134477-40-0

Upstream product

• 59080-49-8 methyl 8-aminooctanoate 
• 1002-57-9 8-Aminooctanoic acid 
• 501-53-1 benzyl chloroformate 
• 19008-71-0 8-aminooctan-1-ol 
• 134477-39-7 8-<(benzyloxycarbonyl)amino>octan-1-ol 

Downstream Products

• 152564-55-1 ethyl (E)-10-<(benzyloxycarbonyl)amino>-4--2-(formylamino)dec-3-enoate 
• 134477-43-3 ethyl 10-<(benzyloxycarbonyl)amino>-2-(formylamino)-3-hydroxy-4-methylenedecanoate 
• 134477-42-2 ethyl 5-<8-<(benzyloxycarbonyl)amino>oct-1-en-2-yl>oxazoline-4-carboxylate 
• 152564-54-0 ethyl (E)-10-<(benzyloxycarbonyl)amino>-4-(bromomethyl)-2-(formylamino)dec-3-enoate 
• 134477-41-1 8-<(benzyloxycarbonyl)amino>-2-methyleneoctanal 

Relevant academic research and scientific papers

Synthesis of linear and cyclic guazatine derivatives endowed with antibacterial activity

Antibiotic resistance has reached alarming levels in many clinically-relevant human pathogens, and there is an increasing clinical need for new antibiotics active on drug-resistant Gram-negative pathogens who rapidly evolve towards pandrug resistance phenotypes. Here, we report on two related classes of guanidinic compounds endowed with antibacterial activity. The two best compounds (9a and 13d) exhibited the most potent antibacterial activity with MIC values ranging 0.12-8 μg/ml with most tested pathogens, including both Gram-positive and Gram-negative bacteria. Interestingly, MIC values were not affected (1-8 μg/ml) when measured using recent clinical isolates with various antibiotic resistance determinants. The results reported herein identify guazatine derivatives as an interesting starting point for the optimization of a potentially novel class of antibacterial agents.

Efficient synthesis of iminoctadine, a potent antifungal agent and polyamine oxidase inhibitor (PAO)

Iminoctadine (1,17-diguanidino-9-azaheptadecane), isolated from a mixture of polyamines and guanidines known as guazatine that is used in agriculture as a fungicide, showed interesting activity as human antifungal agent and PAO inhibitor. In this paper, w

Synthesis and Binding Properties of 2-Amino-5-phosphono-3-pentenoic Acid Photoaffinity Ligands as Probes for the Glutamate Recognition Site of the NMDA Receptor

Four ω-benzoylated (E)-2,10-diamino-4-(phosphonomethyl)dec-3-enoic acids have been synthesized and tested in vitro for binding to the glutamate recognition site of the NMDA (N-methyl-D-aspartate) receptor.The ω-4-azidosalicylamide derivative 24 was iodinated to give the photoaffinity ligand 25 (CGP 55802 A) which showed an IC50 value of 34 nM in the in vitro 3H>CGP 39653 binding assay.This compound and its radioactive 125I-form are the first photoaffinity ligands for the NMDA receptor with high affinity to the glutamate recognition site.