- Indole-like derivatives and application thereof
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The invention relates to indole-like derivatives and application thereof. The compounds have a structure as shown in a formula I. The compounds have ROR [gamma] t regulating activity and are expected to be used for preparing medicines for preventing and treating diseases related to ROR [gamma] t.
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- Influences of Histidine-1 and Azaphenylalanine-4 on the Affinity, Anti-inflammatory, and Antiangiogenic Activities of Azapeptide Cluster of Differentiation 36 Receptor Modulators
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Azapeptide analogues of growth hormone releasing peptide-6 (GHRP-6) exhibit promising affinity, selectivity, and modulator activity on the cluster of differentiation 36 receptor (CD36). For example, [A1, azaF4]- and [azaY4
- Chignen Possi, Kelvine,Mulumba, Mukandila,Omri, Samy,Garcia-Ramos, Yesica,Tahiri, Houda,Chemtob, Sylvain,Ong, Huy,Lubell, William D.
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supporting information
p. 9263 - 9274
(2017/11/30)
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- Ligand Specific Efficiency (LSE) Index for PET Tracer Optimization
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Ligand efficiency indices are widely used to guide chemical optimization in drug discovery, due to their predictive value in the early steps of optimization. At later stages, however, as more complex properties become critical for success, indices relying on calculated, rather than experimental, parameters become less informative. This problem is particularly acute when developing positron emission tomography (PET) imaging agents, for which nonspecific binding (NSB) to membranes and non-target proteins is a frequent cause of failure. NSB cannot be predicted using in silico parameters. To address this gap, we explored the use of the experimentally determined chromatographic hydrophobicity index on immobilized artificial membranes, CHI(IAM), to guide the optimization of NSB. The ligand specific efficiency (LSE) index was defined as the ratio between affinity (pIC50or pKd) and the logarithmic value of CHI(IAM). It allows for quantification of binding affinity to the target of interest, relative to NSB. Its use was illustrated by the optimization of PET tracer candidates for the prostacyclin receptor.
- Auberson, Yves P.,Briard, Emmanuelle,Sykes, David,Reilly, John,Healy, Mark
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p. 1415 - 1427
(2016/07/16)
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- Synthesis and antirhinovirus activity of 6-(dimethylamino)-2-(trifluoromethyl)-9-(substituted benzyl)-9H-purines
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A series of 6-(dimethylamino)-2-(trifluoromethyl)-9-(substituted benzyl)purines was synthesized and tested for antirhinovirus activity. Most of the compounds were synthesized by alkylation of 6-chloro-2-(trifluoromethyl)-9H-purine with the appropriate benzyl halide followed by displacement of the chloro group with dimethylamine. Alternatively, 6-(dimethylamino)-2-(trifluoromethyl)purine was alkylated with the appropriate benzyl halide. Although several different aryl substituents provided compounds with IC50's = 0.03 μM against rhinovirus serotype 1B, no congener was significantly more active than the parent 2. Twenty-three compounds were tested against 18 other serotypes, but none exhibited a uniform profile of activity.
- Kelley,Linn,Selway
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p. 1757 - 1763
(2007/10/02)
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