99185-71-4Relevant academic research and scientific papers
FLUORESCENT PROBES FOR DRUG PERMEABILITY IN GRAM NEGATIVE BACTERIA
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Paragraph 0208; 0210, (2020/02/05)
Described are compounds and methods useful in measuring membrane permeability and efflux transporter activity in bacteria, including multidrug resistance Gram negative bacteria.
5 - Fluoro - 2, 4 - disubstituted amino pyrimidine derivative and its preparation and use
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Paragraph 0173; 0174; 0175; 0176, (2019/05/28)
The invention belongs to the field of chemical medicine and particularly relates to a 5-fluorine-2,4-bis-substituted aminopyrimidine derivative and a preparation method and application thereof. The structure of the 5-fluorine-2,4-bis-substituted aminopyri
A method for inhibiting PRMT7 compound and its preparation method and application (by machine translation)
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Paragraph 0026; 0038-0041, (2018/10/04)
The invention belongs to the field of chemical medicine, and in particular relates to a method for inhibiting PRMT7 compound, its formula is as follows: In some embodiments of the compounds proved that, this compound can to PRMT7 produce better inhibitio
Small molecule inhibitors of anthrax lethal factor toxin
Williams, John D.,Khan, Atiyya R.,Cardinale, Steven C.,Butler, Michelle M.,Bowlin, Terry L.,Peet, Norton P.
, p. 419 - 434 (2014/01/17)
This manuscript describes the preparation of new small molecule inhibitors of Bacillus anthracis lethal factor. Our starting point was the symmetrical, bis-quinolinyl compound 1 (NSC 12155). Optimization of one half of this molecule led to new LF inhibitors that were desymmetrized to afford more drug-like compounds.
The divergent transformations of aromatic o-aminonitrile with carbonyl compound
Tang, Jianhong,Li, Jiarong,Zhang, Lijun,Ma, Shuling,Shi, Daxin,Zhang, Qi,Yang, Liupan,Wang, Xiuzhen,Liu, Xuan,Liu, Change
experimental part, p. 533 - 542 (2012/08/27)
A modified Friedlaender conversion of the cyclocondensation of aromatic o-aminonitriles with carbonyl compounds was discovered. Systematic studies reveal that both the new transformation and the classic Friedlaender annulation in the presence of ZnCl2 constitute a pair of divergent reaction, and thecontrolled PDF transformation of this divergent reaction was achieved in the present of bases.
Search for new pharmacophores for antimalarial activity. Part I: Synthesis and antimalarial activity of new 2-methyl-6-ureido-4-quinolinamides
Madapa,Tusi,Sridhar,Kumar,Siddiqi,Srivastava,Rizvi,Tripathi,Puri,Shiva Keshava,Shukla,Batra
scheme or table, p. 203 - 221 (2011/03/19)
A total of 80 new 2-methyl-6-ureido-4-quinolinamides were synthesized and evaluated for their antimalarial activity. Several analogs elicited the antimalarial effect at MIC of 0.25 mg/mL against the chlooquine-sensitive P. falciparum strain. The IC50
A new synthetic approach of N-(4-amino-2-methylquinolin-6-yl)-2-(4- ethylphenoxymethyl)benzamide (JTC-801) and its analogues and their pharmacological evaluation as nociceptin receptor (NOP) antagonists
Sestili, Isabella,Borioni, Anna,Mustazza, Carlo,Rodomonte, Andrea,Turchetto, Luciana,Sbraccia, Maria,Riitano, Daniela,Del Giudice, Maria Rosaria
, p. 1047 - 1057 (2007/10/03)
A series of 4-amino-2-methylquinoline and 4-aminoquinazoline derivatives, including the reference NOP antagonist JTC-801, were synthesized by an alternative pathway and their in vitro pharmacological properties were investigated. 3-Substitution of the qui
Amide derivatives and nociceptin antagonists
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, (2008/06/13)
The present invention relates to a compound of the formula [1′] wherein R2is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1′] as an active ingredient. The compound [1′] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1′] as a nociceptin antagonist or analgesic.
