1335312-29-2

Upstream product

• 458-37-7 curcumin 
• 6945-92-2 2-hydrazinyl acetic acid ethyl ester hydrochloride 

Downstream Products

• 1264718-62-8 2-[3,5-bis((E)-4-hydroxy-3-methoxystyryl)-1H-pyrazol-1-yl]-N-(prop-2-yn-1-yl)acetamide 
• 1335312-31-6 2-(3,5-bis((E)-4-hydroxy-3-methoxystyryl)-1H-pyrazol-1-yl) acetic acid 
• 1264718-69-5 2-(3,5-bis((E)-4-hydroxy-3-methoxystyryl)-1H-pyrazol-1-yl)-N-((1-(2-(2-(2-hydroxyethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methyl)acetamide 

Relevant academic research and scientific papers

Synthesis of labeled curcumin derivatives as tools for in vitro blood brain barrier trafficking studies

Successful drug delivery to the brain is crucial for the therapy of many neurological disorders, including Alzheimer's disease. A stable tritiated pyrazole curcumin derivative, exhibiting ability to interact with Aβ peptide, has been synthesized to allow

MACROMOLECULAR PRODRUG-BASED THERMOSENSITIVE INJECTABLE GEL AS A NOVEL DRUG DELIVERY PLATFORM

This application discloses prodrug-based thermosensitive gel ("ProGel") comprised of conjugates of dmg molecules with water-soluble polymeric carriers, which are capable of controlled release of the dmg molecules into the tissue of a subject. Use of the ProGel-Drug conjugates for treatment of various diseases or disorders and methods of preparing them are also disclosed.

Curcumin derivatives with improved physicochemical properties and nanoliposomes surface-decorated with the derivatives with very high affinity for amyloid-beta1-42 peptide

Amyloid β (Aβ) aggregates are considered as possible targets for therapy and/or diagnosis of Alzheimer disease (AD). It has been previously shown that curcumin targets Aβ plaques and interferes with their formation, suggesting a potential role for prevention or treatment of AD. In the present invention, curcumin-derivatives with improved physicochemical properties were synthesized and a "click chemistry" as well as a conventional liposome preparation method, were used to generate nanoliposomes decorated with the curcumin derivatives. These derivatives were designed to maintain the planar structure required for interaction with Aβ, as directly confirmed by Surface Plasmon Resonance experiments. Surface Plasmon Resonance experiments, measuring the binding of flowing liposomes to immobilized Aβ1-42, indicated that the liposomes exposing curcumin derivatives have extremely high affinity for Aβ1-42 fibrils (1-5 nM), likely because of the occurrence of multivalent interactions. The present invention describes the synthesis of the curcumin derivatives and the preparation and characterization of new nanoliposomes with a very high affinity for Aβ1-42 fibrils, to be exploited as vectors for the targeted delivery of new diagnostic and therapeutic molecules for AD.