1420290-84-1Relevant articles and documents
Discovery of niclosamide and its O-alkylamino-tethered derivatives as potent antibacterial agents against carbapenemase-producing and/or colistin resistant Enterobacteriaceae isolates
Xu, Jimin,Pachón-Ibá?ez, María Eugenia,Cebrero-Cangueiro, Tania,Chen, Haiying,Sánchez-Céspedes, Javier,Zhou, Jia
, p. 1399 - 1402 (2019/04/10)
Carbapenemase-producing Enterobacteriaceae (CPE) represents the most worrisome evolution of the antibiotic resistance crisis, which is almost resistant to most of available antibiotics. This situation is getting even worse particularly due to the recent emergence of colistin resistance. Herein, niclosamide, an FDA-approved traditional drug, and its novel O-alkylamino-tethered derivatives were discovered as new and potent antibacterial agents against carbapenemase-producing and/or colistin resistant Enterobacteriaceae isolates. Among these molecules, compound 10 (HJC0431) with 4-aminobutyl moiety showed the broad antibacterial activities, effective against 6 strains. In vitro checkerboard and time-kill course studies demonstrated the synergistic effects of the screened compounds with colistin against the corresponding strains with various degrees.
Discovery of O-alkylamino-tethered niclosamide derivatives as potent and orally bioavailable anticancer agents
Chen, Haijun,Yang, Zhengduo,Ding, Chunyong,Chu, Lili,Zhang, Yusong,Terry, Kristin,Liu, Huiling,Shen, Qiang,Zhou, Jia
supporting information, p. 180 - 185 (2013/03/29)
Niclosamide has been identified to potently inhibit the activation, nuclear translocation, and transactivation of STAT3. Nevertheless, the poor aqueous solubility and bioavailability of niclosamide have hindered its further clinical development for cancer therapy. To discover new molecules with enhanced druglike properties, a series of novel O-alkylamino-tethered derivatives of niclosamide have been designed, synthesized, and biologically evaluated. Among them, compound 11 (HJC0152) has been demonstrated to significantly suppress MDA-MB-231 xenograft tumor growth in vivo (ip and po), indicating its great potential as efficacious and orally bioavailable therapeutics for human cancer.