762292-63-7Relevant academic research and scientific papers
Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17)
Blass, Benjamin E.,Iyer, Pravin,Abou-Gharbia, Magid,Childers, Wayne E.,Gordon, John C.,Ramanjulu, Mercy,Morton, George,Arumugam, Premkumar,Boruwa, Joshodeep,Ellingboe, John,Mitra, Sayan,Reddy Nimmareddy, Rajashekar,Paliwal, Shalini,Rajasekhar, Jamallamudi,Shivakumar, Savithiri,Srivastava, Pratima,Tangirala, Raghuram S.,Venkataramanaiah, Konda,Bobbala, Ramreddy,Yanamandra, Mahesh,Krishnakanth Reddy
supporting information, p. 2270 - 2274 (2018/05/28)
The synthesis of steroid hormones is critical to human physiology and improper regulation of either the synthesis of these key molecules or activation of the associated receptors can lead to disease states. This has led to intense interest in developing c
Design, synthesis and structure–activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands
Szymańska, Ewa,Cha?upnik, Paulina,Szczepańska, Katarzyna,Cu?ado Moral, Ana Maria,Pickering, Darryl S.,Nielsen, Birgitte,Johansen, Tommy N.,Kie?-Kononowicz, Katarzyna
, p. 5568 - 5572 (2016/11/09)
A new series of carboxyaryl-substituted phenylalanines was designed, synthesized and pharmacologically characterized in vitro at native rat ionotropic glutamate receptors as well as at cloned homomeric kainate receptors GluK1–GluK3. Among them, six compounds bound to GluK1 receptor subtypes with reasonable affinity (Kivalues in the range of 4.9–7.5?μM). A structure–activity relationship (SAR) for the obtained series, focused mainly on the pharmacological effect of structural modifications in the 4- and 5-position of the phenylalanine ring, was established. To illustrate the results, molecular docking of the synthesized series to the X-ray structure of GluK1 ligand binding core was performed. The influence of individual substituents at the phenylalanine ring for both the affinity and selectivity at AMPA, GluK1 and GluK3 receptors was analyzed, giving directions for future studies.
NOVEL CYTOCHROME P450 INHIBITORS AND THEIR METHOD OF USE
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Paragraph 0390; 0391, (2016/10/08)
Embodiments of the present invention relate to novel cytochrome P450 inhibitors and pharmaceutical compositions thereof having a disease-modifying action in the treatment of diseases associated with the production of cortisol that include metabolic syndro
Substituted Heterocyclic Ethers and Their Use in CNS Disorders
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Page/Page column 27, (2009/05/28)
The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
PPAR ACTIVE COMPOUNDS
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Page/Page column 66; 67, (2008/12/08)
Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ.
Aminoacetamide acyl guanidines as beta-secretase inhibitors
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Page/Page column 18-19, (2008/06/13)
There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R25, R26 and R27 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
