- PYRAZOLYLBENZO[D]IMIDAZOLE DERIVATIVES
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A compound represented by the general Formula (I), whereinhydrogen atoms shown as attached to pyrazole and benzimidazole rings are attached to one of nitrogen atoms of the pyrazole or benzimidazole ring, respectively; R1 represents -X-Q-P, wherein X is absent or represents –CH2-, –C(O)-, or –C(O)NH-(CH2)k-, wherein k is 0, 1 or 2; Q is selected from the group consisting of Q1, Q2, Q3, Q4 and Q5; P is absent or represents straight-or branched-chain C1-C3 alkyl, –(CH2)l-NR2R3, or–(CH2)m-C(O)-NR2R3, wherein l and m independently of each other represent 0, 1 or 2, with the proviso that when B in Q1 represents oxygen atom, then P is absent;and R2and R3 independently represent C1 or C2 alkyl, or R2 and R3 together with nitrogen atom to which they are both attached form a 6- membered saturated heterocyclicring, wherein one of carbon atoms can be replaced with oxygen, -NH-or –N(C1-C2)alkyl-; and acid addition salts thereof. The compound can be useful in the treatment of cancer diseases. (I)
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Page/Page column 21
(2014/09/29)
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- Design of a highly sensitive fluorescent probe for interfacial electron transfer on a TiO2 surface
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Single-molecule fluorescent probe: The formation of the highly fluorescent 4-NHOH form of a 3,4-dinitrophenyl-substituted boron dipyrromethane dye can be used to study interfacial electron transfer on individual TiO2 particles (see picture; B yellow, C gray, F green, H white, O red). Kinetic and image analyses of the resulting fluorescence bursts reveal temporal dynamics of molecular interactions and reactive-site distributions.
- Tachikawa, Takashi,Wang, Nan,Yamashita, Soichiro,Cui, Shi-Cong,Majima, Tetsuro
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supporting information; experimental part
p. 8593 - 8597
(2011/01/10)
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- Catalytic asymmetric syntheses of tyrosine surrogates
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(Chemical Equation Presented) Amino acid esters 5-11 as tyrosine mimics have been synthesized in excellent enantioselectivity (up to 99.6% ee) and in good overall chemical yields. The key step in the sequence was the Burk's [Rh(COD)(2R,5R)-Et-DuPhos]BF4-catalyzed asymmetric hydrogenation of enamides with a variety of reactive functional groups.
- Han, Xiaojun,Civiello, Rita L.,Fang, Haiquang,Wu, Dedong,Gao, Qi,Chaturvedula, Prasad V.,Macor, John E.,Dubowchik, Gene M.
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experimental part
p. 8502 - 8510
(2009/04/04)
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- A bioinspired construct that mimics the proton coupled electron transfer between P680?+ and the Tyrz-his190 pair of photosystem II
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A bioinspired hybrid system, composed of colloidal TiO2 nanoparticles surface modified with a photochemically active mimic of the PSII chlorophyll-Tyr-His complex, undergoes photoinduced stepwise electron transfer coupled to proton motion at the phenolic site. Low temperature electron paramagnetic resonance studies reveal that injected electrons are localized on TiO2 nanoparticles following photoexcitation. At 80 K, 95% of the resulting holes are localized on the phenol moiety and 5% are localized on the porphyrin. At 4.2 K, 52% of the holes remain trapped on the porphyrin. The anisotropic coupling tensors of the phenoxyl radical are resolved in the photoinduced D-band EPR spectra and are in good agreement with previously reported g-tensors of tyrosine radicals in photosystem II. The observed temperature dependence of the charge shift is attributed to restricted nuclear motion at low temperature and is reminiscent of the observation of a trapped high-energy state in the natural system. Electrochemical studies show that the phenoxyl/phenol couple of the model system is chemically reversible and thermodynamically capable of water oxidation. Copyright
- Moore, Gary F.,Hambourger, Michael,Gervaldo, Miguel,Poluektov, Oleg G.,Rajh, Tijana,Gust, Devens,Moore, Thomas A.,Moore, Ana L.
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supporting information; experimental part
p. 10466 - 10467
(2009/02/05)
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- Calcitonin gene related peptide receptor antagonists
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The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
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- CALCITONIN GENE RELATED PEPTIDE RECEPTOR ANTAGONISTS
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The presnt invention relates to compounds of Formula (I), as antagonists of calcitonin gene-related peptide receptors ("CGRP-receptor"), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
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