- Optical Control of CRAC Channels Using Photoswitchable Azopyrazoles
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The Ca2+ release-activated Ca2+ (CRAC) channels control many Ca2+-modulated physiological processes in mammals. Hyperactivating CRAC channels are known to cause several human diseases, including Stormorken syndrome. Here, we show the design of azopyrazole-derived photoswitchable CRAC channel inhibitors (designated piCRACs), which enable optical inhibition of store-operated Ca2+ influx and downstream signaling. Moreover, piCRAC-1 has been applied in vivo to alleviate thrombocytopenia and hemorrhage in a zebrafish model of Stormorken syndrome in a light-dependent manner.
- Yang, Xingye,Ma, Guolin,Zheng, Sisi,Qin, Xiaojun,Li, Xiang,Du, Lupei,Wang, Youjun,Zhou, Yubin,Li, Minyong
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p. 9460 - 9470
(2020/06/27)
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- AMINOPEPTIDASE A INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.
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Page/Page column 51
(2020/06/10)
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- Benzylic C?H Functionalisation by [Et3SiH+KOtBu] leads to Radical Rearrangements in o-tolyl Aryl Ethers, Amines and Sulfides
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Reaction of Et3SiH+KOtBu with diaryl ethers, sulfides and amines that feature an ortho alkyl group leads to rearrangement products. The rearrangements arise from formation of benzyl radicals, likely formed through hydrogen atom abstraction by triethylsilyl radicals. The rearrangements involve cyclisation of the benzyl radical onto the partner arene, which, from computation, is the rate determining step. In the case of diaryl ethers, Truce-Smiles rearrangements arise from radical cyclisations to form 5-membered rings, but for diarylamines, cyclisations to form dihydroacridines are observed. (Figure presented.).
- Arokianathar, Jude N.,Kolodziejczak, Krystian,Bugden, Frances E.,Clark, Kenneth F.,Tuttle, Tell,Murphy, John A.
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supporting information
p. 2260 - 2267
(2020/05/06)
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- One-Step Synthesis of Substituted Benzofurans from ortho- Alkenylphenols via Palladium-Catalyzed C=H Functionalization
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A dehydrogenative oxygenation of C(sp2)=H bonds with intramolecular phenolic hydroxy groups has been developed, which provides a straightforward and concise access to structurally diversely benzofurans from ortho-alkenylphenols. The reaction is catalyzed by palladium on carbon (Pd/C) without any oxidants and sacrificing hydrogen acceptors.
- Yang, Dejun,Zhu, Yifei,Yang, Na,Jiang, Qiangqiang,Liu, Renhua
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supporting information
p. 1731 - 1735
(2016/06/09)
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- Arylchalcogenoarylalkyl-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof
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The invention relates to compounds of formula (I) wherein the groups R and R′ A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
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Page/Page column 49
(2011/04/14)
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- Novel phenyl-substituted imidazolidines, process for preparation thereof, medicaments comprising said compounds and use thereof
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The invention relates to compounds of formula (I) wherein the groups have stated meanings, and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.
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Page/Page column 48
(2011/08/04)
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- Novel highly potent and selective nonsteroidal aromatase inhibitors: Synthesis, biological evaluation and structure-activity relationships investigation
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In further pursuing our search for potent and selective aromatase inhibitors, a new series of molecules was designed and synthesized, exploring possible structural modifications of a previously identified xanthone scaffold. Among them, highly potent compounds, with inhibitory activity in the low nanomolar range, were found. In particular, substitution of the heterocyclic oxygen atom in the xanthone core by a sulfur atom and/or increase in structure flexibility seemed to be favorable for the interaction with the enzyme.
- Gobbi, Silvia,Zimmer, Christina,Belluti, Federica,Rampa, Angela,Hartmann, Rolf W.,Recanatini, Maurizio,Bisi, Alessandra
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supporting information; experimental part
p. 5347 - 5351
(2010/10/21)
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- MORPHOLINE DERIVATIVES AS NOREPINEPHRINE REUPTAKE INHIBITORS
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Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.
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Page/Page column 41-42
(2008/06/13)
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- Imidazo heterocyclic compounds
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A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
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