Matches in SemOpenAlex for { <https://semopenalex.org/work/W3161891180> ?p ?o ?g. }
- W3161891180 endingPage "5817" @default.
- W3161891180 startingPage "5804" @default.
- W3161891180 abstract "A series of novel 2,6-dimethyl-4-aminopyrimidine hydrazones 5 were rationally designed and synthesized as pyruvate dehydrogenase complex E1 (PDHc-E1) inhibitors. Compounds 5 strongly inhibited Escherichia coli (E. coli) PDHc-E1 (IC50 values 0.94–15.80 μM). As revealed by molecular docking, site-directed mutagenesis, enzymatic, and inhibition kinetic analyses, compounds 5 competitively inhibited PDHc-E1 and bound in a “straight” pattern at the E. coli PDHc-E1 active site, which is a new binding mode. In in vitro antifungal assays, most compounds 5 at 50 μg/mL showed more than 80% inhibition against the mycelial growth of six tested phytopathogenic fungi, including Botrytis cinerea, Monilia fructigena, Colletotrichum gloeosporioides, andBotryosphaeria dothidea. Notably, 5f and 5i were 1.8–380 fold more potent against M. fructigena than the commercial fungicides captan and chlorothalonil. In vivo, 5f and 5i controlled the growth of M. fructigena comparably to the commercial fungicide tebuconazole. Thus, 5f and 5i have potential commercial value for the control of peach brown rot caused by M. fructigena." @default.
- W3161891180 created "2021-05-24" @default.
- W3161891180 creator A5018889788 @default.
- W3161891180 creator A5038351890 @default.
- W3161891180 creator A5039252463 @default.
- W3161891180 creator A5054183548 @default.
- W3161891180 creator A5055131988 @default.
- W3161891180 creator A5057335398 @default.
- W3161891180 creator A5066053587 @default.
- W3161891180 creator A5071256143 @default.
- W3161891180 creator A5079704942 @default.
- W3161891180 date "2021-05-19" @default.
- W3161891180 modified "2023-10-13" @default.
- W3161891180 title "Design, Synthesis, and Antifungal Activity of 2,6-Dimethyl-4-aminopyrimidine Hydrazones as PDHc-E1 Inhibitors with a Novel Binding Mode" @default.
- W3161891180 cites W1540293909 @default.
- W3161891180 cites W1553041447 @default.
- W3161891180 cites W1966790639 @default.
- W3161891180 cites W1971586343 @default.
- W3161891180 cites W1972253381 @default.
- W3161891180 cites W1974866662 @default.
- W3161891180 cites W1979330531 @default.
- W3161891180 cites W1988818307 @default.
- W3161891180 cites W1989902298 @default.
- W3161891180 cites W1994350395 @default.
- W3161891180 cites W1997598688 @default.
- W3161891180 cites W1999336467 @default.
- W3161891180 cites W2001955938 @default.
- W3161891180 cites W2008717308 @default.
- W3161891180 cites W2017940149 @default.
- W3161891180 cites W2023535483 @default.
- W3161891180 cites W2025875085 @default.
- W3161891180 cites W2027755752 @default.
- W3161891180 cites W2030328572 @default.
- W3161891180 cites W2030523101 @default.
- W3161891180 cites W2032422364 @default.
- W3161891180 cites W2033501336 @default.
- W3161891180 cites W2051531757 @default.
- W3161891180 cites W2059315814 @default.
- W3161891180 cites W2061371173 @default.
- W3161891180 cites W2074513866 @default.
- W3161891180 cites W2090321973 @default.
- W3161891180 cites W2103350097 @default.
- W3161891180 cites W2157935454 @default.
- W3161891180 cites W2166318747 @default.
- W3161891180 cites W2210381486 @default.
- W3161891180 cites W2290420971 @default.
- W3161891180 cites W2316047663 @default.
- W3161891180 cites W2328965931 @default.
- W3161891180 cites W2329128932 @default.
- W3161891180 cites W2330036312 @default.
- W3161891180 cites W2406627128 @default.
- W3161891180 cites W2550278439 @default.
- W3161891180 cites W2764042572 @default.
- W3161891180 cites W2769012525 @default.
- W3161891180 cites W2804822363 @default.
- W3161891180 cites W2806860969 @default.
- W3161891180 cites W2912811544 @default.
- W3161891180 cites W2969781694 @default.
- W3161891180 cites W2974377858 @default.
- W3161891180 cites W2981894022 @default.
- W3161891180 cites W2981998770 @default.
- W3161891180 cites W2991331495 @default.
- W3161891180 cites W3087615753 @default.
- W3161891180 doi "https://doi.org/10.1021/acs.jafc.0c07701" @default.
- W3161891180 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34008970" @default.
- W3161891180 hasPublicationYear "2021" @default.
- W3161891180 type Work @default.
- W3161891180 sameAs 3161891180 @default.
- W3161891180 citedByCount "15" @default.
- W3161891180 countsByYear W31618911802022 @default.
- W3161891180 countsByYear W31618911802023 @default.
- W3161891180 crossrefType "journal-article" @default.
- W3161891180 hasAuthorship W3161891180A5018889788 @default.
- W3161891180 hasAuthorship W3161891180A5038351890 @default.
- W3161891180 hasAuthorship W3161891180A5039252463 @default.
- W3161891180 hasAuthorship W3161891180A5054183548 @default.
- W3161891180 hasAuthorship W3161891180A5055131988 @default.
- W3161891180 hasAuthorship W3161891180A5057335398 @default.
- W3161891180 hasAuthorship W3161891180A5066053587 @default.
- W3161891180 hasAuthorship W3161891180A5071256143 @default.
- W3161891180 hasAuthorship W3161891180A5079704942 @default.
- W3161891180 hasConcept C104317684 @default.
- W3161891180 hasConcept C181199279 @default.
- W3161891180 hasConcept C185592680 @default.
- W3161891180 hasConcept C2775867217 @default.
- W3161891180 hasConcept C2777735867 @default.
- W3161891180 hasConcept C547475151 @default.
- W3161891180 hasConcept C55493867 @default.
- W3161891180 hasConcept C59822182 @default.
- W3161891180 hasConcept C74600772 @default.
- W3161891180 hasConcept C86803240 @default.
- W3161891180 hasConceptScore W3161891180C104317684 @default.
- W3161891180 hasConceptScore W3161891180C181199279 @default.
- W3161891180 hasConceptScore W3161891180C185592680 @default.
- W3161891180 hasConceptScore W3161891180C2775867217 @default.
- W3161891180 hasConceptScore W3161891180C2777735867 @default.
- W3161891180 hasConceptScore W3161891180C547475151 @default.
- W3161891180 hasConceptScore W3161891180C55493867 @default.