FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2461223705> ?p ?o ?g. }

• W2461223705 endingPage "1567" @default.
• W2461223705 startingPage "1551" @default.
• W2461223705 abstract "A series of 2-amino-6-nitrobenzothiazole-derived extended hydrazones were designed, synthesized, and investigated for their ability to inhibit monoamine oxidase A and B (MAO-A/MAO-B). The compounds were found to exhibit inhibitory activities in the nanomolar to micromolar range. Some of the compounds showed excellent potency and selectivity against the MAO-B isoform. N′-(5-Chloro-2-oxoindolin-3-ylidene)-2-(6-nitrobenzothiazol-2-ylamino)acetohydrazide (compound 31) showed the highest MAO-B inhibitory activity (IC50=1.8±0.3 nm, selectivity index [SI]=766.67), whereas compound 6 [N′-(1-(4-bromophenyl)ethylidene)-2-(6-nitrobenzothiazol-2-ylamino)acetohydrazide] was found to be the most active MAO-A inhibitor (IC50=0.42±0.003 μm). Kinetic studies revealed that compounds 6 and 31 exhibit competitive-type reversible inhibition against both MAO-A and MAO-B, respectively. Structure–activity relationship (SAR) studies disclosed several structural aspects significant for potency and the contribution of the methylene spacer toward MAO-B inhibitory potency, with minimal or no neurotoxicity. Molecular modeling studies yielded a good correlation between experimental and theoretical inhibitory data. Binding pose analysis revealed the significance of cumulative effects of π–π stacking and hydrogen bond interactions for effective stabilization of virtual ligand–protein complexes. Further optimization studies of compound 31, including co-crystallization of inhibitor–MAO-B complexes, are essential to develop these compounds as potential therapeutic agents for MAO-B-associated neurodegenerative diseases." @default.
• W2461223705 created "2016-07-22" @default.
• W2461223705 creator A5029053728 @default.
• W2461223705 creator A5058849961 @default.
• W2461223705 date "2016-06-22" @default.
• W2461223705 modified "2023-09-30" @default.
• W2461223705 title "Design, Synthesis, and Evaluation of 2-Amino-6-nitrobenzothiazole-Derived Hydrazones as MAO Inhibitors: Role of the Methylene Spacer Group" @default.
• W2461223705 cites W1964511337 @default.
• W2461223705 cites W1964958542 @default.
• W2461223705 cites W1978071562 @default.
• W2461223705 cites W1983585951 @default.
• W2461223705 cites W1985048122 @default.
• W2461223705 cites W1987438183 @default.
• W2461223705 cites W2006911538 @default.
• W2461223705 cites W2007487695 @default.
• W2461223705 cites W2008440959 @default.
• W2461223705 cites W2012516949 @default.
• W2461223705 cites W2015764609 @default.
• W2461223705 cites W2037039276 @default.
• W2461223705 cites W2042386533 @default.
• W2461223705 cites W2042695207 @default.
• W2461223705 cites W2043812738 @default.
• W2461223705 cites W2046204255 @default.
• W2461223705 cites W2050864578 @default.
• W2461223705 cites W2054253103 @default.
• W2461223705 cites W2057885343 @default.
• W2461223705 cites W2059476028 @default.
• W2461223705 cites W2064579921 @default.
• W2461223705 cites W2066213050 @default.
• W2461223705 cites W2066786160 @default.
• W2461223705 cites W2082633706 @default.
• W2461223705 cites W2085580151 @default.
• W2461223705 cites W2115187133 @default.
• W2461223705 cites W2134996660 @default.
• W2461223705 cites W2135193909 @default.
• W2461223705 cites W2155633484 @default.
• W2461223705 cites W2159710882 @default.
• W2461223705 cites W2181180129 @default.
• W2461223705 cites W2323471917 @default.
• W2461223705 doi "https://doi.org/10.1002/cmdc.201600202" @default.
• W2461223705 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27332045" @default.
• W2461223705 hasPublicationYear "2016" @default.
• W2461223705 type Work @default.
• W2461223705 sameAs 2461223705 @default.
• W2461223705 citedByCount "21" @default.
• W2461223705 countsByYear W24612237052017 @default.
• W2461223705 countsByYear W24612237052018 @default.
• W2461223705 countsByYear W24612237052019 @default.
• W2461223705 countsByYear W24612237052020 @default.
• W2461223705 countsByYear W24612237052021 @default.
• W2461223705 countsByYear W24612237052022 @default.
• W2461223705 countsByYear W24612237052023 @default.
• W2461223705 crossrefType "journal-article" @default.
• W2461223705 hasAuthorship W2461223705A5029053728 @default.
• W2461223705 hasAuthorship W2461223705A5058849961 @default.
• W2461223705 hasConcept C112887158 @default.
• W2461223705 hasConcept C116569031 @default.
• W2461223705 hasConcept C118792377 @default.
• W2461223705 hasConcept C155647269 @default.
• W2461223705 hasConcept C161790260 @default.
• W2461223705 hasConcept C170493617 @default.
• W2461223705 hasConcept C178790620 @default.
• W2461223705 hasConcept C181199279 @default.
• W2461223705 hasConcept C185592680 @default.
• W2461223705 hasConcept C202751555 @default.
• W2461223705 hasConcept C2776024655 @default.
• W2461223705 hasConcept C2777454769 @default.
• W2461223705 hasConcept C2777752497 @default.
• W2461223705 hasConcept C32909587 @default.
• W2461223705 hasConcept C55493867 @default.
• W2461223705 hasConcept C57992300 @default.
• W2461223705 hasConcept C71240020 @default.
• W2461223705 hasConceptScore W2461223705C112887158 @default.
• W2461223705 hasConceptScore W2461223705C116569031 @default.
• W2461223705 hasConceptScore W2461223705C118792377 @default.
• W2461223705 hasConceptScore W2461223705C155647269 @default.
• W2461223705 hasConceptScore W2461223705C161790260 @default.
• W2461223705 hasConceptScore W2461223705C170493617 @default.
• W2461223705 hasConceptScore W2461223705C178790620 @default.
• W2461223705 hasConceptScore W2461223705C181199279 @default.
• W2461223705 hasConceptScore W2461223705C185592680 @default.
• W2461223705 hasConceptScore W2461223705C202751555 @default.
• W2461223705 hasConceptScore W2461223705C2776024655 @default.
• W2461223705 hasConceptScore W2461223705C2777454769 @default.
• W2461223705 hasConceptScore W2461223705C2777752497 @default.
• W2461223705 hasConceptScore W2461223705C32909587 @default.
• W2461223705 hasConceptScore W2461223705C55493867 @default.
• W2461223705 hasConceptScore W2461223705C57992300 @default.
• W2461223705 hasConceptScore W2461223705C71240020 @default.
• W2461223705 hasIssue "14" @default.
• W2461223705 hasLocation W24612237051 @default.
• W2461223705 hasLocation W24612237052 @default.
• W2461223705 hasOpenAccess W2461223705 @default.
• W2461223705 hasPrimaryLocation W24612237051 @default.
• W2461223705 hasRelatedWork W1928036484 @default.
• W2461223705 hasRelatedWork W1985341453 @default.
• W2461223705 hasRelatedWork W1986935641 @default.
• W2461223705 hasRelatedWork W2077472737 @default.

• next