4-aminopiperidine and 4-nitrobenzylthioinosine

4-aminopiperidine has been researched along with 4-nitrobenzylthioinosine* in 1 studies

*4-nitrobenzylthioinosine: inhibitor of nucleoside transport; acts on ENT1 [MeSH]

Trials

1 trial(s) available for 4-aminopiperidine and 4-nitrobenzylthioinosine

Article	Year
Structure activity relationship of N-1 substituted 1,5-naphthyrid-2-one analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-9). Bioorganic & medicinal chemistry letters, 2022, 11-01, Volume: 75 Novel bacterial topoisomerase inhibitors (NBTIs) are the newest members of gyrase inhibitor broad-spectrum antibacterial agents, represented by the most advanced member, gepotidacin, a 4-amino-piperidine linked NBTI, which is undergoing phase III clinical trials for treatment of urinary tract infections (UTI). We have extensively reported studies on oxabicyclooctane linked NBTIs, including AM-8722. The present study summarizes structure activity relationship (SAR) of AM-8722 leading to identification of 7-fluoro-1-cyanomethyl-1,5-naphthyridin-2-one based NBTI (16, AM-8888) with improved potency and spectrum (MIC values of 0.016-4 μg/mL), with Pseudomonas aeruginosa being the least sensitive strain (MIC 4 μg/mL). Topics: Anti-Bacterial Agents; DNA Gyrase; DNA Topoisomerase IV; Microbial Sensitivity Tests; Staphylococcus aureus; Structure-Activity Relationship; Thioinosine; Topoisomerase II Inhibitors; Topoisomerase Inhibitors	2022

Article

Year

Structure activity relationship of N-1 substituted 1,5-naphthyrid-2-one analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-9).

Bioorganic & medicinal chemistry letters, 2022, 11-01, Volume: 75

Novel bacterial topoisomerase inhibitors (NBTIs) are the newest members of gyrase inhibitor broad-spectrum antibacterial agents, represented by the most advanced member, gepotidacin, a 4-amino-piperidine linked NBTI, which is undergoing phase III clinical trials for treatment of urinary tract infections (UTI). We have extensively reported studies on oxabicyclooctane linked NBTIs, including AM-8722. The present study summarizes structure activity relationship (SAR) of AM-8722 leading to identification of 7-fluoro-1-cyanomethyl-1,5-naphthyridin-2-one based NBTI (16, AM-8888) with improved potency and spectrum (MIC values of 0.016-4 μg/mL), with Pseudomonas aeruginosa being the least sensitive strain (MIC 4 μg/mL).

Topics: Anti-Bacterial Agents; DNA Gyrase; DNA Topoisomerase IV; Microbial Sensitivity Tests; Staphylococcus aureus; Structure-Activity Relationship; Thioinosine; Topoisomerase II Inhibitors; Topoisomerase Inhibitors

2022