1460301-35-2

Upstream product

• 1251836-88-0 methyl 3’-hydroxybiphenyl-2-carboxylate 
• 92379-10-7 3’-hydroxybiphenyl-2-carboxylic acid 
• 1460306-69-7 C₂₇H₃₂N₂O₇ 
• 1460306-70-0 C₄₂H₅₀N₄O₁₀ 
• 1460306-71-1 C₃₅H₄₂N₄O₈ 
• 1264245-74-0 (2S,4S)-allyl 4-(tert-butoxycarbonylamino)-2-(hydroxymethyl)-pyrrolidine-1-carboxylate 
• 1460306-59-5 (R)-allyl 4-amino-2-(benzyloxycarbonylamino)butanoate toluene-4-sulfonate 

Downstream Products

• 1460301-50-1 benzyl N-[(12R,16S,18S)-8,13-dioxo-16-[(phenoxycarbonyl)amino]-20-oxa-9,14-diazatetracyclo[19.3.1.0²'⁷.0¹⁴'¹⁸]pentacosa-1⁽²⁵⁾,2,4,6,21,23-hexaen-12-yl]carbamate 
• 1460305-87-6 benzyl N-[(12R,16S,18S)-8,13-dioxo-16-{[2-(1-pyrrolidinyl)acetyl]amino}-20-oxa-9,14-diazatetracyclo[19.3.1.0²'⁷.0¹⁴'¹⁸]pentacosa-1⁽²⁵⁾,2,4,6,21,23-hexaen-12-yl]carbamate 

Relevant academic research and scientific papers

CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS

The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS

The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1 ) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.