6109-54-2Relevant academic research and scientific papers
Modifications at C(5) of 2-(2-Pyrrolidinyl)-Substituted 1,4-Benzodioxane Elicit Potent α4β2 Nicotinic Acetylcholine Receptor Partial Agonism with High Selectivity over the α3β4 Subtype
Bavo, Francesco,Pallavicini, Marco,Gotti, Cecilia,Appiani, Rebecca,Moretti, Milena,Colombo, Sara Francesca,Pucci, Susanna,Viani, Paola,Budriesi, Roberta,Renzi, Massimiliano,Fucile, Sergio,Bolchi, Cristiano
, p. 15668 - 15692 (2021/01/09)
A series of diastereomeric 2-(2-pyrrolidinyl)-1,4-benzodioxanes bearing a small, hydrogen-bonding substituent at the 7-, 6-, or 5-position of benzodioxane have been studied for α4β2 and α3β4 nicotinic acetylcholine receptor affinity and activity. Analogous to C(5)H replacement with N and to a much greater extent than decoration at C(7), substitution at benzodioxane C(5) confers very high α4β2/α3β4 selectivity to the α4β2 partial agonism. Docking into the two receptor structures recently determined by cryo-electron microscopy and site-directed mutagenesis at the minus β2 side converge in indicating that the limited accommodation capacity of the β2 pocket, compared to that of the β4 pocket, makes substitution at C(5) rather than at more projecting C(7) position determinant for this pursued subtype selectivity.
Novel Cyclic Phenoxy Compounds and Improved Treatments for Cardiac and Cardiovascular Disease
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Paragraph 0198; 0199; 0200, (2015/02/25)
A compound of formula I, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein either Q1, CR6a and optionally R6b together form a cyclic moiety wh
6-Substituted 1,2-benzoxathiine-2,2-dioxides are isoform-selective inhibitors of human carbonic anhydrases IX, XII and VA
Tanc, Muhammet,Carta, Fabrizio,Scozzafava, Andrea,Supuran, Claudiu T.
supporting information, p. 77 - 80 (2015/01/09)
A series of 6-substituted 2-benzoxathiine-2,2-dioxides were synthesized starting from 2,5-dihydroxybenzaldehyde, and then screened in vitro for their inhibition properties against five human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms. All the compounds
NOVEL CYCLIC PHENOXY COMPOUNDS AND IMPROVED TREATMENTS FOR CARDIAC AND CARDIOVASCULAR DISEASE
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Page/Page column 25, (2013/08/28)
A compound of formula I, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: (Formula (I)) wherein either Q1, CR6a and optionally R6b together form a cy
SAR studies of epoxycurcuphenol derivatives on leukemia CT-CD4 cells
Galindo, José L.G.,Macías, Mariola,Molinillo, José M.G.,Mu?oz-Suano, Alba,Torres, Ascensión,Varela, Rosa M.,García-Cozar, Francisco,Macías, Francisco A.
supporting information, p. 6662 - 6668 (2013/01/15)
Bioactive natural products are a potential source of new pharmaceuticals since they offer new modes of action and more specific activities. The use of derivatization also enables the optimal structure for their biological activity to be determined. In thi
Design, synthesis and SAR study of hydroxychalcone inhibitors of human β-secretase (BACE1)
Ma, Lei,Yang, Zhengyi,Li, Chenjing,Zhu, Zhiyuan,Shen, Xu,Hu, Lihong
experimental part, p. 643 - 648 (2012/04/10)
According to the structural characteristics of isoliquiritigenin from Glycyrrhiza uralensis, a series of hydroxychalcones has been designed, synthesized and evaluated for their in vitro inhibitory activities of β-secretase (BACE1). Structure-activity relationship study suggested that inhibitory activity against BACE1 was governed to a greater extent by the hydroxyl substituent on A-and B-ring of the chalcone, and the most active compound was substituted with four hydroxyl group (17, IC50=0.27 μM).
Active core structure of terfestatin A, a new specific inhibitor of auxin signaling
Hayashi, Ken-ichiro,Yamazoe, Atsushi,Ishibashi, Yuki,Kusaka, Naoyuki,Oono, Yutaka,Nozaki, Hiroshi
, p. 5331 - 5344 (2008/12/20)
The auxins, plant hormones, regulate many aspects of the growth and development of plants. Terfestatin A (TrfA), a novel auxin signaling inhibitor, was identified in a screen of Streptomyces sp. F40 extracts for inhibition of the expression of an auxin-in
ANTIFUNGAL AGENT CONTAINING PYRIDINE DERIVATIVE
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Page/Page column 39-40, (2008/06/13)
The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): (wherein X represents an oxygen atom, a sulfur atom or -NH-, R1 represents a hydrogen atom, a halogen atom, a cyano group, an amino group or a substituent, and R2 and R3 independently represent a hydrogen atom, a halogen atom, a hydroxyl group or a substituent, except for a case in which R2 and R3 are both hydrogen atoms), and an antifungal agent containing the above compound.
SMALL MOLECULE ANTAGONISTS OF XIAP FAMILY PROTEINS
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Page/Page column 96; sheet 12, (2010/02/14)
The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as ant
Synthesis, anticancer activity, and inhibition of tubulin polymerization by conformationally restricted analogues of lavendustin A
Mu, Fanrong,Hamel, Ernest,Lee, Debbie J.,Pryor, Donald E.,Cushman, Mark
, p. 1670 - 1682 (2007/10/03)
Compounds in the lavendustin A series have been shown to inhibit both protein-tyrosine kinases (PTKs) and tubulin polymerization. Since certain lavendustin A derivatives can exist in conformations that resemble both the trans-stilbene structure of the PTK
