56227-55-5Relevant academic research and scientific papers
Design and synthesis of the 4H-chromenone derivatives against psoriasis
Du, Jun Cheng,Han, Xu,Liu, Xin Hua,Yan, Yaoyao,Zhang, Famin,Zhu, Rende
, (2022/02/03)
On basis of Quercetin moiety, two series of 20 new compounds were designed and synthesized accordingly in this study, and their anti-inflammatory activities in vitro and in vivo were evaluated. At last, compound 8A2: 3- (1- (2- (4- (5-bromo-2-chlorobenzoyl) piperazin-1-yl) ethyl)-1H-1,2,3-triazol-4-yl) methoxy)-5,7-dimethoxy-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one with low toxicity was found the best one for inhibiting of NO. Meanwhile, this compound could significantly inhibit the expression of IL-6 (Interleukin-6), TNF-α (Tumor necrosis factor-α) and IL-17 (Interleukin-17), and also significantly down-regulate IL-17 mRNA psoriasis model in vitro. Further studies were performed to establish mouse psoriasis model induced by Imiquimod (IMQ), and the preliminary mechanism indicated that compound 8A2 may alleviate mouse psoriasis through obstructed the JAK1/2-STAT1/3 pathway. This study should be provide a basis for further study of effective treatment of psoriasis.
Diazadispiroalkane derivatives are new viral entry inhibitors
Adfeldt, Rebekka,Schmitz, Janna,Kropff, Barbara,Thomas, Marco,Monakhova, Natalia,H?lper, Julia E.,Klupp, Barbara G.,Mettenleiter, Thomas C.,Makarov, Vadim,Bogner, Elke
supporting information, (2021/03/29)
Herpesviruses are widespread and can cause serious illness. Many currently available antiviral drugs have limited effects, result in rapid development of resistance, and often exhibit dose-dependent toxicity. Especially for human cytomegalovirus (HCMV), new well-tolerated compounds with novel mechanisms of action are urgently needed. In this study, we characterized the antiviral activity of two new diazadispiroalkane derivatives, 11826091 and 11826236. These two small molecules exhibited strong activity against low-passage-number HCMV. Pretreatment of cellfree virus with these compounds greatly reduced infection. Time-of-addition assays where 11826091 or 11826236 was added to cells before infection, before and during infection, or during or after infection demonstrated an inhibitory effect on early steps of infection. Interestingly, 11826236 had an effect by addition to cells after infection. Results from entry assays showed the major effect to be on attachment. Only 11826236 had a minimal effect on penetration comparable to heparin. Further, no effect on virus infection was found for cell lines with a defect in heparan sulfate expression or lacking all surface glycosaminoglycans, indicating that these small molecules bind to heparan sulfate on the cell surface. To test this further, we extended our analyses to pseudorabies virus (PrV), a member of the Alphaherpesvirinae, which is known to use cell surface heparan sulfate for initial attachment via nonessential glycoprotein C (gC). While infection with PrV wild type was strongly impaired by 11826091 or 11826236, as with heparin, a mutant lacking gC was unaffected by either treatment, demonstrating that primary attachment to heparan sulfate via gC is targeted by these small molecules.
INHIBITORS OF PSEUDOMONAS AERUGINOSA VIRULENCE
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Paragraph 0131, (2019/04/16)
Disclosed are piperazine derivative compounds, particularly piperazine derivative compounds having a structure of Formula (I) and methods for preparing these compounds. Also disclosed are use of a therapeutically effective amount of the compound of Formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition therefore for inhibiting quorum sensing of a bacteria.
PYRIMIDYL-DI(DIAZASPIRO-ALKANES) WITH ANTIVIRAL ACTIVITY
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Page/Page column 6, (2017/05/10)
The invention relates to novel pyrimidyl-di(diazaspiro-alkane) derivatives of formula (I) or a pharmaceutically acceptable acid additive salt thereof. The compounds exhibit a wide spectrum of antiviral activity against herpes virus, human immunodeficiency
C-3 NOVEL TRITERPENE WITH C-17 AMINE DERIVATIVES AS HIV INHIBITORS
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Page/Page column 31; 32, (2017/09/15)
The present invention relates to to C-3 novel triterpene with C-17 amine derivatives of formula (I); or pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, prodrugs, compositions or combination thereof, wherein R1, R2, R3, R4, R5 and 'n' are as defined herein. The present invention also relates to pharmaceutical compositions comprising compounds of formula (I) and process for preparing them, and their use for the treatment of viral diseases and particularly HIV mediated diseases.
4, 6-DI (3,12-DIAZA-6, 9-DIAZONIADISPIRO [5.2.5.2] HEXANDECAN-1-YL) -2-METHYL-5-NITROPYRIMIDINE TETRACHLORIDE DIHYDROCHLORIDE HEXAHYDRATE FOR THE TREATMENT OF HERPETIC INFECTION AND A TOPICAL PHARMACEUTICAL COMPOSITION
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Page/Page column 11, (2015/11/23)
?The invention relates to the use of 4, 6-di(3,12-diaza-6,9-diazoniadispiro[5.2.5.2]hexadecan-1-yl)-2-methyl-5-nitropyrimidine tetrachloride dihydrochloride hexahydrate exhibiting activity against herpes virus, for the prevention and treatment of herpetic
Mild and selective Et2Zn-catalyzed reduction of tertiary amides under Hydrosilylation conditions
Kovalenko, Oleksandr O.,Volkov, Alexey,Adolfsson, Hans
supporting information, p. 446 - 449 (2015/03/05)
Diethylzinc (Et2Zn) can be used as an efficient and chemoselective catalyst for the reduction of tertiary amides under mild reaction conditions employing cost-effective polymeric silane (PMHS) as the hydride source. Crucial for the catalytic activity was the addition of a substoichiometric amount of lithium chloride to the reaction mixture. A series of amides containing different additional functional groups were reduced to their corresponding amines, and the products were isolated in good-to-excellent yields.
CDI-mediated monoacylation of symmetrical diamines and selective acylation of primary amines of unsymmetrical diamines
Verma, Sanjeev K.,Ghorpade, Ramarao,Pratap, Ajay,Kaushik
, p. 326 - 329 (2012/04/10)
A highly efficient and green protocol for monoacylation of symmetrical diamines and chemoselective acylation of primary amines of unsymmetrical diamines has been developed.
ANTIVIRAL PYRIMIDINES
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Page/Page column 83, (2010/11/03)
Disclosed herein are novel compounds comprising substituted pyrimidines, pyrazolopyrimtdines, and imidazolopyrimidines, the syntheses thereof, and compositions thereof, including pharmaceutical compositions, comprising the novel pyrimidines, pyrazolopyrimtdines, imidazolpyrimidines and related compounds. Such compounds function to inhibit entry of viruses of the Flaviviridae family, including Hepatitis C virus (HCV), into cells that are susceptible to virus infection. These compounds are useful for the treatment, therapy and/or prophylaxis of viral diseases and infection, including HCV infection.
Bicyclo 4.4.0 antiviral derivatives
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Page/Page column 29, (2008/06/13)
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity
