125163-12-4Relevant articles and documents
NOVEL NUCLEOSIDE PHOSPHORAMIDATE COMPOUND AND USE THEREOF
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Paragraph 0147, (2015/11/24)
The present invention provides a novel nucleoside phosphoramidate compound, or a stereoisomer, salt, hydrate, solvate or crystal thereof for the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The present invention also provides the pharmaceutical composition comprising a compound of the present invention, or a stereoisomer, salt, hydrate, solvate or crystal thereof and a use of the compound or the composition of the present invention in the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The compound of the present invention has a good anti-HCV effect.
HEPATITIS C VIRUS INHIBITORS
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, (2016/01/21)
Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Benzofurazan derivatives as antifungal agents against phytopathogenic fungi
Wang, Lili,Zhang, Ying-Ying,Wang, Lei,Liu, Feng-You,Cao, Ling-Ling,Yang, Jing,Qiao, Chunhua,Ye, Yonghao
, p. 535 - 542 (2014/06/09)
A series of benzofurazan derivatives were prepared and evaluated for their biological activities against four important phytopathogenic fungi, namely, Rhizoctonia solani, Sclerotinia sclerotiorum, Fusarium graminearum and Phytophthora capsici, using the mycelium growth inhibition method. The structures of these compounds were characterized by1H NMR,13C NMR, and HRMS. N-(3-chloro-4-fluorophenyl)-7-nitrobenzo[c][1,2,5] oxadiazol-4-amine (A3) displayed the maximum antifungal activity against R. solani (IC50= 1.91 μg/mL), which is close to that of the positive control Carbendazim (IC50= 1.42 μg/mL). For other benzofurazan derivatives with nitro group at R4position (A series), 9 out of 30 compounds exhibited high antifungal effect against strain R. solani, with IC50values less than 5 μg/mL. Most of the derivatives with substituents at R2and R3positions (B series) displayed moderate growth inhibition against S. sclerotiorum (IC504position and another conjugated aromatic ring at the R1position of the phenyl ring displayed high antifungal capability against strain R. solani. Compounds with substituents at R2and R3position had moderate efficacy against strain S. sclerotiorum.
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa
Reck, Folkert,Ehmann, David E.,Dougherty, Thomas J.,Newman, Joseph V.,Hopkins, Sussie,Stone, Gregory,Agrawal, Nikunj,Ciaccio, Paul,McNulty, John,Barthlow, Herbert,O'Donnell, Jennifer,Goteti, Kosalaram,Breen, John,Comita-Prevoir, Janelle,Cornebise, Mark,Cronin, Mark,Eyermann, Charles J.,Geng, Bolin,Carr, Greg R.,Pandarinathan, Lakshmipathi,Tang, Xuejun,Cottone, Andrew,Zhao, Liang,Bezdenejnih-Snyder, Natascha
, p. 5392 - 5409 (2014/12/10)
Type II bacterial topoisomerases are well validated targets for antimicrobial chemotherapy. Novel bacterial type II topoisomerase inhibitors (NBTIs) of these targets are of interest for the development of new antibacterial agents that are not impacted by
Chemo-enzymatic synthesis and biological evaluation of 5,6-disubstituted benzimidazole ribo- and 2′-deoxyribonucleosides
Konstantinova, Irina D.,Selezneva, Olga M.,Fateev, Ilja V.,Balashova, Tamara A.,Kotovskaya, Svetlana K.,Baskakova, Zoya M.,Charushin, Valery N.,Baranovsky, Alexander V.,Miroshnikov, Anatoly I.,Balzarini, Jan,Mikhailopulo, Igor A.
, p. 272 - 280 (2013/02/25)
A number of new 5,6-disubstituted benzimidazoles have been prepared and their substrate properties for recombinant E. coli purine nucleoside phosphorylase (PNP; the product of the deoD gene) in the transglycosylation reaction were investigated. The heterocyclic bases showed good substrate activity for PNP and the ribo- and 2-deoxyribonucleosides were synthesized. The predominant (OMe and OEt) or exclusive (Oi-Pr, morpholino, and N-methylpiperazino) formation of the 5-substituted 6-fluoro-1-(β-d- ribofuranosyl)benzimidazoles was observed. The formation of the regioisomeric 6- methoxy-, 6-ethoxy-, or 6-isopropoxy-substituted 1-(2-deoxy-β-d- ribofuranosyl)-5-fluorobenzimidazoles was observed in the trans-2- deoxyribosylation reaction of the corresponding bases. The predominant or exclusive formation of the regioisomeric N1-nucleosides with bulky 5-substituents of 6-fluorobenzimidazole points to a large hydrophobic pocket in the E. coli PNP active site that can accommodate these groups. The biological activity of the synthesized nucleosides was studied and revealed no inhibitory activity against a broad variety of DNA and RNA viruses. The compounds also lacked significant cytotoxicity. Georg Thieme Verlag Stuttgart New York.
PYRROLO[1,2-A]QUINOXALIN-5-(4H)-YL)SULFONYLS AND CARBONYLS AND THEIR USE AS ESTROGENIC AGENTS
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Page/Page column 64, (2008/06/13)
This invention provides estrogen receptor modulators having the structure: wherein R1 to R7, R9 and R10 X, Y, and Z are as defined in the specification; or a pharmaceutically acceptable salt thereof.