57817-08-0Relevant academic research and scientific papers
SUBSTITUTED ALKOXYPYRIDINYL INDOLSULFONAMIDES
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Paragraph 0195-0196, (2020/01/08)
The present application relates to alkoxy-substituted pyridinyl indolsulfonamides. The compounds are negative GPR17 modulators and have utility in the treatment of various GPR17 associated disorders.
HETEROCYCLIC COMPOUNDS AS ANTIBIOTIC POTENTIATORS
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Paragraph 1163, (2016/07/05)
The invention relates to heterocyclic compounds and their use as antibiotics and/or as antibiotic potentiators. The compounds may act as colistin potentiators and SOS inhibitors.
Tandem action of the O2- and FADH2-dependent halogenases KtzQ and KtzR produce 6,7-dichlorotryptophan for kutzneride assembly
Heemstra Jr., John R.,Walsh, Christopher T.
supporting information; experimental part, p. 14024 - 14025 (2009/03/11)
Kutznerides are actinomycete-derived antifungal nonribosomal hexadepsipeptides which are assembled from five unsual nonproteinogenic amino acids and one hydroxy acid. Conserved in all structurally characterized kutznerides is a dichlorinated tricyclic hexahydropyrroloindole postulated to be derived from 6,7-dichlorotryptophan. In this Communication, we identify KtzQ and KtzR as tandem acting FADH2-dependent halogenases that work sequentially on free l-tryptophan to generate 6,7-dichloro-l-tryptophan. Kinetic characterization of these two enzymes has shown that KtzQ (along with the flavinreductase KtzS) acts first to chlorinate at the 7-position of l-tryptophan. KtzR, with a ~120 fold preference for 7-chloro-l-tryptophan over l-tryptophan, then installs the second chlorine at the 6-position of 7-chloro-l-tryptophan to generate 6,7-dichloro-l-tryptophan. These findings provide further insights into the enzymatic logic of carbon-chloride bond formation during the biosynthesis of halogenated secondary metabolites. Copyright
3-ACYLINDOLE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
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Page/Page column 7, (2008/12/08)
The invention relates to compounds of formula (I), wherein X, R1, R2, R3, R4 and R5 are as described herein. The invention also includes preparative methods for the preparation of compounds of formula
4-(Heteroaryl-methyl and substituted heteroaryl-methyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists
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Page/Page column 18, (2010/10/20)
Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.
Novel and selective 5-HT(2C/2B) receptor antagonists as potential anxiolytic agents: Synthesis, quantitative structure - Activity relationships, and molecular modeling of substituted 1-(3- pyridylcarbamoyl)indolines
Bromidge, Steven M.,Dabbs, Steven,Davies, David T.,Duckworth, D. Malcolm,Forbes, Ian T.,Ham, Peter,Jones, Graham E.,King, Frank D.,Saunders, Damian V.,Starr, Susannah,Thewlis, Kevin M.,Wyman, Paul A.,Blaney, Frank E.,Naylor, Christopher B.,Bailey, Fiona,Blackburn, Thomas P.,Holland, Vicky,Kennett, Guy A.,Riley, Graham J.,Wood, Martyn D.
, p. 1598 - 1612 (2007/10/03)
The synthesis, biological activity, and molecular modeling of a novel series of substituted 1-(3-pyridylcarbamoyl)indolines are reported. These compounds are isosteres of the previously published indole urea 1 (SB- 206553) and illustrate the use of aromatic disubstitution as a replacement for fused five-membered rings in the context of 5-HT(2C/2B) receptor antagonists. By targeting a region of space previously identified as sterically allowed at the 5-HT(2C) receptor but disallowed at the 5-HT(2A) receptor, we have identified a number of compounds which are the most potent and selective 5-HT(2C/2B) receptor antagonists yet reported. 46 (SB-221284) was selected on the basis of its overall biological profile for further evaluation as a novel, potential nonsedating anxiolytic agent. A CoMFA analysis of these compounds produced a model with good predictive value and in addition good qualitative agreement with both our 5-HT(2C) receptor model and our proposed binding mode for this class of ligands within that model.
