410544-95-5

Basic information

• Product Name: 5-(1,1-Dioxoperhydro-1,2-thiazin-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
• Synonyms: L-870810; 5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
• CAS NO: 410544-95-5
• Molecular Formula: C₂₀H₁₉FN₄O₄S
• Molecular Weight: 430.4527
• Mol File: 410544-95-5.mol
• Article Data: 3

Chemical Properties

• Density: 1.471g/cm³
• Refractive Index: 1.663
• CAS DataBase Reference: 5-(1,1-Dioxoperhydro-1,2-thiazin-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide(CAS DataBase Reference)
• NIST Chemistry Reference: 5-(1,1-Dioxoperhydro-1,2-thiazin-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide(410544-95-5)
• EPA Substance Registry System: 5-(1,1-Dioxoperhydro-1,2-thiazin-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide(410544-95-5)

Safety Data

• Hazardous Substances Data: 410544-95-5(Hazardous Substances Data)

Upstream product

• 410544-56-8 N-(4-fluorobenzyl)-8-hydroxy-5-bromo-1,6-naphthyridine-7-carboxamide 
• 37441-50-2 1,4-butanesultam 
• 699-98-9 Pyridine-2,3-dicarboxylic anhydride 
• 118892-73-2 2,3-pyridinedicarboxylic acid 2-(isopropyl ester) 
• 142777-96-6 isopropyl 3-(chlorocarbonyl)pyridine-2-carboxylate 
• 118892-74-3 3-hydroxymethyl-pyridine-2-carboxylic acid isopropyl ester 
• 412334-35-1 3-{[methoxycarbonylmethyl-(toluene-4-sulfonyl)-amino]-methyl}-pyridine-2-carboxylic acid isopropyl ester 
• 410542-68-6 8-hydroxy-1,6-naphthyridine-7-carboxylic acid methyl ester 
• 410544-37-5 5-bromo-8-hydroxy-[1,6]naphthyridine-7-carboxylic acid methyl ester 
• 606080-41-5 5-(1,1-dioxido-1,2-thiazinan-2-yl)-8-hydroxy-1,6-naphthyridine-7-carboxylic acid 
• 140-75-0 para-fluorobenzylamine 
• 410545-61-8 methyl 5-(1,1-dioxido-1,2-thiazinan-2-yl)-8-(tosyloxy)-1,6-naphthyridine-7-carboxylate 
• 410545-60-7 methyl 5-bromo-8-p-toluenesulfonyloxy-1,6-naphthyridine-7-carboxylate 

Relevant articles and documents

Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent in Vitro Antileishmanial Activity: Initial SAR and Assessment of in Vivo Activity

Visceral leishmaniasis (VL) is a parasitic infection that results in approximately 26 ?000-65 ?000 deaths annually. The available treatments are hampered by issues such as toxicity, variable efficacy, and unsuitable dosing options. The need for new treatments is urgent and led to a collaboration between the Drugs for Neglected Diseases initiative (DNDi), GlaxoSmithKline (GSK), and the University of Dundee. An 8-hydroxynaphthyridine was identified as a start point, and an early compound demonstrated weak efficacy in a mouse model of VL but was hampered by glucuronidation. Efforts to address this led to the development of compounds with improved in vitro profiles, but these were poorly tolerated in vivo. Investigation of the mode of action (MoA) demonstrated that activity was driven by sequestration of divalent metal cations, a mechanism which was likely to drive the poor tolerability. This highlights the importance of investigating MoA and pharmacokinetics at an early stage for phenotypically active series.

Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors

Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the