Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: Pharmacophore identification based on the screening hit closantel
摘要:
This SAR study has shown that the salicylanilide is the pharmacophore for inhibition of the bacteria! two-component system. Hydrophobic substituents improve the potency of inhibitors in this series; however, hydrophobicity is not the sole determinant for inhibition; structural and electronic requirements also exist. Closantel (1) was found to inhibit a two-component system and to have antibacterial activity against drug resistant S. aureus and E. faecium, (C) 1998 Elsevier Science Ltd. All rights reserved.
One-pot synthesis of gem-difluorostyrenes from benzyl bromide via olefination of phosphonium ylide with difluorocarbene
作者:Xiao-Yun Deng、Jin-Hong Lin、Ji-Chang Xiao
DOI:10.1016/j.jfluchem.2015.06.009
日期:2015.11
A new approach for the synthesis of gem-difluorostyrenes from benzyl bromide is described. Quaternization of triphenylphosphine with benzyl bromide to give phosphonium salts, deprotonation of the corresponding phosphonium salts to produce phosphonium ylide, and the subsequent olefination of phosphonium ylide with difluorocarbene generated from difluoromethylene phosphobetaine (Ph3P+CF2CO2−) by decarboxylation
描述了一种由苄基溴合成宝石-二氟苯乙烯的新方法。的三苯基膦与苄基溴,得到鏻盐,相应的鏻盐,以产生磷叶立德,并与二氟卡宾从二氟亚甲基磷酸酯生成鏻内鎓盐的后续烯的脱质子化(PH季铵化3 P + CF 2 CO 2 -可以发生通过脱羧)在一个锅中平稳地进行,以高收率提供最终的宝石-二氟苯乙烯。
Anti-proliferative evaluation of monoterpene derivatives against leukemia
The cure rate of pediatric acute lymphoblastic leukemia (ALL) has significantly improved in the past thirty years, however not all patient cohorts respond well to current chemotherapy regimens. Among the high risk patient cohort is infants with MLL-rearranged (MLL-r) B-ALL, which remains dismal with an overall survival rate <35%. Our program is interested in identifying new molecular scaffolds to better understand the underlying mechanisms and ultimately provide new targeted treatments. Based on a phenotypic screen, phenolic natural products were identified as promising scaffolds for further chemical evaluation. Herein we disclose the effects of a potent anti-proliferative compound 31 against human ALL leukemia cellular models. (C) 2016 Elsevier Masson SAS. All rights reserved.
Ricciardi, Fiore J.; Doukas, Peter H., Heterocycles, 1986, vol. 24, # 4, p. 971 - 977