FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2290420971> ?p ?o ?g. }

• W2290420971 endingPage "1888" @default.
• W2290420971 startingPage "1879" @default.
• W2290420971 abstract "On the basis of previous study on 2-methylpyrimidine-4-ylamine derivatives I, further synthetic optimization was done to find potent PDHc-E1 inhibitors with antibacterial activity. Three series of novel pyrimidine derivatives 6, 11 and 14 were designed and synthesized as potential Escherichia coli PDHc-E1 inhibitors by introducing 1,3,4-oxadiazole-thioether, 2,4-disubstituted-1,3-thiazole or 1,2,4-triazol-4-amine-thioether moiety into lead structure I, respectively. Most of 6, 11 and 14 exhibited good inhibitory activity against E. coli PHDc-E1 (IC50 0.97–19.21 μM) and obvious inhibitory activity against cyanobacteria (EC50 0.83–9.86 μM). Their inhibitory activities were much higher than that of lead structure I. 11 showed more potent inhibitory activity against both E. coli PDHc-E1 (IC50 < 6.62 μM) and cyanobacteria (EC50 < 1.63 μM) than that of 6, 14 or lead compound I. The most effective compound 11d with good enzyme-selectivity exhibited most powerful inhibitory potency against E. coli PDHc-E1 (IC50 = 0.97 μM) and cyanobacteria (EC50 = 0.83 μM). The possible interactions of the important residues of PDHc-E1 with title compounds were studied by molecular docking, site-directed mutagenesis, and enzymatic assays. The results indicated that 11d had more potent inhibitory activity than that of 14d or I due to its 1,3,4-oxadiazole moiety with more binding position and stronger interaction with Lsy392 and His106 at active site of E. coli PDHc-E1." @default.
• W2290420971 created "2016-06-24" @default.
• W2290420971 creator A5027688750 @default.
• W2290420971 creator A5046597133 @default.
• W2290420971 creator A5055131988 @default.
• W2290420971 creator A5057300798 @default.
• W2290420971 creator A5057335398 @default.
• W2290420971 creator A5066053587 @default.
• W2290420971 creator A5071256143 @default.
• W2290420971 creator A5079704942 @default.
• W2290420971 creator A5091044190 @default.
• W2290420971 date "2016-04-01" @default.
• W2290420971 modified "2023-10-17" @default.
• W2290420971 title "Rational design, synthesis and biological evaluation of 1,3,4-oxadiazole pyrimidine derivatives as novel pyruvate dehydrogenase complex E1 inhibitors" @default.
• W2290420971 cites W1971448184 @default.
• W2290420971 cites W1975638761 @default.
• W2290420971 cites W1978675965 @default.
• W2290420971 cites W1984842291 @default.
• W2290420971 cites W1988818307 @default.
• W2290420971 cites W1997598688 @default.
• W2290420971 cites W1999336467 @default.
• W2290420971 cites W2001955938 @default.
• W2290420971 cites W2017940149 @default.
• W2290420971 cites W2018779619 @default.
• W2290420971 cites W2027755752 @default.
• W2290420971 cites W2030328572 @default.
• W2290420971 cites W2036861701 @default.
• W2290420971 cites W2044877192 @default.
• W2290420971 cites W2056954970 @default.
• W2290420971 cites W2059315814 @default.
• W2290420971 cites W2059844222 @default.
• W2290420971 cites W2068083144 @default.
• W2290420971 cites W2069852546 @default.
• W2290420971 cites W2070956161 @default.
• W2290420971 cites W2074513866 @default.
• W2290420971 cites W2078247743 @default.
• W2290420971 cites W2092325101 @default.
• W2290420971 cites W2095046898 @default.
• W2290420971 cites W2095753590 @default.
• W2290420971 cites W2107988416 @default.
• W2290420971 cites W2125576777 @default.
• W2290420971 cites W2210381486 @default.
• W2290420971 cites W4245640678 @default.
• W2290420971 doi "https://doi.org/10.1016/j.bmc.2016.03.011" @default.
• W2290420971 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26972920" @default.
• W2290420971 hasPublicationYear "2016" @default.
• W2290420971 type Work @default.
• W2290420971 sameAs 2290420971 @default.
• W2290420971 citedByCount "31" @default.
• W2290420971 countsByYear W22904209712017 @default.
• W2290420971 countsByYear W22904209712018 @default.
• W2290420971 countsByYear W22904209712019 @default.
• W2290420971 countsByYear W22904209712020 @default.
• W2290420971 countsByYear W22904209712021 @default.
• W2290420971 countsByYear W22904209712022 @default.
• W2290420971 countsByYear W22904209712023 @default.
• W2290420971 crossrefType "journal-article" @default.
• W2290420971 hasAuthorship W2290420971A5027688750 @default.
• W2290420971 hasAuthorship W2290420971A5046597133 @default.
• W2290420971 hasAuthorship W2290420971A5055131988 @default.
• W2290420971 hasAuthorship W2290420971A5057300798 @default.
• W2290420971 hasAuthorship W2290420971A5057335398 @default.
• W2290420971 hasAuthorship W2290420971A5066053587 @default.
• W2290420971 hasAuthorship W2290420971A5071256143 @default.
• W2290420971 hasAuthorship W2290420971A5079704942 @default.
• W2290420971 hasAuthorship W2290420971A5091044190 @default.
• W2290420971 hasConcept C104317684 @default.
• W2290420971 hasConcept C159110408 @default.
• W2290420971 hasConcept C178790620 @default.
• W2290420971 hasConcept C181199279 @default.
• W2290420971 hasConcept C185592680 @default.
• W2290420971 hasConcept C193042331 @default.
• W2290420971 hasConcept C202751555 @default.
• W2290420971 hasConcept C21951064 @default.
• W2290420971 hasConcept C2776568683 @default.
• W2290420971 hasConcept C2777752112 @default.
• W2290420971 hasConcept C2778464347 @default.
• W2290420971 hasConcept C2779321679 @default.
• W2290420971 hasConcept C2779444094 @default.
• W2290420971 hasConcept C2779448499 @default.
• W2290420971 hasConcept C41183919 @default.
• W2290420971 hasConcept C41685203 @default.
• W2290420971 hasConcept C547475151 @default.
• W2290420971 hasConcept C55493867 @default.
• W2290420971 hasConcept C71240020 @default.
• W2290420971 hasConcept C71924100 @default.
• W2290420971 hasConceptScore W2290420971C104317684 @default.
• W2290420971 hasConceptScore W2290420971C159110408 @default.
• W2290420971 hasConceptScore W2290420971C178790620 @default.
• W2290420971 hasConceptScore W2290420971C181199279 @default.
• W2290420971 hasConceptScore W2290420971C185592680 @default.
• W2290420971 hasConceptScore W2290420971C193042331 @default.
• W2290420971 hasConceptScore W2290420971C202751555 @default.
• W2290420971 hasConceptScore W2290420971C21951064 @default.
• W2290420971 hasConceptScore W2290420971C2776568683 @default.
• W2290420971 hasConceptScore W2290420971C2777752112 @default.
• W2290420971 hasConceptScore W2290420971C2778464347 @default.
• W2290420971 hasConceptScore W2290420971C2779321679 @default.

• next