83663-40-5Relevant articles and documents
In vivo phenotypic drug discovery: Applying a behavioral assay to the discovery and optimization of novel antipsychotic agents
Shao, Liming,Campbell, Una C.,Fang, Q. Kevin,Powell, Noel A.,Campbell, John E.,Jones, Philip G.,Hanania, Taleen,Alexandrov, Vadim,Morganstern, Irene,Sabath, Emily,Zhong, Hua M.,Large, Thomas H.,Spear, Kerry L.
, p. 1093 - 1101 (2016/07/06)
Phenotypic drug discovery (PDD) is increasingly being recognized as a viable compliment to target-based drug discovery (TDD). By measuring functional changes, typically at a systems level, PDD can facilitate the identification of compounds having a desirable pharmacology. This capability is particularly important when studying CNS diseases where drug efficacy may require modulation of multiple targets in order to overcome a robust, adaptive biological system. Here, we report the application of a mouse-based high-dimensional behavioral assay to the discovery and optimization of a structurally and mechanistically novel antipsychotic. Lead optimization focused on optimizing complex behavioral features and no explicit effort was made to identify the target (or targets) involved.
HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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, (2013/08/28)
Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
NOVEL PORPHYRAZINE DERIVATIVE AND INTERMEDIATE THEREOF, METHOD FOR PRODUCTION OF NOVEL PORPHYRAZINE DERIVATIVE AND INTERMEDIATE THEREOF, AND USE OF PORPHYRAZINE DERIVATIVE
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Page/Page column 21; 37, (2010/01/07)
A porphyrazine derivative in which porphyrazine forms a condensed ring with thiophene and a skeleton of the thiophene has a functional group such as an alkyl group at position 2 has a high solubility in an organic solvent and exhibits a high crystallinity. Therefore, the porphyrazine derivative is suitably used in crystalline thin-film formation using a solution process. This provides a novel porphyrazine derivative and an intermediate thereof, which porphyrazine derivative has a high solubility in an organic solvent and is excellent in molecular orientation, a method for production of the porphyrazine derivative and the intermediate, and use of the porphyrazine derivative and the intermediate.
Bromothiophene Reactions. II. A Novel Rearrangement in the Zinc and Acetic Acid Reduction
Alvares-Insua, A. S.,Conde, S.,Corral, C.
, p. 713 - 716 (2007/10/02)
The elimination of the α-bromine atoms of the bromothienylethanolamine derivatives 2a, b, c, d with zinc and acetic acid unexpectedly involved a migration of the ethanolamine side chain from the 3 to the 2 position in the thiophene ring.Experiments carried out with simpler analogous compounds 3, 4 and 6 seem to indicate that this rearrangement takes place only in those cases in which the carbon atom of the side chain next to the ring supports an oxygen atom capable of being protonated in the reaction medium.A tentative mechanism is proposed to explain the experimental results.