{"database":"biostudies-other","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["8(1)"],"submitter":["Choi SR"],"funding":["PHS HHS"],"journal":["Future medicinal chemistry"],"pagination":["11-6"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC5558544"],"abstract":["Menaquinone is used for transporting electrons and is essential for the aerobic and anaerobic respiratory systems of all pathogens and prokaryotes. Many Gram-positive bacteria use only menaquinone in the electron transport system. Thus, menaquinone biosynthesis is a potential target for the development of inhibitors against bacteria including drug-resistant pathogens.After modeling, synthesis and in vitro testing, we determined that 7-methoxy-2-naphthol-based inhibitors targeted the MenA enzyme of the menaquinone biosynthesis pathway. The developmental compounds 1 and 2 were active against Mycobacterium tuberculosis and methicillin-resistant Staphylococcus aureus with a minimal inhibitory concentration of 3-5 μg/ml.Nontraditional bicyclic inhibitors, compounds 1 and 2 could serve as lead compounds for the development of an antimicrobial agent, with activities against M. tuberculosis and methicillin-resistant S. aureus."],"repository":["biostudies-other"],"funding_grant_id":["R01 A1097550"],"data_source":["Europe PMC"],"pubmed_authors":["Hinrichs SH","Narayanasamy P","Bartling AM","Choi SR","Larson MA","Frandsen J"],"additional_accession":[]},"is_claimable":false,"name":"Discovery of bicyclic inhibitors against menaquinone biosynthesis.","description":"Menaquinone is used for transporting electrons and is essential for the aerobic and anaerobic respiratory systems of all pathogens and prokaryotes. Many Gram-positive bacteria use only menaquinone in the electron transport system. Thus, menaquinone biosynthesis is a potential target for the development of inhibitors against bacteria including drug-resistant pathogens.After modeling, synthesis and in vitro testing, we determined that 7-methoxy-2-naphthol-based inhibitors targeted the MenA enzyme of the menaquinone biosynthesis pathway. The developmental compounds 1 and 2 were active against Mycobacterium tuberculosis and methicillin-resistant Staphylococcus aureus with a minimal inhibitory concentration of 3-5 μg/ml.Nontraditional bicyclic inhibitors, compounds 1 and 2 could serve as lead compounds for the development of an antimicrobial agent, with activities against M. tuberculosis and methicillin-resistant S. aureus.","dates":{"release":"2016-01-01T00:00:00Z","publication":"2016 Jan","modification":"2019-08-04T08:27:29Z","creation":"2019-08-04T08:27:29Z"},"accession":"S-EPMC5558544","cross_references":{}}