1552-17-6Relevant academic research and scientific papers
PqsR INVERSE AGONISTS
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Page/Page column 81; 82, (2020/01/31)
The present invention relates to a compound according to general formula (I), which acts as an inhibitor of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS)); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.
5 - [...] -2 alkyl substituted [...] and imidazole compound and use thereof
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Paragraph 0073-0075, (2018/05/07)
The present invention discloses a 5-aryl phenol-2 alkyl substituted urea benzimidazole compound and applications thereof, wherein the compound has a structure represented by a formula (I). According to the present invention, the 5-aryl phenol-2 alkyl subs
Ultrasound synthesis of diaryl ethers
Begunov,Valyaeva,Belyaev,Dobretsova
, p. 1971 - 1974 (2016/05/11)
2,2-Bis[4-(4-nitroaryl)phenyl]hexafluoropropanes appropriate for the synthesis of monomers were prepared by the reaction of 2,2-bis[4-hydroxyphenyl)hexafluoropropane with 1-chloro-4-nitrobenzenes under ultrasonic activation.
New benzimidazole-2-urea derivates as tubulin inhibitors
Wang, Wenna,Kong, Dexin,Cheng, Huimin,Tan, Li,Zhang, Zhang,Zhuang, Xiaoxi,Long, Huoyou,Zhou, Yang,Xu, Yong,Yang, Xiaohong,Ding, Ke
, p. 4250 - 4253 (2014/09/29)
Emerging drug resistance and other drawbacks limit tubulin inhibitors' therapeutic applications and developing novel tubulin inhibitors still attracts intensive efforts. We describe the discovery and structure-activity relationship study of a series of benzimidazole-2-urea derivatives as novel β tubulin inhibitors. The representative compound 6o potently suppressed the proliferation of a panel of human cancer cells (NCI-H460, Colo205, K562, A431, HepG2, Hela, MDA-MB-435S) with IC50 values of 0.040, 0.050, 0.006, 0.026, 1.774, 0.452 and 0.052 μM, respectively. Compound 6o obviously inhibited NCI-H460 spindles formation and induced cell cycle arrest at G2/M phase at 0.10 μM. Computational study suggested that 6o interacts with β tubulin in a novel binding mode. Our results suggested that benzimidazole-2-urea derivatives might be promising tubulin inhibitors with novel binding mode for further development.
Synthesis of 5-substituted and 5.6-disubstituted-2-phenoxymethyl benzimidazoles
Rane,Athlekar,Patil,Bobade,Chowdhary
experimental part, p. 345 - 348 (2012/01/03)
5-Substituted and 5,6-disubstituted-2-phenoxymethyl benzimidazoles [Via to VI-I] were synthesized from 5-substituted and 4,5-disubstituted ortho phenylene diamines (OPD) [IV] with simple or substituted phenoxyacetic acids [V] in 4N HCl. Synthesized compou
BENZIMIDAZOLE QUINOLINONES AND USES THEREOF
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Page 264, (2008/06/13)
Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
A convenient copper-catalyzed direct animation of nitroarenes with 9-alkylhydroxylamines
Seko, Shinzo,Miyake, Kunihito,Kavvamura, Norio
, p. 1437 - 1444 (2007/10/03)
O-Alkylhydroxylamines, particularly O-methylhydroxylamine, aminate nitroarenes in the presence of a strong base and a copper catalyst to give aminonitroarenes in good yields, ortho- or para-Animation with respect to the nitro group takes place, and in some cases the ortho-aminated product is preferentially obtained. With 3-substituted nitrobenzenes where the substituent has a lone pair of electrons, preferential amination occurs at the 2-position to give the sterically most congested 3c-f, 14 and 22g.
Benzimidazole, benzoxazole and benzothiazole compounds
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, (2008/06/13)
A compound of formula (I): STR1 in which: R1 represents halogen or hydroxyl, alkoxy, trihalomethyl, amino, mercapto, alkylthio, trialkylammonium, aryloxy, arylthio, arylsulfonyl, arylsulfonyloxy, cycloalkyloxy, cycloalkylthio, bicycloalkyloxy or bicycloalkylthio, Ra and Rb, which may be identical or different, represent hydrogen or alkyl, X represents oxygen or sulfur or NR, Y represents the group as defined in the description, R2 represents an optionallly substituted aryl, its optical isomers as well as its addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as interleukin-1β inhibitor.
Synthesis and spectral properties of methyl 5-[(o-, m-, and p-r)- phenoxy]-2-benzimidazolecarbamate
Cortes,Anaya
, p. 745 - 748 (2007/10/03)
The preparation of eleven novel methyl 5-[(o-, m-, p-R)-phenoxy-2- benzimidazolecarbamates with possible pharmacological activity as anthelmintics is described. The structure of all products was corroborated by it, 1H-nmr, 13C-nmr and mass spectra.
