Matches in SemOpenAlex for { <https://semopenalex.org/work/W2897557233> ?p ?o ?g. }
- W2897557233 endingPage "9965" @default.
- W2897557233 startingPage "9952" @default.
- W2897557233 abstract "Magnesium plays an important role in infection with Mycobacterium tuberculosis ( Mtb) as a signal of the extracellular environment, as a cofactor for many enzymes, and as a structural element in important macromolecules. Raltegravir, an antiretroviral drug that inhibits HIV-1 integrase is known to derive its potency from selective sequestration of active-site magnesium ions in addition to binding to a hydrophobic pocket. In order to determine if essential Mtb-related phosphoryl transfers could be disrupted in a similar manner, a directed screen of known molecules with integrase inhibitor-like pharmacophores ( N-alkyl-5-hydroxypyrimidinone carboxamides) was performed. Initial hits afforded compounds with low-micromolar potency against Mtb, acceptable cytotoxicity and PK characteristics, and robust SAR. Elucidation of the target of these compounds revealed that they lacked magnesium dependence and instead disappointingly inhibited a known promiscuous target in Mtb, decaprenylphosphoryl-β-d-ribose 2'-oxidase (DprE1, Rv3790)." @default.
- W2897557233 created "2018-10-26" @default.
- W2897557233 creator A5004460784 @default.
- W2897557233 creator A5005460851 @default.
- W2897557233 creator A5016977438 @default.
- W2897557233 creator A5017187552 @default.
- W2897557233 creator A5018322506 @default.
- W2897557233 creator A5033734108 @default.
- W2897557233 creator A5033869506 @default.
- W2897557233 creator A5034087952 @default.
- W2897557233 creator A5039711964 @default.
- W2897557233 creator A5050170408 @default.
- W2897557233 creator A5055539734 @default.
- W2897557233 creator A5057770186 @default.
- W2897557233 creator A5072040245 @default.
- W2897557233 creator A5075148540 @default.
- W2897557233 creator A5088592090 @default.
- W2897557233 creator A5089237387 @default.
- W2897557233 creator A5090012143 @default.
- W2897557233 date "2018-10-10" @default.
- W2897557233 modified "2023-10-16" @default.
- W2897557233 title "Discovery and Structure–Activity-Relationship Study of <i>N</i>-Alkyl-5-hydroxypyrimidinone Carboxamides as Novel Antitubercular Agents Targeting Decaprenylphosphoryl-β-<scp>d</scp>-ribose 2′-Oxidase" @default.
- W2897557233 cites W157842286 @default.
- W2897557233 cites W1976256007 @default.
- W2897557233 cites W1976656389 @default.
- W2897557233 cites W1979658483 @default.
- W2897557233 cites W1985588649 @default.
- W2897557233 cites W1987928733 @default.
- W2897557233 cites W1989828591 @default.
- W2897557233 cites W2003112779 @default.
- W2897557233 cites W2004716497 @default.
- W2897557233 cites W2005550545 @default.
- W2897557233 cites W2006513862 @default.
- W2897557233 cites W2011322868 @default.
- W2897557233 cites W2017227464 @default.
- W2897557233 cites W2020802861 @default.
- W2897557233 cites W2049819919 @default.
- W2897557233 cites W2056676492 @default.
- W2897557233 cites W2059458343 @default.
- W2897557233 cites W2063889189 @default.
- W2897557233 cites W2065037882 @default.
- W2897557233 cites W2068095506 @default.
- W2897557233 cites W2069126433 @default.
- W2897557233 cites W2073895348 @default.
- W2897557233 cites W2077292018 @default.
- W2897557233 cites W2082214470 @default.
- W2897557233 cites W2089068540 @default.
- W2897557233 cites W2098162437 @default.
- W2897557233 cites W2101666067 @default.
- W2897557233 cites W2110699006 @default.
- W2897557233 cites W2111986931 @default.
- W2897557233 cites W2118956677 @default.
- W2897557233 cites W2122267877 @default.
- W2897557233 cites W2123084649 @default.
- W2897557233 cites W2124075951 @default.
- W2897557233 cites W2129816077 @default.
- W2897557233 cites W2130479394 @default.
- W2897557233 cites W2147185188 @default.
- W2897557233 cites W2149802681 @default.
- W2897557233 cites W2155767187 @default.
- W2897557233 cites W2161897582 @default.
- W2897557233 cites W2162106505 @default.
- W2897557233 cites W2502356328 @default.
- W2897557233 cites W2511177309 @default.
- W2897557233 cites W2528123476 @default.
- W2897557233 cites W2565184786 @default.
- W2897557233 cites W2789436041 @default.
- W2897557233 cites W2790319309 @default.
- W2897557233 cites W2790605859 @default.
- W2897557233 cites W2806430653 @default.
- W2897557233 cites W4256118173 @default.
- W2897557233 doi "https://doi.org/10.1021/acs.jmedchem.8b00883" @default.
- W2897557233 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6257622" @default.
- W2897557233 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30350998" @default.
- W2897557233 hasPublicationYear "2018" @default.
- W2897557233 type Work @default.
- W2897557233 sameAs 2897557233 @default.
- W2897557233 citedByCount "27" @default.
- W2897557233 countsByYear W28975572332018 @default.
- W2897557233 countsByYear W28975572332019 @default.
- W2897557233 countsByYear W28975572332020 @default.
- W2897557233 countsByYear W28975572332021 @default.
- W2897557233 countsByYear W28975572332022 @default.
- W2897557233 countsByYear W28975572332023 @default.
- W2897557233 crossrefType "journal-article" @default.
- W2897557233 hasAuthorship W2897557233A5004460784 @default.
- W2897557233 hasAuthorship W2897557233A5005460851 @default.
- W2897557233 hasAuthorship W2897557233A5016977438 @default.
- W2897557233 hasAuthorship W2897557233A5017187552 @default.
- W2897557233 hasAuthorship W2897557233A5018322506 @default.
- W2897557233 hasAuthorship W2897557233A5033734108 @default.
- W2897557233 hasAuthorship W2897557233A5033869506 @default.
- W2897557233 hasAuthorship W2897557233A5034087952 @default.
- W2897557233 hasAuthorship W2897557233A5039711964 @default.
- W2897557233 hasAuthorship W2897557233A5050170408 @default.
- W2897557233 hasAuthorship W2897557233A5055539734 @default.
- W2897557233 hasAuthorship W2897557233A5057770186 @default.
- W2897557233 hasAuthorship W2897557233A5072040245 @default.