68216-65-9Relevant academic research and scientific papers
Synthesis and Evaluation of Novel 7- and 8-Aminophenoxazinones for the Detection of β-Alanine Aminopeptidase Activity and the Reliable Identification of Pseudomonas aeruginosa in Clinical Samples
Bedernjak, Alexandre F.,Zaytsev, Andrey V.,Babolat, Michèle,Cellier, Marie,James, Arthur L.,Orenga, Sylvain,Perry, John D.,Groundwater, Paul W.,Anderson, Rosaleen J.
, p. 4476 - 4487 (2016/06/13)
A series of novel 8-aminophenoxazin-3-one and 7-aminophenoxazin-3-one chromogens and their corresponding β-alanine derivatives were synthesized and evaluated for their ability to detect β-alanyl aminopeptidase activity in bacteria known to hydrolyze β-ala
PHARMACEUTICAL COMPOSITIONS AND METHODS OF PREVENTING, TREATING, OR INHIBITING INFLAMMATORY DISEASES, DISORDERS, OR CONDITIONS OF THE SKIN, AND DISEASES, DISORDERS, OR CONDITIONS ASSOCIATED WITH COLLAGEN DEPLETION
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, (2009/01/23)
The present invention provides compositions and methods for preventing, treating, or inhibiting inflammatory diseases, disorders, or conditions of the skin, and diseases, disorders, or conditions associated with collagen depletion using one or more estrogenic agents.
NOVEL ESTROGEN RECEPTOR LIGANDS
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Page/Page column 31, (2009/11/29)
The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt: wherein R3 is selected from the group consisting of ORA; -CHO; -C(O)C1-4alkyl; -C(O)phenyl; -O-C(O)RA; and N(RB)2; R6 is selected from certain cyclic groups defined in the specification; and the remaining groups are defined in the specification; together with a pharmaceutically acceptable carrier. Most of the compounds are novel. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
Tetracyclic compounds as estrogen ligands
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Page/Page column 15; 21, (2010/02/15)
This invention provides estrogen receptor modulators having the structure: wherein R1, R2, R3, R4, Q, n, R8, R9, R10, and R11 have been defined in the specification; o
A Convergent Synthesis of the Macrocyclic Core of Cytotrienins: Application of RCM for Macrocyclization
Evano, Gwilherm,Schaus, Jennifer V.,Panek, James S.
, p. 525 - 528 (2007/10/03)
(Equation presented) The asymmetric synthesis of the fully elaborated macrocyclic core of cytotrienins A-D, potent apoptosis-inducing agents, is described. Synthetic highlights include the construction of the aniline bond using a copper-mediated amidation and the use of a ring-closing metathesis (RCM) reaction to efficiently install the (E,E,E)-triene and simultaneously construct the macrocyclic lactam.
Substituted 2-phenyl benzofurans as estrogenic agents
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, (2008/06/13)
This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.
1,2,3,4-Tetrahydroisoquinoline analogs of phenylalkylamine stimulants and hallucinogens
Malmusi, Luca,Dukat, Malgorzata,Young, Richard,Teitler, Milt,Darmani, Nissar A.,Ahmad, Bashir,Smith, Carol,Glennon, Richard A.
, p. 400 - 411 (2007/10/03)
Conformationally constrained, 1,2,3,4-tetrahydroisoquinoline (TIQ) analogs of central stimulant (e.g. amphetamine) and hallucinogenic (e.g. DOM) phenylalkylamines were prepared and evaluated to determine the contribution to activity of this conformational
Serotonin receptor affinities of psychoactive phenalkylamine analogues
Glennon,Liebowitz,Anderson III
, p. 294 - 299 (2007/10/02)
Employing a rat fundus model, the serotonin (5-HT) receptor affinities of 45 phenalkylamine analogues were determined. Phenethylamine and phenylisopropylamine possess relatively low receptor affinities; in general, mono-, di-, and trimethoxylation enhance affinity. Of the disubstituted compounds, methoxyl groups at the 2 and 5 positions are optimal for imparting a high affinity. 4-Methylation, 4-ethylation and 4-bromination also enhance receptor affinity, while N,N-dimethylation of the terminal amine decreases affinity. α-Methylation of phenethylamines has little effect on affinity when racemates are examined. Introduction of a benzylic keto group can either increase or decrease affinity, depending upon the presence of other aromatic substituents. The most behaviorally active compounds were found to possess the highest 5-HT receptor affinities, while less active compounds were found to possess lower affinities.
