- CHEMICAL MODULATORS OF STORE-OPERATED CALCIUM CHANNELS AND THEIR THERAPEUTIC APPLICATIONS
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Methods of identification of inhibitors of calcium release-activated calcium (CRAC) channel and small molecule inhibitors of CRAC channel, including methods of their synthesis and pharmaceutical use, are disclosed.
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Paragraph 0131
(2019/04/14)
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- Synthesis and Antimicrobial Evaluation of New Pyrrolo-isoxazolidine Derivatives
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In the present study, pyrrolo-isoxazolidines 3(a-l) and 4(a-e), 4g, 4i, 4j have been synthesized by using the 1,3-dipolar cycloaddition reactions of nitrones 1(a-l) with ester substituted N-aryl maleimide (2b). These heterocycles have been obtained in cis and trans diastereomeric forms. The structures of newly synthesized heterocycles have been confirmed from their spectroscopic parameters such as IR,1H NMR,13C NMR and ESI-MS. The in vitro antimicrobial evaluation of these compounds were also investigated. Most of the prepared heterocycles showed significant antimicrobial properties. C3-phenyl substituted products exhibited the remarkable antibacterial behaviours while C3-thienyl/furyl substituted heterocycles proved themselves potent antifungal agents.
- Yusuf, Mohamad,Shehneela,Singh, Baldev
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p. 220 - 228
(2018/12/11)
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- 4-(3-Dialkylamino-2,5-dioxopyrrolidin-1-yl)benzoic acid esters
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Reactions of alkyl 4-aminobenzoates with maleic anhydride give the corresponding alkyl 4-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoates, and the latter are converted into 4-(3-dialkylamino-2,5-dioxo-2,3,4,5-tetrahydro-1H- pyrrol-1-yl)benzoates by treatme
- Kolyamshin,Danilov,Kol'Tsov
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p. 393 - 396
(2007/10/03)
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- Investigation of arene-arene interaction in stereoselective MCPBA epoxidation
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Effect of arene-arene interaction in stereoselective MCPBA epoxidation was investigated using 5,6-dimethyl-2-phenyl-3a,4,7,7a-tetrahydroisoindole-1,3-diones 1. From the good correlation between the stereoselectivity of the products and Hammett's coefficients of para-substituents (σP) on the phenyl group, it was found that polar/π interaction between the phenyl group and MCPBA is the main interaction for controlling the stereoselectivity in the reaction. Other arene-arene interactions, charge-transfer complexation and edge-to-face interaction, were assumed to be much weaker than polar/π interaction in this reaction.
- Kishikawa, Keiki,Naruse, Mamoru,Kohmoto, Shigeo,Yamamoto, Makoto,Yamaguchi, Kentaro
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p. 462 - 468
(2007/10/03)
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- Compounds containing a michael-acceptor, especially maleimide or maleic acid derivatives, directly or indirectly linked to a chromophore and their use in long lasting sunscreen compositions
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The present invention relates to compounds which are useful as sunscreens. The compounds persist on the skin for much longer than conventional sunscreens because they comprise a Michael acceptor linked directly or indirectly to a chromophore. The Michael acceptor is capable of undergoing a conjugate addition reaction with thiol groups present in cysteine residues of keratin and thus the compound is chemically bound to the skin and will not be removed by immersion in water.
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- INFLUENCE OF MEDIUM AND SUBSTITUENTS ON ACYLATION OF AROMATIC AMINES AND THEIR POLYMERIC ANALOGS WITH MALEIC ANHYDRIDE
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Correlation relationships describing the influence of substituents and solvents on the rate of acylation of aromatic amines and their polymeric analogs with maleic anhydride have been derived.
- Donya, A. P.,Pakter, M. K.,Sokhina, S. I.
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p. 2093 - 2097
(2007/10/02)
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