883726-97-4

Upstream product

• 369-25-5 methyl 3,4-difluorobenzoate 
• 247035-21-8 methyl 3-fluoro-4-{4-(methanesulfonyloxy)piperidin-1-yl}benzoate 
• 247035-20-7 methyl (4-azidopiperidin-1-yl)-3-fluorobenzoate 
• 247035-19-4 methyl 3-fluoro-4-(4-hydroxypiperidin-1-yl)benzoate 
• 5382-16-1 4-HYDROXYPIPERIDINE 
• 247035-22-9 methyl (4-aminopiperidin-1-yl)-3-fluorobenzoate 
• 137743-46-5 2-tert-butyloxycarbonylaminoethyl isothiocyanate 

Downstream Products

• 247034-20-4 tert-butyl (2S)-benzenesulfonylamino-3-[3-fluoro-4-{4-(4,5-dihydro-1H-imidazol-2-ylamino)piperidin-1-yl}benzoylamino]propionate 
• 247035-25-2 3-fluoro-4-{4-(4,5-dihydro-1H-imidazol-2-ylamino)piperidin-1-yl}benzoic acid 

Relevant academic research and scientific papers

Tricyclic pharmacophore-based molecules as novel integrin αvβ3 antagonists. Part 2: Synthesis of potent αvβ3/αIIbβ3 dual antagonists

We synthesized 4-aminopiperidine derivatives of our prototype integrin αvβ3 antagonist 1 in an attempt to increase the activity and water solubility. Introduction of one or two hydrophilic moieties into the central aromatic ring and/or the benzene ring at the C-terminus of 1 increased water solubility and enhanced inhibition of cell adhesion. The results of a structure-activity relationships (SAR) study indicated that the torsion angle between the central aromatic ring and the piperidine ring, and the acidity at the sulfonamide moiety, might be important for αvβ 3 receptor binding activity. Some of these compounds are novel and potent αvβ3/αIIbβ 3 dual antagonists with acceptable water solubility and a satisfactory early absorption, distribution, metabolism, excretion, and toxicity (ADMET) profile.