- Butylphthalide derivative and application thereof in preparation of drugs for protecting nerve cells
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The invention relates to biological medicine. The invention provides a butylphthalide derivative and an application thereof in preparation of drugs for protecting nerve cells, and more specifically, the invention provides application of a butylphthalide d
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Paragraph 0049
(2021/08/25)
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- Preparation of 2-phenyl-3-hydroxyquinoline-4(1H)-one-5-carboxamides as potential anticancer and fluorescence agents
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The synthesis of 3-hydroxyquinoline-4(1H)-one derivatives bearing substituted phenyl in position 2 and variously substituted carboxamide group in position 5 is described, with use of 3-nitrophthalic anhydride, α-haloketones and primary amines as the starting materials. The synthetic approach was inspired by the preparation of analogous derivatives reported previously. However, a different strategy had to be developed with the corresponding bis(phenacyl)-3-aminophthalates as the key intermediates. Synthesized hydroxyquinolinones, as well as their intermediates, were tested for their cytotoxic activity towards various cancer and non-malignant cell lines. The fluorescent properties of these compounds have also been evaluated. In both fields, interesting data were obtained and compared to isomeric compounds that have been studied in the past.
- Funk, Petr,Motyka, Kamil,D?ubák, Petr,Znojek, Pawel,Gurská, Soňa,Kusz, Joachim,McMaster, Claire,Hajdúch, Marián,Soural, Miroslav
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p. 48861 - 48867
(2015/06/16)
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- Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use
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Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page/Page column 22; 63
(2010/02/11)
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- Condensed pyridazinyl guanidines, their production and use
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Pyridazinyl guanidines of the formula: wherein ring A is a benzene ring or a nitrogen-containing 6-membered aromatic ring, each of which may be substituted; and R1is an aromatic ring group which may be substituted, or a salt thereof, which have activity for inhibiting Na-H exchange and are useful as a prophylactic/therapeutic agent for ischemic cardiovascular diseases such as myocardial infarction and arrythmia.
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- Utility of Complementary Molecular Reactivity and Molecular Recognition (CMR/R) Technology and Polymer-Supported Reagents in the Solution-Phase Synthesis of Heterocyclic Carboxamides
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The use of our recently reported chemical library purification strategy in the development of a herbicidal lead, N-(3-benzoylphenyl)-3-(1,1-dimethylethyl)-1-methyl-1H-pyrazole-5-carboxamide (3), is described. The approach applying fundamental properties of complementary molecular reactivity and molecular recognition (CMR/R) as the basis for a general purification strategy was utilized. Polymeric reagents were used in the synthesis to generate reactive species involved in product formation, and complementary molecular reactivity/molecular recognition polymer 8 (CMR/R polymer 8) was used in the solution-phase syntheses of building blocks, primary libraries, and lead refinement libraries. An extension of the CMR/R methodology was applied, utilizing a sequestration enabling reagent (SER), transforming a reactant into an electrophilic species sequestrable by CMR/R polymer 8. This library purification strategy enabled rapid lead generation and lead refinement to afford herbicide 27o. The CMR/R solid-phase purification technique enabled a simple, general, and powerful protocol, eliminating the usual tedious and time-consuming methods required for solution-phase product purification. The result was the synthesis of hundreds of compounds, prepared in a relatively short time, leading to a compound with a 4-fold improvement in herbicidal activity over the initial lead.
- Parlow, John J.,Mischke, Deborah A.,Woodard, Scott S.
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p. 5908 - 5919
(2007/10/03)
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- Aspects of Tautomerism: Part X - Neighbouring Group Effects on the Structure and Reactivity Patterns of Acid Chlorides
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The influence of neighbouring groups on the structure and reactivity patterns of over one hundred acid chlorides derived from γ- and δ-keto acids, 1,2- and 1,3-dicarboxylic acid half-esters and diacid chlorides have been examined.Contrary to reports in the literature, text books and monographs, evidence has been obtained for the non-existence of tautomerism between the isomeric pairs of either acid chlorides or half-ester acid chlorides.ce.
- Bhatt, M. Vivekananda,El Ashry, Shaker H.,Somayaji, Vishwanatha
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p. 473 - 486
(2007/10/02)
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