the presence of this catalyst, the C-H activation of various unsymmetrically substituted O-acyl oximes selectively occurred at ...
Bo Sun, Tatsuhiko Yoshino, M. Kanai, S. Matsunaga   +3 more
semanticscholar   +1 more source

Multistep Reactions Initiated by Amine‐Based Organometallic Methods

European Journal of Organic Chemistry, EarlyView.
The advent of C–H activation and other organometallic methodologies making use of transient directing groups or free amines themselves for the elaboration of amine substrates provides unique access to cascade‐type reactions that can generate significant molecular complexity in one pot. The pursuit of atom‐ and step‐economical pathways to access complex
Victoria D. Ho, Olutayo N. Farinde, Kendra K. Shrestha, Michael C. Young   +3 more
wiley   +1 more source

Screening of antidiabetic and antioxidant potential along with phytochemicals of Annona genus: a review

Future Journal of Pharmaceutical Sciences, 2021
Background Annona species can be found in the subtropical and tropical parts of the world. Because of their medicinal capabilities and highly exotic edible fruits, they are one of the most important members of the Annonaceae family.
Shadman Sakib Chowdhury, Abu Montakim Tareq, Syed Mohammed Tareq, Saifuddin Farhad, Mohammed Abu Sayeed   +4 more
doaj   +1 more source

Halocyclization of o-(Alkynyl)styrenes. Synthesis of 3-Halo-1H-indenes [PDF]

, 2010
Junta de Castilla y Leon (BU021A09 and GR-172), Ministerio de Educacion y Ciencia (MEC), FEDER (CTQ2007-61436/BQU and CTQ2009-09949/BQU), MEC (FPU grant), Juan de la Cierva, Ramon y Cajal and "Young Foreign Researchers" (SB2009-0186 ...
Fernández Rodríguez, Manuel A., García García, Patricia, Martínez Cuezva, Alberto, Rashid, Muhammad A., Rodríguez, Félix, Sanz Díez, Roberto   +5 more
core   +1 more source

Diastereoselectivity in the Synthesis of m‐ and p‐Substituted 3‐Aryl‐2‐trichloromethyl‐1,3‐thiazolidin‐4‐one Sulfoxides With Oxone

Journal of Heterocyclic Chemistry, EarlyView.
Highly selective oxidation of thiazolidin‐4‐ones to sulfoxides and sulfones with Oxone and KMnO4, respectively. ABSTRACT S‐Oxidation of 3‐Aryl‐2‐trichloromethyl‐1,3‐thiazolidin‐4‐ones with Oxone was investigated. For all compounds evaluated, selective oxidation to the sulfoxide versus the sulfone was realized using 3 equivalents of Oxone at room ...
Ahmed Y. Nuriye, Kevin C. Cannon, Anna Sigmon, John Tierney   +3 more
wiley   +1 more source

Inhibitors of the Detoxifying Enzyme of the Phytoalexin Brassinin Based on Quinoline and Isoquinoline Scaffolds

Molecules, 2017
The detoxification of the phytoalexin brassinin to indole-3-carboxaldehyde and S-methyl dithiocarbamate is catalyzed by brassinin oxidase (BOLm), an inducible fungal enzyme produced by the plant pathogen Leptosphaeria maculans.
M. Soledade C. Pedras, Abbas Abdoli, Vijay K. Sarma-Mamillapalle   +2 more
doaj   +1 more source

The Cyclisation of l-Aryl-2-Benzamidoalkan-l-Ols to 4,5-DihydroOxazoles or Isoquinolines [PDF]

, 1990
The cyclisation of several N-benzoyl derivatives of 2-amino-l-phenylpropan-l-ol w~e carried out employing the Pictet-Cams modification ofthe BischlerNapieralski reaction. The formation of4, 5-dihydro-oxazoles orisoquinolines depends on the substituents
Md. Sharif, Atan, O. Fitton, Alan
core