21092-94-4Relevant academic research and scientific papers
RAPAFUCIN DERIVATIVE COMPOUNDS AND METHODS OF USE THEREOF
-
Paragraph 0480-0481, (2021/04/02)
The present disclosure provides macrocyclic compounds inspired by the immunophilin ligand family of natural products FK506 and rapamycin. The generation of a Rapafucin library of macrocyles that contain FK506 and rapamycin binding domains should have grea
3,4-dihydroxyacetophenone derivative, preparation method, application and pharmaceutical composition thereof
-
Paragraph 0063; 0075-0080, (2019/02/04)
The invention discloses a 3,4-dihydroxyacetophenone derivative, a preparation method, an application and a pharmaceutical composition. The 3,4-dihydroxyacetophenone derivative comprises a 3,4-resacetophenone fatty acid derivative (I), a 3,4-resacetophenon
Method for synthesizing houttuynine hybridized flavone Houttuynoid A
-
Paragraph 0042; 0043, (2018/05/30)
The invention discloses a method for synthesizing houttuynine hybridized flavone Houttuynoid A. The method mainly comprises the following steps: by taking 3,4-dihydroxy benzaldehyde as an initiator raw material, firstly, selectively protecting four-position hydroxyl, performing an iodination reaction so as to obtain an o-iodophenol structure; further protecting aldehyde by using 1,3-propylene glycol, performing a Michael addition reaction with methyl-2-undecynoate so as to obtain an intermittent, and further performing an intracellular Heck reaction on the intermittent so as to obtain a key intermittent 2,3-di-substituted benzofuran structure; deprotecting the aldehyde of the benzofuran structure, performing a Claisen-Schmidt reaction with trihydroxyacetophenone monohydrate so as to obtaina chalcone structure, further performing iodine-catalyzed ring closure and DMDO (Dimethyldioxirane) oxidation so as to obtain a flavonol structure, furthermore removing a protection group, further reacting with bromo-peracetylated galactose so as to obtain glucoside, finally removing all protection groups, and performing reduction, thereby obtaining a target compound, namely the houttuynine hybridized flavone Houttuynoid A. Related derivatives are synthesized through intermittents of synthesis routs. The method is simple and controllable in reaction and high in yield.
Derivate of houttuyfonate hybrid flavone Houttuynoid A, as well as preparation method and application thereof
-
Paragraph 0061; 0062, (2018/06/26)
The invention discloses a derivate of houttuyfonate hybrid flavone Houttuynoid A, as well as a preparation method and application thereof. The derivate of houttuyfonate hybrid flavone Houttuynoid A, disclosed by the invention, has the activity of resisting herpes simplex I type virus, an in vitro herpes simplex virus resistant activity screening system is used for carrying out activity evaluation,it is found that the houttuyfonate hybrid flavone can inhibit herpes simplex viruses more effectively, it is indicated that the houttuyfonate hybrid flavone has the effects of preventing and curing herpes simplex virus infection, the derivate can be applied in the preparation of herpes simplex virus resistant medicines, and the derivate has good research and development prospects.
NOVEL RENIN INHIBITOR
-
Paragraph 0348; 0349; 0350, (2015/09/22)
The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I] which is useful as a renin inhibitor. wherein R1 is a cycloalkyl group or an alkyl, R22 is an optionally substituted aryl and the like, R is a lower alkyl group, R3, R4, R5 and R6 are the same or different, and are a hydrogen atom, an optionally substituted carbamoyl, an optionally substituted alkyl, or alkoxycarbonyl, or a pharmaceutically acceptable salt thereof.
NITROGEN-CONTAINING SATURATED HETEROCYCLIC COMPOUND
-
Paragraph 0128, (2014/02/15)
The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is -O- and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
C-3' protected monomeric nucleotides and synthesis of oligonucleotides on solid support
-
, (2008/06/13)
Immobilized nucleotide primers of this invention include a modified nucleotide tethered to a support substrate through a linking group. In particular, the modified nucleotide is constructed such that the C-5′ end of the nucleotide is tetherable to the lin
Carboxy-substituted cinnamides: A novel series of potent, orally active LTB4 receptor antagonists
Greenspan, Paul D.,Fujimoto, Roger A.,Marshall, Paul J.,Raychaudhuri, Anil,Lipson, Kenneth E.,Zhou, Huanghai,Doti, Robert A.,Coppa, David E.,Zhu, Lijuan,Pelletier, Roberta,Uziel-Fusi, Susan,Jackson, Robert H.,Chin, Michael H.,Kotyuk, Bernard L.,Fitt, John J.
, p. 164 - 172 (2007/10/03)
A series of carboxy-substituted cinnamides were investigated as antagonists of the human cell surface leukotriene B4 (LTB4) receptor. Binding was determined through measurement of [3H]-LTB4 displacement from hum
Cleavage of the Methylenedioxy Ring. III. Cleavage with Sodium Benzyloxide in Dimethyl Sulfoxide
Kobayashi, Shigeru,Okimoto, Kazuto,Imakura, Yasuhiro
, p. 1567 - 1573 (2007/10/02)
Cleavage of the methylenedioxy ring in aromatic formyl (1-3), nitro (4 and 5), and acetyl (30) compounds with N-sodium benzyloxide-benzyl alcohol in dimethyl sulfoxide gave 3-hydroxybenzene derivatives (19, 22-24, 26, 27, and 33).In the case of the acetyl compound 30, the 4-hydroxybenzene derivative (34) was also obtained as a minor product.Regioselective cleavage of the ring in aromatic compounds having electronwithdrawing groups with nucleophilic oxide anions is discussed.Cleavage of the ring in 1-5 and 30 with 2 N sodium methoxide in dimethyl sulfoxide-dimethylformamide was found to be useful for the practical preparation of 3-hydroxybenzene derivatives (6-10 and 31).Keywords - Cleavage of methylenedioxy ring; regioselectivity; piperonals; 3,4-methylenedioxy-nitrobenzene; 3,4-methylenedioxy-acetophenone; sodium methoxide; sodium phenoxide; sodium benzyloxide; dimethyl sulfoxide; dimethylformamide
