- TASTE-MODIFYING COMPOUNDS AND USES THEREOF
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The present disclosure generally relates to compounds useful as taste modifiers, particularly as compounds useful for enhancing umami taste, and their use in various comestible products, such as food and beverage products.
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Page/Page column 14; 16
(2021/02/19)
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- α-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment
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The main protease of coronaviruses and the 3C protease of enteroviruses share a similar active-site architecture and a unique requirement for glutamine in the P1 position of the substrate. Because of their unique specificity and essential role in viral po
- Zhang, Linlin,Lin, Daizong,Kusov, Yuri,Nian, Yong,Ma, Qingjun,Wang, Jiang,Von Brunn, Albrecht,Leyssen, Pieter,Lanko, Kristina,Neyts, Johan,De Wilde, Adriaan,Snijder, Eric J.,Liu, Hong,Hilgenfeld, Rolf
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p. 4562 - 4578
(2020/03/05)
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- Structure-activity relationship of clovamide and its related compounds for the inhibition of amyloid β aggregation
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Alzheimer's disease (AD), a neurodegenerative disorder, is characterized by aggregation of amyloid β-protein (Aβ). Aβ aggregates through β-sheet formation and induces cytotoxicity against neuronal cells. Inhibition of Aβ aggregation by naturally occurring compounds is thus a promising strategy for the treatment of AD. We have already reported that caffeoylquinic acids and phenylethanoid glycosides, which possess two or more catechol moieties, strongly inhibited Aβ aggregation. Clovamide (1) containing two catechol moieties, isolated from cacao beans (Theobroma cacao L.), is believed to exhibit preventive effects on Aβ aggregation. To investigate the structure-activity relationship of clovamide (1) for the inhibition of Aβ aggregation, we synthesized 1 and related compounds 2–11 through reaction between L-DOPA, D-DOPA, L-tyrosine, or L-phenylalanine and caffeic acid, p-coumaric acid, or cinnamic acid, and compounds 12 and 13 were derived from 1. Among tested compounds 1–13, those containing one or two catechol moieties exhibited potent anti-aggregation activity, whereas the non-catechol-type related compounds showed little or no activity. This suggests that at least one catechol moiety is essential for inhibition of Aβ42 aggregation, and this activity increases depending on the number of catechol moieties. Consequently, clovamide (1) and its related compounds may be a promising therapeutic option for inhibiting Aβ-mediated pathology in AD.
- Tsunoda, Tatsuhiko,Takase, Mio,Shigemori, Hideyuki
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p. 3202 - 3209
(2018/05/05)
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- Anti-enteroviral 71(EV71) 4-iminooxazolidine-2-ketone compound as well as preparation method and application of anti-enteroviral 71(EV71) 4-iminooxazolidine-2-ketone compound
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The invention discloses a 4-iminooxazolidine-2-ketone enterovirus 71(EV71) 3C protease inhibitor of which the structural general formula is shown as a compound (M), each variable in the structure is defined as the specification, and the compounds are used for effectively inhibiting or stopping the replication of enterovirus 71. The invention relates to discovery and application of a compound with a structure shown as the formula (M) as well as various optical isomers of the compound, a pharmaceutically active metabolite, a medicinal salt, a solvate and a prodrug of the compound in preparation of antiviral drugs for treating hand-foot-mouth virus infection diseases and also relates to an intermediate for preparing the compound with the structure shown as the formula (M) and a synthesis method.
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Paragraph 0096; 0097; 0098
(2018/03/24)
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- Exceptionally small supramolecular hydrogelators based on aromatic-aromatic interactions
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We report herein the use of an aromatic-aromatic interaction to produce small molecule hydrogelators that self-assemble in water and form molecular nanofibers in the resulting hydrogels. Among these hydrogelators, a hydrogelator (6) made from a phenyl-alanine and a cinnamoyl group represents the lowest molecular weight (MW = 295.33 g/mol) peptide-based hydrogelator prepared to date. The supramolecular hydrogels were characterized by transmission electron micrograph (TEM) and fluorescence spec-troscopy, and the results obtained by both techniques correlate well with their rheological properties. Notably, compound 6 can undergo cis/trans-isomerization upon UV irradiation.
- Shi, Junfeng,Gao, Yuan,Yang, Zhimou,Xu, Bing
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supporting information; experimental part
p. 167 - 172
(2011/05/19)
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- Preparation and synthetic applications of N-(α,β-unsaturated acyl)-α-amino acid derivatives
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N-(α,β-Unsaturated acyl)-α-amino acids, amides and esters are structural motifs of many biologically active natural products. An alternate and advantageous approach for the synthesis of N-(α,β-unsaturated acyl)-α-amino acid derivatives is developed via ac
- Katritzky, Alan R.,Gyanda, Reena,Meher, Nabin K.,Song, Yuming
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experimental part
p. 1249 - 1259
(2010/10/03)
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- Design and synthesis of α,β-unsaturated carbonyl compounds as potential ACE inhibitors
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The α,β-unsaturated amide that is incorporated into the basic structural frame of a simple substrate molecule of angiotensin converting enzyme was found to serve as a Michael acceptor for the catalytic carboxylate of Glu-127, inhibiting the enzyme irreversibly. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
- Choo, Hea-Young Park,Peak, Kyung-Hee,Park, Jongsei,Kim, Dong Hyun,Chung, Hak Soon
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p. 643 - 648
(2007/10/03)
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- Pharmaceutical composition having an excellent absorption property
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A compound represented by the formula: STR1 wherein R1 is a hydrogen atom, a fluorine atom, a nitro group, a hydroxyl group or a hydroxyl group protected by an esterifying group; X is CO or SO2 ; --Y-- is a straight bond, a lower alkylene group, a substituted or unsubstituted vinylene group, or group having the formula --CH2 --O-- or --O--CH2 --; R2 is a substituted or unsubstituted phenyl or naphthyl group, or R2 --Y--CO is N-benzyloxycarbonylphenylalanyl, N-benzyloxycarbonyl-4-fluorophenylalanyl or N-(m-methoxycinnamoyl)-phenylalanyl group; or a non-toxic salt thereof is disclosed along with pharmaceutical compositions containing these compounds and methods of using these compositions to increase the rate of absorption of medicines.
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