179334-20-4Relevant academic research and scientific papers
Myricetin derivative containing sulfonyl piperazine as well as preparation method and application thereof
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Paragraph 0029; 0035-0036; 0089; 0095-0096, (2021/01/24)
The invention discloses a myricetin derivative containing sulfonyl piperazine as well as a preparation method and application of the myricetin derivative. The structural general formula of the myricetin derivative is shown in the specification, and n is t
Discovery of Novel Chromone Derivatives Containing a Sulfonamide Moiety as Anti-ToCV Agents through the Tomato Chlorosis Virus Coat Protein-Oriented Screening Method
Jiang, Donghao,Chen, Jixiang,Zan, Ningning,Li, Chunyi,Hu, Deyu,Song, Baoan
, p. 12126 - 12134 (2021/10/26)
A number of novel chromone derivatives containing sulfonamide moieties were designed and synthesized, and the activity of compounds against tomato chlorosis virus (ToCV) was assessed using the ToCVCP-oriented screening method. Comparative molecular field analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA) models were established based on the dissociation constant (Kd) values of the target compounds, and compound 35 was designed and synthesized with the aid of CoMFA and CoMSIA models. The study of affinity interaction indicated that compound 35 exhibited excellent affinity with ToCVCP with a Kd value of 0.11 μM, which was better than that of the positive control agents xiangcaoliusuobingmi (0.44 μM) and ningnanmycin (0.79 μM). In addition, the in vivo inhibitory effect of compound 35 on the ToCVCP gene was evaluated by the quantitative real-time polymerase chain reaction. ToCVCP gene expression levels of the compound 35 treatment group were reduced by 67.2%, which was better than that of the positive control agent ningnanmycin (59.5%). Therefore, compound 35 can be used as a potential anti-ToCV drug in the future.
Novel benzo[ b ]thiophene derivatives as new potential antidepressants with rapid onset of action
Berrade, Luis,Aisa, Bárbara,Ramirez, María J.,Galiano, Silvia,Guccione, Salvatore,Moltzau, Lise Román,Levy, Finn Olav,Nicoletti, Ferdinando,Battaglia, Giuseppe,Molinaro, Gemma,Aldana, Ignacio,Monge, Antonio,Perez-Silanes, Silvia
supporting information; experimental part, p. 3086 - 3090 (2011/07/07)
We report benzo[b]thiophene derivatives synthesized according to a dual strategy. 8j, 9c, and 9e with affinity values toward 5-HT7R and 5-HTT were selected to probe their antidepressant activity in vivo using the forced swimming text (FST). The results showed significant antidepressant activity after chronic treatment. 9c was effective in reducing the immobility time in FST even after acute treatment. These findings identify these compounds as a new class of antidepressants with a rapid onset of action.
IMIDAZOLYL-SUBSTITUTED BENZOPHENONE COMPOUNDS
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Page/Page column 34, (2008/06/13)
The compounds of formula (I) in which X, Y, R1 and R2 have the meanings as given in the description are novel effective inhibitors of the inducible nitric oxide synthase.
IMIDAZOLYL-SUBSTITUTED AZABENZOPHENONE COMPOUNDS
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Page/Page column 39, (2010/11/26)
The compounds of formula (I) in which X, Y, R1 and R2 have the meanings as given in the description are novel effective inhibitors of the inducible nitric oxide synthase.
PYRIMIDINE DERIVATIVES AS MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
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Page/Page column 265, (2008/06/13)
The present invention relates to compounds of Formula (I) as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
Certain substituted 1-aryl-3-piperazin-1′-yl propanones
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, (2008/06/13)
Disclosed are compounds of formula I: wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar1and Ar2independently represent aryl groups; and Y is hydrogen; o
Certain substituted 1-aryl-3-piperazin-1'-yl propanones to treat Alzheimer's Disease
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, (2008/06/13)
Disclosed are compounds of formula I: STR1 or the pharmaceutically acceptable salts thereof wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar1 and Ar2 i
Substituted 1-aryl-3-piperazin-1'-yl propanones
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, (2008/06/13)
Disclosed are compounds of formula I: STR1 wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar1 and Ar2 independently represent aryl groups; and Y is hydr
