- POLYCYCLIC AMINES AS OPIOID RECEPTOR MODULATORS
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The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
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Paragraph 0129; 0289
(2018/10/11)
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- A double bond-conjugated dimethylnitrobenzene-type photolabile nitric oxide donor with improved two-photon cross section
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Abstract Photocontrollable NO donors enable precise spatiotemporal release of NO under physiological conditions. We designed and synthesized a novel dimethylnitrobenzene-type NO donor, Flu-DNB-DB, which contains a carbon-carbon double bond in place of the
- Ieda, Naoya,Hishikawa, Kazuhiro,Eto, Kei,Kitamura, Kai,Kawaguchi, Mitsuyasu,Suzuki, Takayoshi,Fukuhara, Kiyoshi,Miyata, Naoki,Furuta, Toshiaki,Nabekura, Junichi,Nakagawa, Hidehiko
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supporting information
p. 3172 - 3175
(2015/07/08)
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- Chemoselective reduction and self-immolation based FRET probes for detecting hydrogen sulfide in solution and in cells
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Hydrogen sulfide (H2S) has been regarded as the third gaseous transmitter. Based on the mechanism of chemoselective azido reduction and self-immolation, five fluorescence resonance energy transfer (FRET) probes for the detection of H2S were designed and synthesized. The effect of functional substitution of the self-immolative moiety on azido reduction and quinone-methide rearrangement were investigated. Their fluorescence responses and chemoselectivity for H2S detection were evaluated in solutions and in cells. This strategy may provide a general route for designing H 2S probes with many commercially available FRET pairs. the Partner Organisations 2014.
- Chen, Bifeng,Wang, Peng,Jin, Qingqing,Tang, Xinjing
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supporting information
p. 5629 - 5633
(2014/07/22)
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- Visible light-induced nitric oxide release from a novel nitrobenzene derivative cross-conjugated with a coumarin fluorophore
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Nitric oxide (NO) is a well-known free-radical molecule which is endogenously biosynthesised and shows various functions in mammals. To investigate NO functions, photocontrollable NO donors, compounds which release NO in response to light, are expected to
- Kitamura, Kai,Ieda, Naoya,Hishikawa, Kazuhiro,Suzuki, Takayoshi,Miyata, Naoki,Fukuhara, Kiyoshi,Nakagawa, Hidehiko
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supporting information
p. 5660 - 5662
(2015/01/08)
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- Peroxynitrite generation from a NO-releasing nitrobenzene derivative in response to photoirradiation
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Photocontrollable ONOO- generation from a nitrobenzene derivative was demonstrated. The designed compound released NO in response to photoirradiation, and the resulting semiquinone reduced molecular oxygen to generate O2-; reaction of the two generated ONOO -, as confirmed with an ONOO- fluorescent probe, HKGreen-3.
- Ieda, Naoya,Nakagawa, Hidehiko,Horinouchi, Taeko,Peng, Tao,Yang, Dan,Tsumoto, Hiroki,Suzuki, Takayoshi,Fukuhara, Kiyoshi,Miyata, Naoki
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supporting information; experimental part
p. 6449 - 6451
(2011/06/27)
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- Effect of the ortho modification of azobenzene on the photoregulatory efficiency of DNA hybridization and the thermal stability of its eis form
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We synthesized various azobenzenes methylated at their ortho positions with respect to the azo bond for more effective photoregulation of DNA hybridization. Photoregulatory efficiency, evaluated from the change of T m (ΔTm) induced by trans-cis isomerization, was significantly improved for all ortho-modified azobenzenes compared with non-modified azobenzene due to the more stabilized trans form and the more destabilized cis form. Among the synthesized azobenzenes, 4-carboxy-2',6'- dimethylazobenzene (2',6'-Me-Azo), in which two ortho positions of the distal benzene ring with respect to carboxyl group were methylated, exhibited the largest ΔTm, whereas the newly synthesized 2,6-Me-Azo (4-carboxy-2,6- dimethylazobenzene), which possesses two methyl groups on the two ortho positions of the other benzene ring, showed moderate improvement of ΔTm. Both NMR spectroscopic analysis and computer modeling revealed that the two methyl groups on 2',6'-Me-Azo were located near the imino protons of adjacent base pairs; these stabilized the DNA duplex by stacking interactions in the trans form and destabilized the DNA duplex by steric hindrance in the cis form. In addition, the thermal stability of cis-2',6'-Me-Azo was also greatly improved, but not that of cis2,6-Me-Azo. Solvent effects on the half-life of the cis form demonstrated that cis-to-trans isomerization of all the modified azobenzenes proceeded through an inversion route. Improved thermal stability of 2',6'-Me-Azo but not 2,6-Me-Azo in the eis form was attributed to the retardation of the inversion process due to steric hindrance between lone pair electrons of the π orbital of the nitrogen atom and the methyl group on the distal benzene ring.
- Nishioka, Hidenori,Liang, Xingguo,Asanuma, Hiroyuki
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supporting information; experimental part
p. 2054 - 2062
(2010/07/05)
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- NOVEL ACYLAMINOBENZAMIDE DERIVATIVES
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The present invention relates to novel Acylaminobenzamide derivatives represented by the following formula (I) and use thereof as pesticides: wherein V represents an aromatic ring group of V1 to V5 described in the detailed description, Q represents an ar
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Page/Page column 74
(2010/04/03)
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- Photoinduced nitric oxide release from a hindered nitrobenzene derivative by two-photon excitation
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(Chemical Equation Presented) Here, we demonstrated photoinduced NO generation from a 2,6-dimethylnitrobenzene-based compound (Flu-DNB) via a two-photon excitation (TPE) process. After pulse laser irradiation to a solution of Flu-DNB, oxidation products of NO were observed. This is the first account of a non-nitrosyl-chelated metal ion containing NO donor which can be controlled by the TPE technique.
- Hishikawa, Kazuhiro,Nakagawa, Hidehiko,Furuta, Toshiaki,Fukuhara, Kiyoshi,Tsumoto, Hiroki,et al.
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supporting information; experimental part
p. 7488 - 7489
(2009/10/16)
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- Discovery, Modeling, and Human Pharmacokinetics of N-(2-Acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl) -thiophene-2-carboxamide (TBC3711), a Second Generation, ETA Selective, and Orally Bioavailable Endothelin Antagonist
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Sitaxsentan (1) (Wu et al. J. Med. Chem. 1997, 40, 1690) is our first endothelin antagonist being evaluated in clinical trials. It has demonstrated biological effects in an acute hemodynamic study in CHF (Givertz et al. Circulation 2000, 101, 2922), an op
- Wu, Chengde,Decker, E. Radford,Blok, Natalie,Bui, Huong,You, Tony J.,Wang, Junmei,Bourgoyne, Andree R.,Knowles, Vippra,Berens, Kurt L.,Holland, George W.,Brock, Tommy A.,Dixon, Richard A. F.
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p. 1969 - 1986
(2007/10/03)
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- Synthesis and binding studies of bowl-shaped hosts for quaternary ammoniums
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Two bowl-shaped hosts for quaternary ammonium salts were synthesized and their binding properties, along with the anion effect, were systematically examined and compared in CDCl3.
- Jeong, Kyu-Sung,Shin, Kwang Hoon,Kim, Soong-Hyun
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p. 1166 - 1167
(2007/10/03)
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- Piperazine compounds and medicinal use thereof
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The present invention relates to a piperazine compound of the formula wherein R1and R2are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4and R5are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6and R7are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8and R9are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds. The compound of the present invention has superior TNF-α production inhibitory effect and/or IL-10 production promoting effect, and, since it is free of or shows only strikingly reduced expression of an effect on the central nervous system, the compound is useful as a highly safe and superior TNF-α production inhibitor an/or IL-10 production promoter and is useful as an agent for the prophylaxis or treatment of various diseases caused by abnormal TNF-α production, diseases curable with IL-10, such as chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases due to infection, autoimmune diseases, allergic diseases, and TNF-α mediated diseases.
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- Migrations in Oxidations of Mesidine
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The oxidation of mesidine in methanolic media by ferricyanide, dichromate, and persulfate afforded an anil 4 containing a shifted methoxymethyl group in addition to the principal anil 3 formed by oxidative dealkylation.Possible intermediates 6, 7, and 8 were prepared and oxidized to the product anils.Oxidations of related anilines 9, 10, and 13 did not parallel those of mesidine but afforded analogues of 3.There is significant spectral evidence for anils with alkyl shifts but little for anils analogous to 4.
- Goldstein, Stephen L.,McNelis, Edward
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p. 1613 - 1620
(2007/10/02)
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