- NOVEL BENZODIAZEPINE DERIVATIVES AND USES THEREOF
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The present disclosure provides compounds and compositions capable of extending lifespan, and methods of use thereof.
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Paragraph 0492-0494
(2019/12/24)
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- NOVEL MACROCYCLIC DIACETYLENE COMPOUND AND METHOD FOR MANUFACTURING THEREOF
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The present invention relates to a macrocyclic diacetylene compound, and a production method thereof. More specifically, the present invention relates to a macrocyclic diacetylene compound enabling production of diameter-adjustable polydiacetylene nanotube. The present invention further relates to a production method thereof. According to the present invention, it is possible to produce diacetylene nanotube having various ranges of diameter by undergoing crystallization of the diacetylene compound, and polydiacetylene nanotube can be formed by making the diacetylene nanotube irradiated with ultraviolet light or gamma rays.COPYRIGHT KIPO 2018
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Paragraph 0250; 0255
(2018/04/12)
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- The flexibility-complementarity dichotomy in receptor-ligand interactions
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Synthetic supramolecular complexes provide an opportunity for quantitative systematic exploration of the relationship between chemical structure and molecular recognition phenomena. A family of closely related zinc porphyrin-pyridine complexes was used to examine the interplay of conformational flexibility and geometric complementarity in determining the selectivity of molecular recognition events. The association constants of 48 zinc porphyrin-pyridine complexes were measured in two different solvents, toluene and 1,1,2,2-tetrachloroethane (TCE). These association constants were used to construct 32 chemical double mutant cycles to dissect the free energy contributions of intramolecular H-bonds between the phenol side arms of the porphyrins and the ester or amide side arms of the pyridine ligands. Effective molarities (EM) for the intramolecular interactions were determined by comparison with the corresponding intermolecular H-bonding interactions. The values of EM do not depend on the solvent and are practically identical for amide and ester H-bond acceptors located at the same site on the ligand framework. However, there are variations of an order of magnitude in EM depending on the flexibility of the linker used to connect the H-bond acceptors to the pyridine ligands. Rigid aromatic linkers give values of EM that are an order of magnitude higher than the values of EM for the corresponding ester linkers, which have one additional torsional degree of freedom. However, the most flexible ether linkers give values of EM that are also higher than the values of EM for the corresponding ester linkers, which have one less torsional degree of freedom. Although the penalty for conformational restriction on binding is higher for the more flexible ether linkers, this flexibility allows optimization of the geometric complementarity of the ligand for the receptor, so there is a trade off between preorganization and fit.
- Sun, Hongmei,Hunter, Christopher A.,Llamas, Eva Marina
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p. 1444 - 1453
(2015/02/19)
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- Symmetric double-headed aminopyridines, a novel strategy for potent and membrane-permeable inhibitors of neuronal nitric oxide synthase
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We report novel neuronal nitric oxide synthase (nNOS) inhibitors based on a symmetric double-headed aminopyridine scaffold. The inhibitors were designed from crystal structures of leads 1 and 2 (Delker, S. L.; Ji, H.; Li, H.; Jamal, J.; Fang, J.; Xue, F.; Silverman, R. B.; Poulos, T. L.Unexpected binding modes of nitric oxide synthase inhibitors effective in the prevention of cerebral palsy. J. Am. Chem. Soc. 2010, 132, 5437-5442) and synthesized using a highly efficient route. The best inhibitor, 3j, showed low nanomolar inhibitory potency and modest isoform selectivity. It also exhibited enhanced membrane permeability. Inhibitor 3j binds to both the substrate site and the pterin site in nNOS but only to the substrate site in eNOS. These compounds provide a basis for further development of novel, potent, isoform selective, and bioavailable inhibitors for nNOS.
- Xue, Fengtian,Fang, Jianguo,Delker, Silvia L.,Li, Huiying,Martásek, Pavel,Roman, Linda J.,Poulos, Thomas L.,Silverman, Richard B.
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experimental part
p. 2039 - 2048
(2011/05/30)
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- Aminopyridine Dimer Compounds, Compositions and Related Methods for Neuronal Nitric Oxide Synthase Inhibition
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Nitric oxide synthase (NOS) inhibitor compounds comprising bi-terminal aromatic ring moieties, and related methods of NOS inhibition.
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Page/Page column 9
(2010/08/18)
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