1179804-57-9Relevant academic research and scientific papers
Design and structural optimization of novel 2H-benzo[h]chromene derivatives that target AcrB and reverse bacterial multidrug resistance
Wang, Yinhu,Alenazy, Rawaf,Gu, Xinjie,Polyak, Steven W.,Zhang, Panpan,Sykes, Matthew J.,Zhang, Na,Venter, Henrietta,Ma, Shutao
, (2021)
Drug efflux pumps have emerged as a new drug targets for the treatment of bacterial infections in view of its critical role in promoting multidrug resistance. Herein, novel chromanone and 2H-benzo[h]chromene derivatives were designed by means of integrated molecular design and structure-based pharmacophore modeling in an attempt to identify improved efflux pump inhibitors that target Escherichia coli AcrB. The compounds were tested for their efflux inhibitory activity, ability to inhibit efflux, and the effect on bacterial outer and inner membranes. Twenty-three novel structures were identified that synergized with antibacterials tested, inhibited Nile Red efflux, and acted specifically on the AcrB. Among them, WK2, WL7 and WL10 exhibiting broad-spectrum and high-efficiency efflux inhibitory activity were identified as potential ideal AcrB inhibitors. Molecular modeling further revealed that the strong π-π stacking interactions and hydrogen bond networks were the major contributors to tight binding of AcrB.
Design, synthesis, and biological evaluation of 2-(5-methyl-1H-pyrazol-1-yl) acetamide derivatives as androgen receptor antagonists
Dong, Junze,Zhang, Jingya,Li, Zilu,Asnake, Solomon,Zhang, Daoguang,Olsson, Per-Erik,Zhao, Guisen
, p. 380 - 386 (2019)
Androgen receptor (AR) signaling is often activated in prostate cancer (PCa) cells, and blockage of this signaling by AR antagonists is an important strategy in PCa therapy. In this study, we designed and synthesized a series of 2-(5-methyl-1H-pyrazol-1-y
1,3-disubstituted pyrazole derivative as well as preparation method and application thereof
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Paragraph 0078; 0079; 0080; 0081; 0087, (2018/03/24)
The invention discloses a 1,3-disubstituted pyrazole derivative as well as a preparation method and application thereof. The compound has a structure shown as a general formula (I). The invention further provides a preparation method of the compounds and
Substituted imidazoline-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof
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Page/Page column 80-81, (2011/05/16)
The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
