Beilstein Journal of Organic Chemistry p. 1700 - 1704 (2012)
Update date:2022-09-26
Topics:
Dittrich, Torsten
Hanekop, Nils
Infed, Nacera
Schmitt, Lutz
Braun, Manfred
The inhibition of ABC (ATP binding cassette) transporters is considered a powerful tool to reverse multidrug resistance. Zosuquidar featuring a difluorocyclopropyl-annulated dibenzosuberyl moiety has been found to be an inhibitor of the P-glycoprotein, one of the best-studied multidrug efflux pumps. Twelve 5-oxyisoquinoline derivatives, which are analogues of zosuquidar wherein the dibenzosuberyl-piperazine moiety is replaced by either a diarylaminopiperidine or a piperidone-derived acetal or thioacetal group, have been synthesized as pure enantiomers. Their inhibitory power has been evaluated for the bacterial multidrugresistance ABC transporter LmrCD and fungal Pdr5. Four of the newly synthesized compounds reduced the transport activity to a higher degree than zosuquidar, being up to fourfold more efficient than the lead compound in the case of LmrCD and about two times better for Pdr5.
View MoreNIGNXIA XINDACHANG TECHNOLOGY CO.,LTD
website:https://xdcchemical.com/
Contact:86-311-85758226
Address:North Industry Area, Wuji
Shaanxi King Stone Enterprise Company Limited
Contact:86-29-88353805,13609285751
Address:.209 Keji Road Hi-Tech industrial Develpment Zone .Xian China
Shandong Yuanli Science and Technology Co., Ltd.
Contact:86-0536-6777557
Address:Zhuliu Industiral Park,Changle County
KangZhiYuan Pharmaceutical Company Limited
Contact:(Sabrina)86-20-85273232
Address:4th floor, building B, Dadi industry zone, Tangxia, Tianhe, Guangzhou, China
Zibo Ocean International Trade Co.,Ltd
Contact:+86 533 5160706
Address:1117, Hongtai Bld., Songling rd, Zichuan,Zibo,Shandong,China
Doi:10.1016/j.ejmech.2012.10.011
(2012)Doi:10.1021/ol303213r
(2013)Doi:10.1039/c2ob26974k
(2013)Doi:10.1021/ja00039a021
(1992)Doi:10.1055/s-0032-1317159
(2012)Doi:10.3762/bjoc.14.163
(2018)