88915-29-1Relevant academic research and scientific papers
Multi-target A beta oligomerization inhibitor
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Paragraph 0036; 0037; 0038, (2017/07/20)
The invention discloses a multi-target A beta oligomerization inhibitor. A general structural formula of the multi-target A beta oligomerization inhibitor is described in the specification, wherein R1 is one of hydrogen, straight chain alkyl, branched chain alkyl, alkoxy and halogen; R2 is one of hydrogen, straight chain alkyl, branched chain alkyl, alkoxy, halogen, a benzene ring, a hexa-heteroaromatic ring, a penta-heteroaromatic ring, a hepta-heteroarmoatic ring, naphthalene, anthracene, naphthoquinone, a multi-aromatic ring system and substituents thereof; R3 is one of hydrogen, straight chain alkyl, branched chain alkyl, halogen, carboxyl, nitryl, sulfonyl, amino, phosphate and substituents thereof; and n is equal to 1-5. The multi-target A beta oligomerization inhibitor disclosed by the invention is designed on the basis of A beta oligomerization process characteristics, a natural pharmacophore and other key enzyme active center structures, is novel in structure and obvious in activity and has good A beta oligomerization inhibitory effect, better water solubility and better performance in the aspects of transmembrane performance, activity and the like.
Synthesis method and application of multi-target A beta oligomerization inhibitor
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Paragraph 0046; 0047, (2017/07/22)
The invention discloses a synthesis method and application of a multi-target A beta oligomerization inhibitor. The synthesis method comprises the following steps: (1) taking bromaniline or derivatives thereof and (1-benzylpiperidine-4-yl)methylamine or derivatives thereof as starting raw materials, and carrying out Suzuki coupling reaction for preparing an intermediate II; (2) taking the intermediate II and 1,3-dibromopropane or other analogues as raw materials, and carrying out SN2 reaction for preparing an intermediate III with an alkyl chain; and (3) taking the intermediate III with the alkyl chain and imidazole or derivatives thereof as raw materials, and carrying out SN2 reaction for preparing the target product multi-target A beta oligomerization inhibitor. The synthesis method disclosed by the invention is simple and reliable in route, high in yield and more suitable for large-scale preparation. The multi-target A beta oligomerization inhibitor is applied to preparation of an A beta oligomerization inhibitor anti-AD medicine, a glutaminyl cyclase inhibitor anti-AD medicine and an acetylcholin esterase inhibitor anti-AD medicine and can be applied to kits of A beta oligomerization, glutaminyl cyclase and acetylcholin esterase.
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: Effects of fused heterocycles on antiviral activity and pharmacokinetic properties
Kim, Dooseop,Wang, Liping,Hale, Jeffrey J.,Lynch, Christopher L.,Budhu, Richard J.,MacCoss, Malcolm,Mills, Sander G.,Malkowitz, Lorraine,Gould, Sandra L.,Demartino, Julie A.,Springer, Martin S.,Hazuda, Daria,Miller, Michael,Kessler, Joseph,Hrin, Renee C.,Carver, Gwen,Carella, Anthony,Henry, Karen,Lineberger, Janet,Schleif, William A.,Emini, Emilio A.
, p. 2129 - 2134 (2007/10/03)
A series of 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists containing a variety of fused heterocycles at the 4-position of the piperidine side chain has been discovered, which are orally bioavailable with potent anti-HIV activity.
