FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2949099935> ?p ?o ?g. }

• W2949099935 endingPage "751" @default.
• W2949099935 startingPage "740" @default.
• W2949099935 abstract "This research has provided the most active 5-HT6R agents among 1,3,5-triazine derivatives investigated to date and has also identified the world's first selenium-containing 5-HT6R ligands. The studies are focused on design, synthesis, biological evaluation and docking-supported SAR analysis for novel 5-HT6R agents as derivatives of lead structure 4-(4-methylpiperazin-1-yl)-6-(phenoxymethyl)-1,3,5-triazin-2-amine (7). The lead modifications included an introduction of: (i) various small substituents at benzene ring, (ii) a branched ether linker or (iii) the ether oxygen replacement with other chalcogen (S, Se) or sulfonyl moiety. Hence, a series of new compounds (7-24) was synthesized and examined on their affinities for 5-HT6R and selectivity, in respect to the 5-HT1AR, 5-HT2AR, 5-HT7R and dopamine D2 receptor, in the radioligand binding assays. For representative most active compounds functional bioassays and toxicity profile in vitro and antidepressant-like activity in vivo were examined. The 2-isopropyl-5-methylphenyl derivative (10) was found as the most active triazine 5-HT6R antagonist (Ki = 11 nM). SAR analysis indicated, that an exchange of oxygen to selenium (7 vs. 22), and especially, to sulfur (7 vs. 19) was beneficial to increase both affinity and antagonistic action for 5-HT6R. Surprisingly, an introduction of SO2 caused a drastic decrease of the 5-HT6R affinity, which was explained at a molecular level based on docking studies. All in vivo tested compounds (10, 18 and 21) did not show any risk of toxicity in the safety studies in vitro." @default.
• W2949099935 created "2019-06-27" @default.
• W2949099935 creator A5003331896 @default.
• W2949099935 creator A5008486745 @default.
• W2949099935 creator A5010942734 @default.
• W2949099935 creator A5028320053 @default.
• W2949099935 creator A5028540077 @default.
• W2949099935 creator A5032411753 @default.
• W2949099935 creator A5035403793 @default.
• W2949099935 creator A5037054363 @default.
• W2949099935 creator A5038634831 @default.
• W2949099935 creator A5048295093 @default.
• W2949099935 creator A5058388777 @default.
• W2949099935 creator A5060640473 @default.
• W2949099935 creator A5064011310 @default.
• W2949099935 creator A5067048725 @default.
• W2949099935 creator A5071406940 @default.
• W2949099935 creator A5081072732 @default.
• W2949099935 creator A5085355095 @default.
• W2949099935 creator A5088814932 @default.
• W2949099935 date "2019-09-01" @default.
• W2949099935 modified "2023-10-17" @default.
• W2949099935 title "Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT6" @default.
• W2949099935 cites W1967844645 @default.
• W2949099935 cites W1970706983 @default.
• W2949099935 cites W1979420282 @default.
• W2949099935 cites W1981482395 @default.
• W2949099935 cites W1990138922 @default.
• W2949099935 cites W1998211867 @default.
• W2949099935 cites W2003363126 @default.
• W2949099935 cites W2009551881 @default.
• W2949099935 cites W2016783112 @default.
• W2949099935 cites W2047905218 @default.
• W2949099935 cites W2057485900 @default.
• W2949099935 cites W2062495736 @default.
• W2949099935 cites W2070703400 @default.
• W2949099935 cites W2072859799 @default.
• W2949099935 cites W2074631079 @default.
• W2949099935 cites W2090829498 @default.
• W2949099935 cites W2102729078 @default.
• W2949099935 cites W2134433202 @default.
• W2949099935 cites W2192084687 @default.
• W2949099935 cites W2222589778 @default.
• W2949099935 cites W2338880661 @default.
• W2949099935 cites W2339439476 @default.
• W2949099935 cites W2606727359 @default.
• W2949099935 cites W2618256032 @default.
• W2949099935 cites W2734366189 @default.
• W2949099935 cites W2753063582 @default.
• W2949099935 cites W2767052958 @default.
• W2949099935 cites W2771668368 @default.
• W2949099935 cites W2781718743 @default.
• W2949099935 cites W2786547465 @default.
• W2949099935 cites W2787867420 @default.
• W2949099935 cites W2789692188 @default.
• W2949099935 cites W2806149887 @default.
• W2949099935 cites W2808749151 @default.
• W2949099935 cites W2895330513 @default.
• W2949099935 cites W2066105708 @default.
• W2949099935 doi "https://doi.org/10.1016/j.ejmech.2019.06.022" @default.
• W2949099935 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31229876" @default.
• W2949099935 hasPublicationYear "2019" @default.
• W2949099935 type Work @default.
• W2949099935 sameAs 2949099935 @default.
• W2949099935 citedByCount "16" @default.
• W2949099935 countsByYear W29490999352019 @default.
• W2949099935 countsByYear W29490999352020 @default.
• W2949099935 countsByYear W29490999352021 @default.
• W2949099935 countsByYear W29490999352022 @default.
• W2949099935 countsByYear W29490999352023 @default.
• W2949099935 crossrefType "journal-article" @default.
• W2949099935 hasAuthorship W2949099935A5003331896 @default.
• W2949099935 hasAuthorship W2949099935A5008486745 @default.
• W2949099935 hasAuthorship W2949099935A5010942734 @default.
• W2949099935 hasAuthorship W2949099935A5028320053 @default.
• W2949099935 hasAuthorship W2949099935A5028540077 @default.
• W2949099935 hasAuthorship W2949099935A5032411753 @default.
• W2949099935 hasAuthorship W2949099935A5035403793 @default.
• W2949099935 hasAuthorship W2949099935A5037054363 @default.
• W2949099935 hasAuthorship W2949099935A5038634831 @default.
• W2949099935 hasAuthorship W2949099935A5048295093 @default.
• W2949099935 hasAuthorship W2949099935A5058388777 @default.
• W2949099935 hasAuthorship W2949099935A5060640473 @default.
• W2949099935 hasAuthorship W2949099935A5064011310 @default.
• W2949099935 hasAuthorship W2949099935A5067048725 @default.
• W2949099935 hasAuthorship W2949099935A5071406940 @default.
• W2949099935 hasAuthorship W2949099935A5081072732 @default.
• W2949099935 hasAuthorship W2949099935A5085355095 @default.
• W2949099935 hasAuthorship W2949099935A5088814932 @default.
• W2949099935 hasConcept C116073593 @default.
• W2949099935 hasConcept C150903083 @default.
• W2949099935 hasConcept C159110408 @default.
• W2949099935 hasConcept C178790620 @default.
• W2949099935 hasConcept C185592680 @default.
• W2949099935 hasConcept C202751555 @default.
• W2949099935 hasConcept C207001950 @default.
• W2949099935 hasConcept C21951064 @default.
• W2949099935 hasConcept C2776303721 @default.

• next