Jiang, Cheng-Shi; Fu, Yan; Zhang, Li; Gong, Jing-Xu; Wang, Zhen-Zhong; Xiao, Wei; Zhang, Hai-Yan; Guo, Yue-Wei published the artcile< Synthesis and biological evaluation of novel marine-derived indole-based 1,2,4-oxadiazoles derivatives as multifunctional neuroprotective agents>, SDS of cas: 229009-40-9, the main research area is indole oxadiazole preparation SAR neurotoxicity neuroprotective activity Alzheimer; 1,2,4-Oxadiazole derivatives; Amyloid-β-peptide; Neuroprotective activity; Oxygen–glucose deprivation; Phidianidines.
Phidianidines I [R = H, Br], isolated from the marine opisthobranch mollusk Phidiana militaris, present the first example of natural products possessing an 1,2,4-oxadiazole ring system and show various bioactivities. However, the structure-activity relationship study related to I has not been reported yet. As our ongoing effect toward marine-derived potential neuroprotective agents, a series of phidianidine-based derivatives II [R = ph, 4-Me-C6H4, 4-Et-C6H4, etc.] have been synthesized and evaluated for neuroprotective effects against amyloid-β25-35 (Aβ25-35)-, hydrogenperoxide (H2O2)-, and oxygen-glucose deprivation (OGD)-induced neurotoxicity in SH-SY5Y cells. The bioassay results indicated that some of analogs, especially II [R = 4-OEt-C6H4] and II [R = 4-OPr-C6H4], exhibited good in vitro neuroprotective effects in the above three screening models. The preliminary SAR study indicated that substituent groups introduced to the benzene ring play a crucial role in their bioactivity. In particular, the linear alkoxy group at 4-position favors the neuroprotective activity, while a bulky group could lead the activity decrease or loss. These findings could provide an alternative strategy for the development of novel indole-based 1,2,4-oxadiazole derivatives for the treatment of Alzheimer’s disease.
Bioorganic & Medicinal Chemistry Letters published new progress about Alzheimer disease. 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, SDS of cas: 229009-40-9.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics