Matches in SemOpenAlex for { <https://semopenalex.org/work/W2912811544> ?p ?o ?g. }
Showing items 1 to 96 of
96
with 100 items per page.
- W2912811544 endingPage "2420" @default.
- W2912811544 startingPage "2413" @default.
- W2912811544 abstract "Cyanobacterial pyruvate dehydrogenase multienzyme complex E1 (PDHc E1) is a potential target enzyme for finding inhibitors to control harmful cyanobacterial blooms. In this study, a series of novel triazole thiamin diphosphate (ThDP) analogs were designed and synthesized by modifying the substituent group of triazole ring and optimizing triazole-benzene linker as potential cyanobacterial PDHc E1 (Cy-PDHc E1) inhibitors. Their inhibitory activities against Cy-PDHc E1 in vitro and algicide activities in vivo were further examined. Most of these compounds exhibited prominent inhibitory activities against Cy-PDHc E1 (IC50 1.48–4.48 μM) and good algicide activities against Synechocystis PCC6803 (EC50 0.84–2.44 µM) and Microcystis aeruginosa FACHB905 (EC50 0.74–1.77 µM). Especially, compound 8d showed not only the highest inhibitory activity against Cy-PDHc E1 (IC50 1.48 μM), but also the most powerful inhibitory selectivity between Cy-PDHc E1 (inhibitory rate 98.90%) and porcine PDHc E1 (inhibitory rate only 9.54%). Furthermore, the potential interaction between compound 8d and Cy-PDHc E1 was analyzed by a molecular docking method and site-directed mutagenesis and enzymatic analysis and fluorescence spectral analysis. These results indicated that compound 8d could be used as a hit compound for further optimization and might have potential to be developed as a new algicide." @default.
- W2912811544 created "2019-02-21" @default.
- W2912811544 creator A5002661071 @default.
- W2912811544 creator A5046273989 @default.
- W2912811544 creator A5051380367 @default.
- W2912811544 creator A5054183548 @default.
- W2912811544 creator A5057300798 @default.
- W2912811544 creator A5057335398 @default.
- W2912811544 creator A5066053587 @default.
- W2912811544 creator A5071256143 @default.
- W2912811544 creator A5079704942 @default.
- W2912811544 date "2019-06-01" @default.
- W2912811544 modified "2023-10-13" @default.
- W2912811544 title "Design, synthesis and biological evaluation of novel inhibitors against cyanobacterial pyruvate dehydrogenase multienzyme complex E1" @default.
- W2912811544 cites W1640953885 @default.
- W2912811544 cites W1972667333 @default.
- W2912811544 cites W1973172918 @default.
- W2912811544 cites W1976116913 @default.
- W2912811544 cites W1986191025 @default.
- W2912811544 cites W1988818307 @default.
- W2912811544 cites W2001955938 @default.
- W2912811544 cites W2006838082 @default.
- W2912811544 cites W2012808560 @default.
- W2912811544 cites W2017940149 @default.
- W2912811544 cites W2023535483 @default.
- W2912811544 cites W2059315814 @default.
- W2912811544 cites W2064511231 @default.
- W2912811544 cites W2068083144 @default.
- W2912811544 cites W2073504782 @default.
- W2912811544 cites W2074513866 @default.
- W2912811544 cites W2081350198 @default.
- W2912811544 cites W2106174087 @default.
- W2912811544 cites W2114520383 @default.
- W2912811544 cites W2159614853 @default.
- W2912811544 cites W2170898470 @default.
- W2912811544 cites W2251204990 @default.
- W2912811544 cites W2290420971 @default.
- W2912811544 cites W2341149581 @default.
- W2912811544 cites W2764042572 @default.
- W2912811544 cites W2769012525 @default.
- W2912811544 cites W2804822363 @default.
- W2912811544 cites W4211010233 @default.
- W2912811544 doi "https://doi.org/10.1016/j.bmc.2019.01.021" @default.
- W2912811544 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30692021" @default.
- W2912811544 hasPublicationYear "2019" @default.
- W2912811544 type Work @default.
- W2912811544 sameAs 2912811544 @default.
- W2912811544 citedByCount "10" @default.
- W2912811544 countsByYear W29128115442019 @default.
- W2912811544 countsByYear W29128115442020 @default.
- W2912811544 countsByYear W29128115442021 @default.
- W2912811544 countsByYear W29128115442022 @default.
- W2912811544 countsByYear W29128115442023 @default.
- W2912811544 crossrefType "journal-article" @default.
- W2912811544 hasAuthorship W2912811544A5002661071 @default.
- W2912811544 hasAuthorship W2912811544A5046273989 @default.
- W2912811544 hasAuthorship W2912811544A5051380367 @default.
- W2912811544 hasAuthorship W2912811544A5054183548 @default.
- W2912811544 hasAuthorship W2912811544A5057300798 @default.
- W2912811544 hasAuthorship W2912811544A5057335398 @default.
- W2912811544 hasAuthorship W2912811544A5066053587 @default.
- W2912811544 hasAuthorship W2912811544A5071256143 @default.
- W2912811544 hasAuthorship W2912811544A5079704942 @default.
- W2912811544 hasConcept C181199279 @default.
- W2912811544 hasConcept C185592680 @default.
- W2912811544 hasConcept C55493867 @default.
- W2912811544 hasConcept C71240020 @default.
- W2912811544 hasConcept C88099638 @default.
- W2912811544 hasConceptScore W2912811544C181199279 @default.
- W2912811544 hasConceptScore W2912811544C185592680 @default.
- W2912811544 hasConceptScore W2912811544C55493867 @default.
- W2912811544 hasConceptScore W2912811544C71240020 @default.
- W2912811544 hasConceptScore W2912811544C88099638 @default.
- W2912811544 hasFunder F4320321001 @default.
- W2912811544 hasIssue "12" @default.
- W2912811544 hasLocation W29128115441 @default.
- W2912811544 hasLocation W29128115442 @default.
- W2912811544 hasOpenAccess W2912811544 @default.
- W2912811544 hasPrimaryLocation W29128115441 @default.
- W2912811544 hasRelatedWork W1158080041 @default.
- W2912811544 hasRelatedWork W1164537646 @default.
- W2912811544 hasRelatedWork W1795884996 @default.
- W2912811544 hasRelatedWork W1816182920 @default.
- W2912811544 hasRelatedWork W1850986032 @default.
- W2912811544 hasRelatedWork W2015269539 @default.
- W2912811544 hasRelatedWork W2017243037 @default.
- W2912811544 hasRelatedWork W204747089 @default.
- W2912811544 hasRelatedWork W2080203695 @default.
- W2912811544 hasRelatedWork W4242974861 @default.
- W2912811544 hasVolume "27" @default.
- W2912811544 isParatext "false" @default.
- W2912811544 isRetracted "false" @default.
- W2912811544 magId "2912811544" @default.
- W2912811544 workType "article" @default.