- Quantum yield improvement of red-light-emitting firefly luciferin analogues for in vivo bioluminescence imaging
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The dimethylamino group of AkaLumine ((4S)-2-[(1E,3E)-4-[4-(dimethylamino)phenyl]-1,3-butadien-1-yl]-4,5-dihydro-4-thiazolecarboxylic acid), a red-light-emitting firefly luciferin analogue, was replaced by cyclic amino groups (1-pyrrolidinyl, 1-piperidino, 1-azepanyl, and 4-morpholino) to give AkaLumine analogues exhibiting desirable bioluminescence with emission maxima in the red region (656–667 nm). In particular, a bioluminescence reaction of 1-pyrrolidinyl analogue with a recombinant Photinus pyralis luciferase showed a higher quantum yield than that with AkaLumine, giving an improved bioluminescence intensity. The 1-pyrrolidinyl analogue also showed the strongest luminescence in whole-body luciferase-expressing mice among the analogues, indicating that a quantum yield improvement of a luciferin analogue is effective to increase bioluminescence imaging intensity.
- Kiyama, Masahiro,Iwano, Satoshi,Otsuka, Satoshi,Lu, Shijia W.,Obata, Rika,Miyawaki, Atsushi,Hirano, Takashi,Maki, Shojiro A.
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p. 652 - 660
(2018/01/04)
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- The Role of N-Substituents in Radiationless Deactivation of Aminated Derivatives of a Locked GFP Chromophore
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We report the creation of a novel group of the ABDI-BF2 fluorescent dyes based on the conformationally locked GFP chromophore. We studied the intramolecular mechanism of radiationless deactivation of the ABDI-BF2 fluorophore by introducing the various substituents at the nitrogen atom. The results of this study and our previous work allowed us to claim that in case of ABDI-BF2 this deactivation is determined by the formation of the nonfluorescent internal charge transfer exited state with a planar quinoidal structure. The electronic effects have a greater impact on the radiationless deactivation than the conformation. Thus, the introduction of an electron-donating group is more effective than the creation of rigid derivatives. The presented dyes are characterized by high fluorescence quantum yields and pH-independence in the physiological pH range, making them promising candidates for a wide spectrum of fluorescence labeling applications.
- Baleeva, Nadezhda S.,Zaitseva, Snezhana O.,Gorbachev, Dmitriy A.,Smirnov, Alexander Yu.,Zagudaylova, Marina B.,Baranov, Mikhail S.
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supporting information
p. 5219 - 5224
(2017/09/29)
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- QUINOLINE-DERIVED AMIDE MODULATORS OF VANILLOID VR1 RECEPTOR
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This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to quinoline-derived amides that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
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Page 156-157
(2008/06/13)
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- Imidazole derivatives
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The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof. The compounds of the formulas (I) and (XII) and pharmaceutically acceptable salts thereof of the present invention inhibit IL-4 and IL-5 production by Th2 cells and are effective for the prophylaxis and treatment of allergic diseases such as atopic dermatitis, bronchial asthma, allergic rhinitis and the like.
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- Ultrasound effect on the synthesis of 4-alkyl-(aryl)aminobenzaldehydes
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The sonochemical nucleophilic aromatic substitutions on 4-fluorobenzaldehyde with different azacycloalkanes and azoles have been studied. A beneficial ultrasound effect was observed, reactions were clean and high yields of the products were isolated after 15 min sonication.
- Magdolen, Peter,Me?iarová, Mária,Toma, ?tefan
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p. 4781 - 4785
(2007/10/03)
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- Photoconductive properties of PVK-based photorefractive polymer composites doped with fluorinated styrene chromophores
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We have synthesized nine anisotropic chromophores, with different degrees of fluorination, and studied the effect of the chromophore's ionization potential on charge-transfer complexation, photoconductivity, and response time in photorefractive polymer mi
- Hendrickx, Eric,Zhang, Yadong,Ferrio, Kyle B.,Herlocker, Jon A.,Anderson, Jeff,Armstrong, Neal R.,Mash, Eugene A.,Persoons, Andre P.,Peyghambarian, Nasser,Kippelen, Bernard
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p. 2251 - 2258
(2007/10/03)
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