- N-acetamido galactose modified 3-nitrophthalimide derivative, preparation method, application and liver targeting probe
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The invention provides an N-acetamido galactose modified 3-nitrophthalimide derivative, a preparation method and an application of the N-acetamido galactose modified 3-nitrophthalimide derivative, anda liver targeting probe. The preparation method of the fluorescent probe is simple, and the obtained fluorescent probe takes N-acetamido galactose as a liver targeting group and 3-nitrophthalimide asa CO response group, can be used as a CO detection reagent, is good in selectivity and high in sensitivity, can target liver cells and liver tissues, and can be used for dynamically monitoring the COlevel.
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Paragraph 0041; 0045-0046
(2020/10/20)
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- A fluorescent ESIPT probe for imaging co-releasing molecule-3 in living systems
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CO-releasing molecule-3 (CORM-3) has been widely used recently as a convenient and safe CO donor to release exogenous CO in living cells and to study the effects of CO on cellular systems. Accordingly, development of effective methods for detecting and tracking CORM-3 in living systems is of great significance. In this work, a readily available fluorescent probe for detection of CORM-3 was reported for the first time. This probe is based on an excited-state intramolecular proton transfer (ESIPT) dye phthalimide and uses the reducing ability of CORM-3 to convert a nitro group to an amino group, and more importantly, it can be used for rapid, highly selective, and sensitive detection of CORM-3 with a distinct turn-on green fluorescence change in aqueous solution, living cells, and animals, thus providing a useful tool for studying CORM-3 in living systems.
- Feng, Weiyong,Feng, Shumin,Feng, Guoqiang
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p. 8602 - 8606
(2019/08/26)
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- SMALL MOLECULES AGAINST CEREBLON TO ENHANCE EFFECTOR T CELL FUNCTION
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Disclosed are small molecules against cereblon to enhance effector T cell function. Methodos of making thes molecules and methods of using them to treat various disease states are also disclosed.
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Page/Page column 140
(2017/10/11)
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- A facile and green synthesis of novel imide and amidic acid derivatives of phenacetin as potential analgesic and anti-pyretic agents
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Facile and green syntheses of potential analgesic and antipyretic compounds, N-(4-ethoxy-phenyl)-2-(1,3- dioxo-1,3-dihydroisoindol-2-yl)acetamide derivatives 6a-g and N-[(4-ethoxy-phenylcarbamoyl)methyl]phthalamic acid derivatives 10a-g have been developed. Two synthetic routes (A and B) have been established for the preparation of 6a-g. In the route-A, 4-ethoxyaniline 2 was reacted with chloroacetyl chloride 3 in a solution of potassium acetate and acetic acid to yield N-(4-ethoxyphenyl)-2-chloroacetamide 4. The latter was reacted with imide compounds 5a-g either in triethanolamine as a green solvent or in solid phase in the presence of TEBAC and KI to yield 6a-g. Alternatively, in the route-B, reaction of anhydrides 7a-g with glycine 8 yielded the (1, 3-dioxo-1, 3-dihydroisoindol-2-yl)acetic acid derivatives 9a-g which on reaction with 2 either in triethnolamine and DCC as a dehydrating agent or in solid phase in the presence of DCC gave 6a-g. The latter were hydrolyzed in 0.5N ethanolic KOH to afford 10a-g.
- Reddy, Yervala D.,Kumar, Padam P.,Devi, Bhoomireddy R.,Dubey, Pramod K.,Kumari, Yalamanchili B.
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- Synthesis and screening of cyclooxygenase inhibitory activity of some 1,3-dioxoisoindoline derivatives
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In this study, 15 compounds bearing N,Nphthaloylacetamide structure designed by the molecular simplification approach based on thalidomide structure were synthesized and evaluated for inhibitory potencies against cyclooxgenase (COX) isoenzymes, namely COX-1 and COX-2. The results suggested that the N,Nphthaloylacetamide structure, as a primary amide, has inhibitory activity against cyclooxygenase isoenzymes with a higher COX-1 selectivity. The conversion of the primary amide to secondary or tertiary derivatives lowered the potency but favored the COX-2 selectivity thus yielding the compounds with stronger COX-2 inhibiting activity. ECV · Editio Cantor Verlag.
- Cizmecioglu, Murat,Pabuccuoglu, Varol,Ballar, Petek,Pabuccuoglu, Aysun,Soyer, Zeynep
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experimental part
p. 186 - 190
(2011/10/10)
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- Method of inhibiting binding of nerve growth factor to p75 NTR receptor
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The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTRcommon neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTRcomprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101and Phe86of nerve growth factor.
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