40547-58-8Relevant academic research and scientific papers
Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation
Hu, Yun,Yang, Yaqi,Yu, Yanjun,Wen, Gesi,Shang, Nana,Zhuang, Wei,Lu, Dihan,Zhou, Binhua,Liang, Baoxia,Yue, Xin,Li, Feng,Du, Jun,Bu, Xianzhang
, p. 6033 - 6053 (2013/09/02)
Alzheimer's disease (AD) is associated with impaired Aβ degradation in the brain. Enhancing the process of Aβ clearance is an attractive potential AD therapy. Treatment with LXR agonists may reduce Aβ levels in vivo. However, the clinical potential of man
Structurally simple inhibitors of lanosterol 14α-demethylase are efficacious in a rodent model of acute Chagas disease
Suryadevara, Praveen Kumar,Olepu, Srinivas,Lockman, Jeffrey W.,Ohkanda, Junko,Karimi, Mandana,Verlinde, Christophe L. M. J.,Kraus, James M.,Schoepe, Jan,Van Voorhis, Wesley C.,Hamilton, Andrew D.,Buckner, Frederick S.,Gelb, Michael H.
experimental part, p. 3703 - 3715 (2010/04/24)
We report structure-activity studies of a large number of dialkyl imidazoles as inhibitors of Trypanosoma cruzi lanosterol-14α-demethylase (L14DM). The compounds have a simple structure compared to posaconazole, another L14DM inhibitor that is an anti-Chagas drug candidate. Several compounds display potency for killing T. cruzi amastigotes in vitro with values of EC 50 in the 0.4-10 nM range. Two compounds were selected for efficacy studies in a mouse model of acute Chagas disease. At oral doses of 20-50 mg/kg given after establishment of parasite infection, the compounds reduced parasitemia in the blood to undetectable levels, and analysis of remaining parasites by PCR revealed a lack of parasites in the majority of animals. These dialkyl imidazoles are substantially less expensive to produce than posaconazole and are appropriate for further development toward an anti-Chagas disease clinical candidate.
ANTIBACTERIAL AGENTS
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Page/Page column 17, (2008/06/13)
The present invention provides a compound of Formula (I) Or a pharmaceutically acceptable salt thereof wherein: W is CH2NHC(=Z)R1, C(=Z)NHR2, or CH2het; X is H, C1-6alkyl, or C2-6alkenyl; Y is H, or F; Z is O, or S; R1 is C1-6alkyl, NHC1-6alkyl, C3-7cycloalkyl, C2-6alkenyl, or OC1-4alkyl; R2 is H, C1-4alkyl, or -OC1-4alkyl; and het is a five-(5) or six-(6) membered heterocyclic ring having 1-4 heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen within the ring, wherein each carbon atom in het is optionally substituted with C1-4alkyl, C2-4alkenyl, C2-4alkynyl, halo, OR3, CN, NO2, NHR3R3, oxo, CF3, OCF3, C(=O)C1-4alkyl, OC(=O)C1-4alkyl, or C(=O)OR3; wherein R3 is H, or C1-4alkyl.
N-sulfamoyl-N'-benzopyranpiperidine compounds and uses thereof
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Page/Page column 8, (2008/06/13)
N-sulfamoyl-N′-benzopyranpiperidine compounds of formula I and their physiologically acceptable acid addition salts, pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and related concomitant and/or secondary diseases or conditions.
N-SULFAMOYL-N’-BENZOPYRANPIPERIDINES AS INHBITORS OF CARBONIC ANHYDRASES
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Page/Page column 15-16, (2008/06/13)
The present invention relates to novel N-sulfamoyl-N'-benzopyranpiperidines of general formula (I) and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the prophylaxis and/or treatment and/or prevention and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and its concomitant and/or secondary diseases or conditions.
QSAR studies of paeonol analogues for inhibition of platelet aggregation
Doble, Mukesh,Karthikeyan,Padmaswar,Akamanchi
, p. 5996 - 6001 (2007/10/03)
Various paeonol analogues were synthesized and tested in vitro as inhibitors of platelet aggregation. Structural properties (or descriptors) of paeonol analogues were calculated and the structure-activity relationships were determined. Several multiple linear and nonlinear regression models and back-propagation neural network model were tested and the latter using relative positive charge, hydration energy, and hydrophilic factor as inputs gave the best data fitting with R2 = 0.89 and qpre2=0.66. The correlation coefficient between antiplatelet inhibition activity with an interaction energy between the paeonol compounds with COX-1 enzyme is only 0.39.
PYRAZOLE COMPOUNDS
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Page 44-45, (2008/06/13)
Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as cancers. In the formulae, Ar is an aryl, aryl(C1-C6 alkyl), aryl(C1-C6 alkyl), heteroaryl, heteroarylaryl(C1-C6 alkyl), or heteroarylaryl(C1-C6 alkyl) group, any of which being optionally substituted in the aryl or heteroaryl part thereof; R1, is hydrogen or optionally substituted Cl-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or Cl-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and ring A is a non aromatic carbocyclic or heterocyclic ring wherein (i) a ring carbon is optionally substituted, and/or (ii) a ring nitrogen is optionally substituted by a group of formula -(Alk1)p (Cyc)n-(Alk3)m-(Z)r (Alk2)s Q where Alk1, Alk2 and Alk3 are optionally substituted C1-C3 alkyl, Cyc is an optionally substituted carbocyclic or heterocyclic radical; m, n, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=O)-, -S02-, -C(=O)O-, -OC(=O)-, -NW-, -C(=O)NRA-, -NRAC(=O)-, -SO2NRA- , or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical.
Synthesis and in-vitro evaluation of platelet aggregation inhibitory activity of paeonol and its analogues
Akamanchi,Padmawar,Thatte,Rege,Dahanukar
, p. 323 - 329 (2007/10/03)
Paeonol (1-(2-hydroxy-4-methoxyphenyl)ethanone) and a series of substituted 1-(2-hydroxyphenyl)ethanone derivatives were synthesized and screened as inhibitors of platelet aggregation. The compounds with the greatest anti-platelet potential among the series tested were 1-(2,5-dihydroxyphenyl)ethanone (65.36% inhibition at 300 μM against 5 μM ADP), paeonol(36.31%), 1-(2-hydroxy-5-methoxyphenyl)ethanone (24.47%), 1-(2-hydroxy-5-nitrophenyl) ethanone (30.40%) and 1-(5-chloro-2-hydroxy-4-methylphenyl)ethanone (24.43%).
4-oxospiro[benzopyran-2,4'-piperidines] as selective α(1a)-adrenergic receptor antagonists
Nerenberg, Jennie B.,Erb, Jill M.,Bergman, Jeffrey M.,O'Malley, Stacey,Chang, Raymond S. L.,Scott, Ann L.,Broten, Theodore P.,Bock, Mark G.
, p. 291 - 294 (2007/10/03)
The 4-oxospiro[benzopyran-2,4'-piperidine] ring system is contained within potent class III antiarrhythmic agents. We highlight how these agents can be chemically transformed into a new class of potent (25-fold) α(1a)-receptor subtype adrenergic antagonists.
Amino-benzofuryl-and thienyl-derivatives
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, (2008/06/13)
6-Amino-benzofuryl- and thienyl-derivatives can be prepared by reacting appropriate amino-substituted benzoyl phenols with appropriate substituted acetophenones and subsequent modification of the substituents. The compounds are useful for the treatment of
