69813-89-4Relevant academic research and scientific papers
Design, synthesis and evaluation of a series of 5-methoxy-2,3-naphthalimide derivatives as AcrB inhibitors for the reversal of bacterial resistance
Jin, Chaobin,Alenazy, Rawaf,Wang, Yinhu,Mowla, Rumana,Qin, Yinhui,Tan, Jin Quan Eugene,Modi, Natansh Deepak,Gu, Xinjie,Polyak, Steven W.,Venter, Henrietta,Ma, Shutao
, p. 882 - 889 (2019)
A series of novel 5-methoxy-2,3-naphthalimide derivatives were designed, synthesized and evaluated for their biological activities. In particular, the ability of the compounds to synergize with antimicrobials, to inhibit Nile Red efflux, and to target AcrB was assayed. The results showed that the most of the tested compounds more sensitized the Escherichia coli BW25113 to the antibiotics than the parent compounds 7c and 15, which were able to inhibit Nile Red efflux. Significantly, compound A5 possessed the most potent antibacterial synergizing activity in combination with levofloxacin by 4 times and 16 times at the concentration of 8 and 16 μg/mL, respectively, whilst A5 could effectively abolish Nile Red efflux at 100 μM. Additionally, target effect of A5 was confirmed in the outer- or inner membrane permeabilization assays. Therefore, A5 is an excellent lead compound for further structural optimization.
2. 3 - Naphthalenedicarboxylic acid imide derivative and its preparation method and application (by machine translation)
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Paragraph 0103; 0105, (2019/01/05)
The invention provides a compound of formula I illustrated compound or isomer thereof or solvates or salts and its preparation method and application, the compounds of the HAUGLAND gram negative bacteria over-expression AcrB has better antibacterial synergistic activity and efflux inhibitory activity. (by machine translation)
On the total synthesis and determination of the absolute configuration of rishirilide B: Exploitation of subtle effects to control the sense of cycloaddition of o-quinodimethides
Yamamoto, Kana,Hentemann, Martin F.,Allen, John G.,Danishefsky, Samuel J.
, p. 3242 - 3252 (2007/10/03)
The total synthesis of racemic rishirilide B has been accomplished. The synthesis serves to define the relative relationships of its stereogenic centers. Also, starting with readily available chiral pool, ent-rishirilide B was synthesized, thereby demonst
Photothermal Side-Chain Bromination of Methyl-, Dimethyl-, and Trimethylbenzenes with N-Bromosuccinimide
Mataka, Shuntaro,Liu, Guo-Bin,Sawada, Tsuyoshi,Kurisu, Masayoshi,Tashiro, Masashi
, p. 1113 - 1119 (2007/10/02)
Tri- and dibromination of methyl-, dimethyl-, and trimethylbenzenes with N-bromosuccinimide were accomplished by photothermal reaction with a tungsten lamp in carbon tetrachloride or benzene. (Dibromomethyl)arenes and (tribromomethyl) derivatives were produced depending upon a solvent used and a substituent on the benzene ring.In the bromination of methylbenzenes without a substituent on the ortho-position, (tribromomethyl)benzenes were formed.On the other hand, ortho-substituted methylbenzenes gave (dibromomethyl)benzenes. α,β-Dibromo-1,2-diarylstilbenes were formed via the debrominative carbon-carbon coupling reaction of ...
THE SELECTIVE BENZYLIC BROMINATION OF o-XYLENES. A USEFUL SYNTHESIS OF PHTHALIDES
Box, Vernon, G. S.,Yiannikouros, George P.
, p. 1261 - 1270 (2007/10/02)
The free radical bromination of aryl methyl groups can be controlled by the strategic positioning of a remote stereo-electronic blocking group on the aryl ring.This tactic leads to the efficient synthesis of selectively benzylically brominated molecules which are useful synthetic intermediates.This methodology has been applied to the synthesis of some phthalides.
