959615-84-0

Upstream product

• 959615-83-9 1-(1,3-dioxolan-2-ylmethyl)-1,5-naphthyridin-2(1H)-one 
• 1003947-25-8 1-allyl-1,5-naphthyridin-2(1H)-one 
• 67-56-1 methanol 
• 10261-82-2 1,5-naphthyridin-2(1H)-one 
• 27017-69-2 2-methoxy-[1,5]-naphthyridine 
• 23443-25-6 6-methoxy-1,5-naphthyridin-4-ol 
• 881658-92-0 8-bromo-2-methoxy-1,5-naphthyridine 

Downstream Products

• 1173896-38-2 1-(2-(4-((3,4-dichlorobenzyl)amino)piperidin-1-yl)ethyl)-1,5-naphthyridin-2(1H)-one 

Relevant academic research and scientific papers

Mycobacterium tuberculosis gyrase inhibitors as a new class of antitubercular drugs

One way to speed up the TB drug discovery process is to search for antitubercular activity among compound series that already possess some of the key properties needed in anti-infective drug discovery, such as whole-cell activity and oral absorption. Here, we present MGIs, a new series of Mycobacterium tuberculosis gyrase inhibitors, which stem from the long-term efforts GSK has dedicated to the discovery and development of novel bacterial topoisomerase inhibitors (NBTIs). The compounds identified were found to be devoid of fluoroquinolone (FQ) cross-resistance and seem to operate through a mechanism similar to that of the previously described NBTI GSK antibacterial drug candidate. The remarkable in vitro and in vivo antitubercular profiles showed by the hits has prompted us to further advance the MGI project to full lead optimization.

NAPHTHYRIDIN-2 (1 H)-ONE COMPOUNDS USEFUL AS ANTIBACTERIALS

Compounds of Formula (I) wherein substituents R1, R2 and R5 are as defined, and Ar represents substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, furanyl, imidazolyl and thiophenyl substituted by a hydroxyalkyl substituent and an optional other substituent; compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.

NOVEL HETEROCYCLIC COMPOUND OR SALT THEREOF AND INTERMEDIATE THEREOF

Disclosed is a compound represented by the general formula: [wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom] or a salt thereof, which is useful as an antibacterial agent.