Matches in SemOpenAlex for { <https://semopenalex.org/work/W2767505980> ?p ?o ?g. }
- W2767505980 endingPage "1676" @default.
- W2767505980 startingPage "1667" @default.
- W2767505980 abstract "Over recent years, many RNA viruses have been “re-discovered”, including life-threatening flaviviruses, such as Dengue, Zika, and several encephalitis viruses. Since no specific inhibitors are currently available to treat these infections, there is a pressing need for new therapeutics. Among the flaviviral proteins, NS5 RNA-dependent RNA polymerase (RdRp) represents a validated target being essential for viral replication and it has no human analog. To date, few NS5 RdRp inhibitor chemotypes have been reported and no inhibitors are currently in clinical development. In this context, after an in vitro screening against Dengue 3 NS5 RdRp of our in-house HCV NS5B inhibitors focused library, we found that 2,1-benzothiazine 2,2-dioxides are promising non-nucleoside inhibitors of flaviviral RdRp with compounds 8 and 10 showing IC50 of 0.6 and 0.9 μM, respectively. Preliminary structure-activity relationships indicated a key role for the C-4 benzoyl group and the importance of a properly functionalized C-6 phenoxy moiety to modulate potency. Compound 8 acts as non-competitive inhibitor and its proposed pose in the so-called N pocket of the RdRp thumb domain allowed to explain the key contribution of the benzoyl and the phenoxy moieties for the ligand binding." @default.
- W2767505980 created "2017-11-17" @default.
- W2767505980 creator A5010835490 @default.
- W2767505980 creator A5013762333 @default.
- W2767505980 creator A5020731665 @default.
- W2767505980 creator A5034854833 @default.
- W2767505980 creator A5043864360 @default.
- W2767505980 creator A5045160799 @default.
- W2767505980 creator A5049415937 @default.
- W2767505980 creator A5054053277 @default.
- W2767505980 creator A5057923752 @default.
- W2767505980 creator A5058320949 @default.
- W2767505980 creator A5066081837 @default.
- W2767505980 creator A5088646672 @default.
- W2767505980 date "2018-01-01" @default.
- W2767505980 modified "2023-10-07" @default.
- W2767505980 title "Functionalized 2,1-benzothiazine 2,2-dioxides as new inhibitors of Dengue NS5 RNA-dependent RNA polymerase" @default.
- W2767505980 cites W1500266350 @default.
- W2767505980 cites W1757990252 @default.
- W2767505980 cites W1967404435 @default.
- W2767505980 cites W1969630443 @default.
- W2767505980 cites W1975650895 @default.
- W2767505980 cites W1981910825 @default.
- W2767505980 cites W1986476355 @default.
- W2767505980 cites W1995584986 @default.
- W2767505980 cites W2021169961 @default.
- W2767505980 cites W2028198504 @default.
- W2767505980 cites W2038684454 @default.
- W2767505980 cites W2040231819 @default.
- W2767505980 cites W2053484442 @default.
- W2767505980 cites W2053490656 @default.
- W2767505980 cites W2054056331 @default.
- W2767505980 cites W2087028046 @default.
- W2767505980 cites W2114779636 @default.
- W2767505980 cites W2118547293 @default.
- W2767505980 cites W2119473061 @default.
- W2767505980 cites W2127287358 @default.
- W2767505980 cites W2130479394 @default.
- W2767505980 cites W2170534481 @default.
- W2767505980 cites W2176826107 @default.
- W2767505980 cites W2203857662 @default.
- W2767505980 cites W2206069791 @default.
- W2767505980 cites W2222589778 @default.
- W2767505980 cites W2272006634 @default.
- W2767505980 cites W2334412610 @default.
- W2767505980 cites W2485464167 @default.
- W2767505980 cites W2523604740 @default.
- W2767505980 cites W2529109442 @default.
- W2767505980 cites W2531217889 @default.
- W2767505980 cites W2952885642 @default.
- W2767505980 cites W4210433968 @default.
- W2767505980 cites W4211002680 @default.
- W2767505980 cites W2952977088 @default.
- W2767505980 doi "https://doi.org/10.1016/j.ejmech.2017.10.064" @default.
- W2767505980 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29137867" @default.
- W2767505980 hasPublicationYear "2018" @default.
- W2767505980 type Work @default.
- W2767505980 sameAs 2767505980 @default.
- W2767505980 citedByCount "21" @default.
- W2767505980 countsByYear W27675059802019 @default.
- W2767505980 countsByYear W27675059802020 @default.
- W2767505980 countsByYear W27675059802021 @default.
- W2767505980 countsByYear W27675059802022 @default.
- W2767505980 countsByYear W27675059802023 @default.
- W2767505980 crossrefType "journal-article" @default.
- W2767505980 hasAuthorship W2767505980A5010835490 @default.
- W2767505980 hasAuthorship W2767505980A5013762333 @default.
- W2767505980 hasAuthorship W2767505980A5020731665 @default.
- W2767505980 hasAuthorship W2767505980A5034854833 @default.
- W2767505980 hasAuthorship W2767505980A5043864360 @default.
- W2767505980 hasAuthorship W2767505980A5045160799 @default.
- W2767505980 hasAuthorship W2767505980A5049415937 @default.
- W2767505980 hasAuthorship W2767505980A5054053277 @default.
- W2767505980 hasAuthorship W2767505980A5057923752 @default.
- W2767505980 hasAuthorship W2767505980A5058320949 @default.
- W2767505980 hasAuthorship W2767505980A5066081837 @default.
- W2767505980 hasAuthorship W2767505980A5088646672 @default.
- W2767505980 hasConcept C104317684 @default.
- W2767505980 hasConcept C135763542 @default.
- W2767505980 hasConcept C151730666 @default.
- W2767505980 hasConcept C159047783 @default.
- W2767505980 hasConcept C181199279 @default.
- W2767505980 hasConcept C185592680 @default.
- W2767505980 hasConcept C2776449523 @default.
- W2767505980 hasConcept C2779343474 @default.
- W2767505980 hasConcept C2781426373 @default.
- W2767505980 hasConcept C2781463415 @default.
- W2767505980 hasConcept C41258723 @default.
- W2767505980 hasConcept C55493867 @default.
- W2767505980 hasConcept C67705224 @default.
- W2767505980 hasConcept C71240020 @default.
- W2767505980 hasConcept C82381507 @default.
- W2767505980 hasConcept C86803240 @default.
- W2767505980 hasConcept C98274493 @default.
- W2767505980 hasConceptScore W2767505980C104317684 @default.
- W2767505980 hasConceptScore W2767505980C135763542 @default.
- W2767505980 hasConceptScore W2767505980C151730666 @default.
- W2767505980 hasConceptScore W2767505980C159047783 @default.