95639-99-9Relevant academic research and scientific papers
Structural optimization of natural product nordihydroguaretic acid to discover novel analogues as AcrB inhibitors
Alenzy, Rawaf,Liu, Xingbang,Ma, Shutao,Ma, Yingang,Mowla, Rumana,Polyak, Steven W.,Song, Di,Teng, Yuetai,Venter, Henrietta,Wang, Yinhu
, (2019/12/24)
Drug efflux pumps confer multidrug resistance to dangerous bacterial pathogens which makes these proteins promising drug targets. Herein, we present initial chemical optimization and structure-activity relationship (SAR) data around a previously described efflux pump inhibitor, nordihydroguaretic acid (NDGA). Four series of novel NDGA analogues that target Escherichia coli AcrB were designed, synthesized and evaluated for their ability to potentiate the activity of antibiotics, to inhibit AcrB-mediated substrate efflux and reduce off-target activity. Nine novel structures were identified that increased the efficacy of a panel of antibiotics, inhibited drug efflux and reduced permeabilization of the bacterial outer and inner membranes. Among them, WA7, WB11 and WD6 possessing broad-spectrum antimicrobial sensitization activity were identified as NDGA analogues with favorable properties as potential AcrB inhibitors, demonstrating moderate improvement in potency as compared to NDGA. In particular, WD6 was the most broadly active analogue improving the activity of all four classes of antibacterials tested.
In vitro antioxidant and cytotoxic activity of some synthetic riparin-derived compounds
Nunes, Geandra B.L.,Policarpo, Paola R.,Costa, Luciana M.,Silva, Teresinha G. Da,Militao, Gardenia Carmen G.,Camara, Celso A.,Filho, Jose Maria Barbosa,Gutierrez, Stanley Juan C.,Islam, Mohammed T.,De Freitas, Rivelilson M.
, p. 4595 - 4607 (2014/05/20)
This study aimed to study the in vitro antioxidant activity and cytotoxicity on tumor cells lines of six synthetic substances derived from riparins. All the substances showed antioxidant activity and riparins C, D, E, F presented cell growth inhibition rates greater than 70%, suggesting that these molecules have antitumor properties. These substances also caused greater than 80% releases of cytoplasmic lactate dehydrogenase enzyme (LDH). Although the antioxidant and antitumor properties presented herein require further assessment, the outcomes indicate that these novel riparins are promising biologically active compounds.
A simple one-pot synthesis of benzoxazine-2,4-diones and benzothiazine-2,4-diones
Zhu, Xiaoxiang,Yu, Qian-sheng,Greig, Nigel H.,Flippen-Anderson, Judith L.,Brossi, Arnold
, p. 115 - 128 (2007/10/03)
A simple and efficient procedure has been developed for a one-pot synthesis of substituted benzoxazine-2,4-diones and benzothiazine-2,4-diones directly from salicylic acid (or thiosalicylic acid) and amines.
