Authors He, YJ; Fu, TT; Li, YY; Xue, WW; Cui, MC; Wang, L; Niu, MD; Peng, ZP; Jia, JH in SPRINGER published article about POSITRON-EMISSION-TOMOGRAPHY; IMAGING AGENTS; ALZHEIMERS-DISEASE; PLAQUES; BINDING; PROBES; BENZOTHIAZOLE; PET in [He, Yujia; Wang, Liang; Niu, Mengda; Peng, Zhiping; Jia, Jianhua] Chongqing Med Univ, Coll Basic Med, Dept Radiol Med & Oncol, Chongqing 400016, Peoples R China; [Fu, Tingting; Xue, Weiwei] Chongqing Univ, Sch Pharmaceut Sci, Chongqing 401331, Peoples R China; [Li, Yuying; Cui, Mengchao] Beijing Normal Univ, Coll Chem, Key Lab Radiopharmaceut, Minist Educ, Beijing 100875, Peoples R China in 2021.0, Cited 30.0. HPLC of Formula: C7H8O2. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5
Cerebral amyloid angiopathy (CAA) commonly found in the aged is pathologically characterized by beta-amyloid (A beta) deposition in the walls of arteries and capillaries of brain. In this study, four flexible multidentate benzyldiamine derivatives as potential probes for cerebrovascular A beta deposition were designed and synthesized. In in vitro inhibition assays, the ligands 18-21 displayed high affinities for A beta aggregates with K-i values of 1.45 +/- 0.53 nM, 1.68 +/- 0.35 nM, 1.16 +/- 0.23 nM and 1.72 +/- 0.19 nM, respectively. A significant improvement in the binding affinity over the monomer, compounds 9-12 or benzyldiamine derivatives, demonstrated the applicability of the multidentate approach. The underlying mechanism of these novel A beta agents was explored by molecular docking technique, which theoretically verified the high affinities of the multidentate benzyldiamine derivatives for A beta aggregates. Moreover, the molecular masses of the ligands 18-21 are more than 700 Dalton, which are believed to be hardly capable of penetrating blood brain barrier. In this regard, these ligands could be used to distinguish CAA from Alzheimer’s disease which is another A beta-related disorder disease. To convert these ligands to positron emission tomography imaging agents, we attempted to radiosynthesize [F-18]18. Though the radiolabeling was not very successful, the preliminary results suggested that these newly proposed multidentate benzyldiamine derivatives may be used as potential A beta imaging agents in cerebral amyloid angiopathy. [GRAPHICS] .
About Mequinol, If you have any questions, you can contact He, YJ; Fu, TT; Li, YY; Xue, WW; Cui, MC; Wang, L; Niu, MD; Peng, ZP; Jia, JH or concate me.. HPLC of Formula: C7H8O2
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles