152594-70-2Relevant academic research and scientific papers
Rational Design of a Near-Infrared Fluorescent Probe Based on a Pyridazinone Scaffold
Zhou, Tongliang,Yang, Lingfei,Liang, Lei,Liu, Hui,Zhu, Yuanjun,Shui, Mengyang,Yuan, Lan,Xu, Fengrong,Niu, Yan,Wang, Chao,Xu, Ping
, p. 3274 - 3281 (2017)
A class of pyridazinone derivatives as near-infrared optical probes in fluorescence microscopy images was designed. The design strategy consisted of the stepwise extension and modification of pyridazinone by expansion of the electron-donating moiety to a larger π-conjugated system and anchoring a subcellular directing group such as triphenylphosphine or morpholine. All the desired products were successfully applied in cell imaging with high subcellular colocalization. Furthermore, these fluorescent probes showed excellent performance in mouse-brain imaging.
Rational Design of Fluorescent Phthalazinone Derivatives for One- and Two-Photon Imaging
Yang, Lingfei,Zhu, Yuanjun,Shui, Mengyang,Zhou, Tongliang,Cai, Yuanbo,Wang, Wei,Xu, Fengrong,Niu, Yan,Wang, Chao,Zhang, Jun-Long,Xu, Ping,Yuan, Lan,Liang, Lei
, p. 12363 - 12370 (2016)
Phthalazinone derivatives were designed as optical probes for one- and two-photon fluorescence microscopy imaging. The design strategy involves stepwise extension and modification of pyridazinone by 1) expansion of pyridazinone to phthalazinone, a larger conjugated system, as the electron acceptor, 2) coupling of electron-donating aromatic groups such as N,N-diethylaminophenyl, thienyl, naphthyl, and quinolyl to the phthalazinone, and 3) anchoring of an alkyl chain to the phthalazinone with various terminal substituents such as triphenylphosphonio, morpholino, triethylammonio, N-methylimidazolio, pyrrolidino, and piperidino. Theoretical calculations were utilized to verify the initial design. The desired fluorescent probes were synthesized by two different routes in considerable yields. Twenty-two phthalazinone derivatives were synthesized and their photophysical properties were measured. Selected compounds were applied in cell imaging, and valuable information was obtained. Furthermore, the designed compounds showed excellent performance in two-photon microscopic imaging of mouse brain slices.
TOLL-LIKE RECEPTOR 8 (TLR8)-SPECIFIC ANTAGONISTS AND METHODS OF MAKING AND USES THEREOF
-
Page/Page column 57, (2019/05/22)
Toll-like receptor 8 (TLR8)-specific inhibitors and methods of using the same in individuals having an autoimmune disease or an inflammatory disorder.
Development of novel proteasome inhibitors based on phthalazinone scaffold
Yang, Lingfei,Wang, Wei,Sun, Qi,Xu, Fengrong,Niu, Yan,Wang, Chao,Liang, Lei,Xu, Ping
, p. 2801 - 2805 (2016/06/08)
In this study we designed a series of proteasome inhibitors using pyridazinone as initial scaffold, and extended the structure with rational design by computer aided drug design (CADD). Two different synthetic routes were explored and the biological evaluation of the phthalazinone derivatives was investigated. Most importantly, electron positive triphenylphosphine group was first introduced in the structure of proteasome inhibitors and potent inhibition was achieved. As 6c was the most potent inhibitor of proteasome, we examined the structure-activity relationship (SAR) of 6c analogs.
