- Synthesis of N-Heterocycles by Reductive Cyclization of Nitroalkenes Using Molybdenum Hexacarbonyl as Carbon Monoxide Surrogate
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The development of a method that uses molybdenum hexacarbonyl [Mo(CO)6] as carbon monoxide (CO) surrogate for the palladium-catalyzed reductive cyclization of nitroalkenes into indoles or thienopyrroles is reported. Several types of nitroalkenes could be transformed into the desired products in excellent yields and in most cases with complete regioselectivities and higher yields than those previously reported with palladium/CO system.
- Su, Zhiyou,Liu, Bo,Liao, Hongze,Lin, Hou-Wen
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supporting information
p. 4059 - 4066
(2020/06/21)
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- Berbamine Analogs Exhibit Differential Protective Effects From Aminoglycoside-Induced Hair Cell Death
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Hearing loss is the third most common chronic health condition in the United States and largely results from damage to sensory hair cells. Major causes of hair cell damage include aging, noise exposure, and medications such as aminoglycoside antibiotics.
- Hudson, Alexandria M.,Lockard, Gavin M.,Namjoshi, Ojas A.,Wilson, Joseph W.,Kindt, Katie S.,Blough, Bruce E.,Coffin, Allison B.
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- Tetrahydroisoquinoline derivative and application thereof
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Provided are a tetrahydroisoquinoline derivative and an application thereof. The invention relates to a compound represented by the formula (V) and a preparation method and an application thereof in medicines. In particular, the invention relates to the d
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Paragraph 0226; 0227; 0228
(2016/10/09)
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- Enantioselective Oxidative Aerobic Dealkylation of N-Ethyl Benzylisoquinolines by Employing the Berberine Bridge Enzyme
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N-Dealkylation methods are well described for organic chemistry and the reaction is known in nature and drug metabolism; however, to our knowledge, enantioselective N-dealkylation has not been yet reported. In this study, exclusively the (S)-enantiomers o
- Gandomkar, Somayyeh,Fischereder, Eva-Maria,Schrittwieser, Joerg H.,Wallner, Silvia,Habibi, Zohreh,Macheroux, Peter,Kroutil, Wolfgang
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supporting information
p. 15051 - 15054
(2016/01/25)
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- Synthesis and structure activity relationship of tetrahydroisoquinoline- based potentiators of GluN2C and GluN2D containing N-Methyl-D-aspartate receptors
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We describe here the synthesis and evaluation of a series of tetrahydroisoquinolines that show subunit-selective potentiation of NMDA receptors containing the GluN2C or GluN2D subunits. Bischler-Napieralski conditions were employed in the key step for the
- Santangelo Freel, Rose M.,Ogden, Kevin K.,Strong, Katie L.,Khatri, Alpa,Chepiga, Kathryn M.,Jensen, Henrik S.,Traynelis, Stephen F.,Liotta, Dennis C.
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supporting information
p. 5351 - 5381
(2013/07/26)
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- Novel hybrids from lamellarin D and combretastatin A 4 as cytotoxic agents
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A new series of hybrids of lamellarin D and combretastatin A 4, 1,2-diphenyl-5,6-dihydropyrrolo [2,1-a] isoquinolines, were designed as cytotoxic agents based on principles of combination in medicinal chemistry and taking the parent compounds' different anti-proliferative mechanisms into consideration. Twenty-two novel hybrids were synthesized through a convenient route, with a key step of core pyrrole formation and evaluated for their anti-proliferative activities in vitro against K-562, A-549, SMMC-7721, SGC-7901 and HCT-116 cancer cell lines. The results showed that some hybrids had good anti-proliferative activities in low IC50 ranges.
- Shen, Li,Yang, Xiaochun,Yang, Bo,He, Qiaojun,Hu, Yongzhou
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experimental part
p. 11 - 18
(2010/03/03)
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- Enantioselective synthesis of (R)-(+)- and (S)-(-)-higenamine and their analogues with effects on platelet aggregation and experimental animal model of disseminated intravascular coagulation
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Optically active tetrahydroisoquinoline alkaloids, (R)-(+)-higenamine (1R) and (S)-(-)-higenamine (1 S), and their optically active 1-naphthylmethyl analogues (2 and 3), were synthesized by enantioselective hydrogenation of the corresponding dihydroisoqui
- Pyo, Mi Kyung,Lee, Duck-Hyung,Kim, Doo-Hyun,Lee, Ji-Hye,Moon, Jong-Cheon,Chang, Ki Churl,Yun-Choi, Hye Sook
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body text
p. 4110 - 4114
(2009/05/26)
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- Method and health food for preventing and/or alleviating psychiatric disorder, and/or for effectuating sedation
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A method for preventing and/or alleviating a psychiatric disorder, and/or effectuating sedation, comprising administering a benzylisoquinoline derivative represented by General Formula (I): wherein R1, R2, R3 and X each re
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Page/Page column 9
(2008/06/13)
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- TETRAHYDROISOQUINOLYL ACETAMIDE DERIVATIVES FOR USE AS OREXIN RECEPTOR ANTAGONISTS
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The invention relates to novel acetamide derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compound
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- Antiplatelet activity of synthetic pyrrolo-benzylisoquinolines
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Pyrrolo-benzylisoquinolines were prepared as target compounds and their antiplatelet aggregation activity, adreno-receptor affinity, and cytotoxicity were screened. Compounds 1d-9d showed specific antiplatelet aggregation activity induced by arachidonic acid and collagen. Among them, 8d and 9d exhibited better activity than the reference drug, aspirin and 9d also showed inhibition of platelet aggregation by all four inducers.
- Kuo, Reen-Yen,Wu, Chin-Chung,Chang, Fang-Rong,Yeh, Jwu-Lai,Chen, Ing-Jun,Wu, Yang-Chang
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p. 821 - 823
(2007/10/03)
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- NOVEL ENANTIOMERS OF TETRAHYDROISOQUINOLINE DERIVATIVES AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, THEIR PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS
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The disclosure concerns novel enantiomers of tetrahydroisoquinoline derivatives and their pharmaceutically acceptable salts, their preparations and pharmaceutical compositions. The enantiomers of tetrahydroisoquinoline derivatives are provided which are useful in stimulating heart rate and hypotensive activity, inhibitory activity against platelet aggregation, and suppressive against inducible NO synthase. The enantiomers of tetrahydroisoquinoline derivatives and their pharmaceutically acceptable salts are effective for treating congestive heart failure, hypertension, thrombosis, inflammation, septicemia, cardiac insufficiency, and disseminated intravascular coagulopathy.
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Page/Page column 41-42
(2008/06/13)
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- Carbon-13 NMR Spectra of Tembamide, Aegeline and Related Amides
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Carbon-13 NMR spectral studies of tembamide (1) and aegeline (2), constituents of Fagara hyemalis and Aegle marmelos respectively, and a series of their structurally related amides (3-13) have been carried out.The assignment of the resonances of two related dimers are also reported.The assignment of the various resonances were made by considering the changes in chemical shifts produced by the change of substituents and also by using 1, 13 and a related compound as model compounds.
- Patra, Amarendra,Mitra, Alok K.,Ghosh, Arundhati,Mukhopadhyay, Prabir K.
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