247033-97-2

Upstream product

• 73734-07-3 (1H-benzimidazol-2-yl)-(1-ethoxycarbonyl-piperidin-4-yl)amine 
• 104472-62-0 (1H-benzimidazol-2-yl)(piperidin-4-yl)amine 
• 58859-46-4 ethyl 4-aminopiperidine-1-carboxylate 
• 247035-02-5 ethyl 4-{4-(1H-benzimidazol-2-ylamino)piperidin-1-yl}benzoate 
• 247035-03-6 4-{4-(1H-benzimidazol-2-ylamino)piperidin-1-yl}benzoic acid 
• 247033-91-6 tert-butyl (2S)-amino-3-[4-[4-{(1-tert-butoxycarbonyl-1H-benzimidazol-2-yl)amino}piperidin-1-yl]benzoylamino]propionate 
• 349-88-2 4-Fluorobenzenesulfonyl chloride 
• 4857-06-1 2-chloro-1H-benzoimidazole 
• 247033-90-5 tert-butyl (2S)-benzyloxycarbonylamino-3-[4-[4-{(1-tert-butoxycarbonyl-1H-benzimidazol-2-yl)amino}piperidin-1-yl]benzoylamino]propionate 
• 247033-88-1 3-{4-[4-(1H-benzoimidazol-2-ylamino)-piperidin-1-yl]-benzoylamino}-2-benzyloxycarbonylamino-propionic acid tert-butyl ester 

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.