- Pharmacophore elucidation of phosphoiodyn A - Potent and selective peroxisome proliferator-activated receptor β/δ agonists with neuroprotective activity
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We report the pharmacophore of the peroxisome proliferator-activated receptor δ (PPARδ) agonist natural product phosphoiodyn A is the phosphonate core. Synthesis of simplified phosphonate esters 13 and 15 provide structurally novel, highly selective and potent PPARδ agonists (EC50 = 78 and 112 nM, respectively). Further, both compounds demonstrate significant neuroprotective activity in an in vitro cellular model indicating that phosphonates may be an effective novel scaffold for the design of therapeutics for the treatment of neurodegenerative disorders.
- Kinarivala, Nihar,Suh, Ji Ho,Botros, Mina,Webb, Paul,Trippier, Paul C.
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- 5-HT3 receptor modulator containing heterocyclic nitrogen as well as preparation method and application thereof
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The invention provides a 5-HT3 receptor modulator containing heterocyclic nitrogen as well as a preparation method and application thereof, belonging to the field of medicinal chemistry. The 5-HT3 receptor modulator containing heterocyclic nitrogen is a c
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- COMPOUND WITH BRANCHING ALKYL CHAINS, METHOD FOR PREPARING THE SAME, AND USE THEREOF IN PHOTOELECTRIC DEVICE
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The invention discloses a compound having branching alkyl chains, the method for preparing the same and use thereof in photoelectric devices. By applying the branching alkyl chains as the solubilizing group to the preparation of organic conjugated molecules (for example, organic conjugated polymers), the number of methylenes between the resultant alky side chains and the backbone, i.e., m>1, which can effectively reduce the effect of the alkyl chains on the backbone π-π stacking, thereby ensuring the solubility of the organic conjugated molecule while greatly increasing the mobility of their carriers. It is suitable for an organic semiconductor material in photoelectric devices such as organic solar cells, organic light emitting diodes and organic field effect transistors, etc.
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- Synthesis of polyisoprene terpenoid dendrons and their applications in oligo(phenylene ethynylene)s as "shells"
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The novel double-stage convergent synthesis of a new class of polyisoprene terpenoid (PIPTP) dendrons is described. PIPTP dendrons bear a highly branched aliphatic hydrocarbon skeleton and a hydrophilic hydroxy focal point functionality. These dendrons have the specific formula C (5×2G+1-5)H(5×2 G+2-8)O, and each dendritic layer is constructed from an isoprene unit. The key branching steps involve a double alkyl-metal addition to an ester functionality, followed by deoxygenation of the resulting tertiary alcohol by triethylsilane and trifluoroacetic acid, then hydrogenation or hydrogenolysis. The dendrons were also attached to oligo(phenylene ethynylene)s (OPEs) so as to function as protective shells to allow fine tuning of the nanoscopic environment around the OPE moiety, and to exert precise control of the packing density and intermolecular interaction between the OPE cores. Fluorescence quantum yield data reveal that the OPE core is better encapsulated by the PIPTP dendrons than by Frechet dendrons.
- Chai, Wen-Yu,Shi, Zi-Fa,An, Peng,Wang, Wei,Wang, Lu-Feng,Cao, Xiao-Ping
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supporting information; experimental part
p. 143 - 155
(2012/03/26)
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- 2-SUBSTITUTED QUINAZOLIN-4-YLAMINE ANALOGUES AS CAPSAICIN RECEPTOR MODULATORS
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Certain 2-substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathologi
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