当前位置： SCI文献检索 > ACS Combinatorial Science期刊下所有文献 > (Hetero-)(arylidene)arylhydrazides as Multitarget-Directed Monoamine Oxidase Inhibitors.

(Hetero-)(arylidene)arylhydrazides as Multitarget-Directed Monoamine Oxidase Inhibitors.

Abstract：

:Fourteen (hetero-)(arylidene)arylhydrazide derivatives (ABH1-ABH14) were synthesized, and their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE) were evaluated. Compound ABH5 most potently inhibited MAO-B with an IC50 value of 0.025 ± 0.0019 μM; ABH2 and ABH3 exhibited high IC50 values as well. Most of the compounds weakly inhibited MAO-A, except ABH5 (IC50 = 3.31 ± 0.41 μM). Among the active compounds, ABH2 showed the highest selectivity index (SI) of 174 for MAO-B, followed by ABH5 (SI = 132). ABH3 and ABH5 effectively inhibited AChE with IC50 values of 15.7 ± 6.52 and 16.5 ± 7.29 μM, respectively, whereas the other compounds were weak inhibitors of AChE. ABH5 was shown to be a reversible competitive inhibitor for MAO-A and MAO-B with Ki values of 0.96 ± 0.19 and 0.024 ± 0.0077 μM, respectively, suggesting that this molecule can be considered as an interesting candidate for further development as a multitarget inhibitor relating to neurodegenerative disorders.

journal_name

ACS Comb Sci

journal_title

ACS combinatorial science

authors

Palakkathondi A,Oh JM,Dev S,Rangarajan TM,Kaipakasseri S,Kavully FS,Gambacorta N,Nicolotti O,Kim H,Mathew B

doi

10.1021/acscombsci.0c00136

subject

Has Abstract

pub_date

2020-11-09 00:00:00

pages

592-599

issue

11

eissn

2156-8952

issn

2156-8944

journal_volume

22

pub_type

杂志文章

相关文献

ACS Combinatorial Science文献大全
  • Solid-Phase Synthesis of Oligopeptides Containing Sterically Hindered Amino Acids on Nonswellable Resin Using 3-Nitro-1,2,4-triazol-1-yl-tris(pyrrolidin-1-yl)phosphonium Hexafluorophosphate (PyNTP) as the Condensing Reagent.

    abstract：:Peptides are still difficult to synthesize when they contain sterically hindered amino acids, such as α,α-disubstituted amino acids and N-substituted amino acids. In this study, solid-phase syntheses of oligopeptides containing multiple α-aminoisobutyric acid (Aib) residues were performed in high yields by using a non...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.7b00184

    authors： Hara RI,Mitsuhashi Y,Saito K,Maeda Y,Wada T

    更新日期：2018-03-12 00:00:00

  • Synthesis of a stereochemically diverse library of medium-sized lactams and sultams via S(N)Ar cycloetherification.

    abstract：:We have implemented an aldol-based "build/couple/pair" (B/C/P) strategy for the synthesis of stereochemically diverse 8-membered lactam and sultam scaffolds via S(N)Ar cycloetherification. Each scaffold contains two handles, an amine and aryl bromide, for solid-phase diversification via N-capping and Pd-mediated cross...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co2000218

    authors： Gerard B,Duvall JR,Lowe JT,Murillo T,Wei J,Akella LB,Marcaurelle LA

    更新日期：2011-07-11 00:00:00

  • Parallel synthesis of a desketoraloxifene analogue library via iodocyclization/palladium-catalyzed coupling.

    abstract：:For a future structure-activity relationship (SAR) study, a library of desketoraloxifene analogues has been prepared by parallel synthesis using iodocyclization and subsequent palladium-catalyzed coupling reactions. Points of desketoraloxifene diversification involve the two phenolic hydroxyl groups and the aliphatic ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co200090p

    authors： Cho CH,Jung DI,Neuenswander B,Larock RC

    更新日期：2011-09-12 00:00:00

  • Simple one-pot synthesis of disulfide fragments for use in disulfide-exchange screening.

    abstract：:Disulfide exchange screening is a method for evaluating the binding of small molecule fragments to proteins that have at least one accessible cysteine. While operationally simple, it does require a large library of small fragment molecules bearing disulfide-containing side chains. These specialized fragments are not a...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co200038g

    authors： Burlingame MA,Tom CT,Renslo AR

    更新日期：2011-05-09 00:00:00

  • Solid-supported cross-metathesis and a formal alkane metathesis for the generation of biologically relevant molecules.

    abstract：:Solid-phase synthetic strategies toward the generation of libraries of biologically relevant molecules were developed using olefin cross-metathesis as a key step. It is remarkably the formal alkane metathesis based on a one-pot, microwave-assisted, ruthenium-catalyzed cross-metathesis and reduction to obtain Csp3-Csp3...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co500176b

    authors： Méndez L,Mata EG

    更新日期：2015-02-09 00:00:00

  • Copper-catalyzed multicomponent coupling/cycloisomerization reaction between substituted 1-formyl-9H-β-carbolines, secondary amines, and substituted alkynes for the synthesis of substituted 3-aminoindolizino[8,7-b]indoles.

    abstract：:A copper-catalyzed efficient one step three component strategy for preparing a library of aminoindolizino[8,7-b]indoles from N-substituted 1-formyl-9H-β-carbolines, secondary amines, and substituted alkynes with high atom economy has been developed. ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co300123y

    authors： Dighe SU,Hutait S,Batra S

    更新日期：2012-12-10 00:00:00

  • Semiautomated Parallel RAFT Copolymerization of Isoprene with Glycidyl Methacrylate.

    abstract：:Copolymerization of isoprene (IP) with glycidyl methacrylate (GMA) was performed under RAFT (reversible addition-fragmentation chain-transfer) polymerization conditions in a platform for high-output experimentation. Covering the range between 1 and 0.2 molar fraction of IP in the feed, four sets of reactions were carr...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.9b00110

    authors： Rosales-Guzmán M,Pérez-Camacho O,Guerrero-Sánchez C,Harrisson S,Torres-Lubián R,Vitz J,Schubert US,Saldívar-Guerra E

    更新日期：2019-12-09 00:00:00

  • Polymer-supported stereoselective synthesis of tetrahydro-2H-oxazolo[3,2-a]pyrazin-5(3H)-ones from N-(2-oxo-ethyl)-derivatized dipeptides via eastbound iminiums.

    abstract：:Polymer-supported N-(2-oxo-ethyl)-derivatized Ser/Thr/Cys-containing dipeptides were synthesized and subjected to acid-mediated tandem N-acylium ion cyclization-nucleophilic addition to yield tetrahydro-2H-oxazolo[3,2-a]pyrazin-5(3H)-ones. The reaction conditions and building-block combinations for stereoselective syn...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co3001567

    authors： La Venia A,Dolenský B,Krchňák V

    更新日期：2013-03-11 00:00:00

  • Effects of the Ion to Growth Flux Ratio on the Constitution and Mechanical Properties of Cr1-x-Alx-N Thin Films.

    abstract：:Cr-Al-N thin film materials libraries were synthesized by combinatorial reactive high power impulse magnetron sputtering (HiPIMS). Different HiPIMS repetition frequencies and peak power densities were applied altering the ion to growth flux ratio. Moreover, time-resolved ion energy distribution functions were measured...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.9b00123

    authors： Banko L,Ries S,Grochla D,Arghavani M,Salomon S,Pfetzing-Micklich J,Kostka A,Rogalla D,Schulze J,Awakowicz P,Ludwig A

    更新日期：2019-12-09 00:00:00

  • Development of Measurement Tools for High-Throughput Experiments of Synchrotron Radiation XRD and XAFS on Powder Libraries.

    abstract：:We propose to minimize the sampling time for high-throughput measurements of powder X-ray diffraction (XRD) and X-ray absorption fine structure (XAFS) in synchrotron radiation. The conventional synchrotron radiation powder X-ray diffraction method requires filling of a capillary tube, but a structure-refining diffract...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.0c00174

    authors： Fujimoto K,Aimi A,Maruyama S

    更新日期：2020-12-14 00:00:00

  • A Novel pseudo-Four-Component Domino Reaction for the Synthesis of Naphtho[2,1-b]furan-2(1H)-ones Using a Nanocatalyst.

    abstract：:In this article, an original one-pot method is utilized to synthesize a variety of derivatives of naphtho[2,1-b]furan-2(1H)-one via a pseudo-four-component domino reaction of aryl aldehydes, acetic anhydride, hippuric acids, and 2-naphthols catalyzed by HSW@SPIONs. This reaction illustrates an array of attractive feat...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.5b00018

    authors： Salami-Ranjbaran E,Khosropour AR,Mohammadpoor-Baltork I,Moghadam M,Tangestaninejad S,Mirkhani V

    更新日期：2015-08-10 00:00:00

  • Ultrasound-assisted sequential multicomponent strategy for the combinatorial synthesis of novel coumarin hybrids.

    abstract：:The present investigation reports an easy access to a library of novel spiro-oxindole-pyrrolizine or pyrrolo[1,2-c]thiazole fused coumarin hybrid heterocycles through a one-pot sequential four-component reactions of 2,2-dimethyl-1,3-dioxane-4,6-dione, salicylaldehydes, isatins, and cyclic α-amino acids under ultrasoun...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co500092b

    authors： Kanchithalaivan S,Sumesh RV,Kumar RR

    更新日期：2014-10-13 00:00:00

  • Application of Silica-Supported Alkylating Reagents in a One-Pot, Sequential Protocol to Diverse Benzoxathiazepine 1,1-Dioxides.

    abstract：:Applications of silica-ROMP reagents in a one-pot, sequential protocol have been developed for the synthesis of a variety of diverse benzoxathiazepine 1,1-dioxides. This protocol includes sulfonylation, intramolecular SNAr, alkylation with silica-supported oligomeric benzyl (Si-OBPn) and triazole (Si-OTPn) phosphates,...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.6b00041

    authors： Faisal S,Maity PK,Zang Q,Samarakoon TB,Sourk RL,Hanson PR

    更新日期：2016-07-11 00:00:00

  • In Vitro Identification of the Hamiltonian Cycle Using a Circular Structure Assisted DNA Computer.

    abstract：:Adleman's illustration of molecular computing using DNA paved the way toward an entirely new direction of computing (Adleman, L. M. Science 1994, 266, 1021). The exponential time complex combinatorial problem on a traditional computer turns out to be a separation problem involving a polynomial number of steps in DNA c...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.9b00150

    authors： Sharma D,Ramteke M

    更新日期：2020-05-11 00:00:00

  • Evaluation of the Two-Dimensional Performances of Low Activity Planar Catalysts: Development and Validation of a True Scanning Reactor.

    abstract：:The development of a scanning reactor for planar catalysts is presented here. With respect to other existing models, this reactor is able to scan catalysts even with low turnover frequencies with a minimum sensed circular area of approximately 6 mm in diameter. The downstream gas analysis is performed with a quaprupol...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.5b00103

    authors： Marelli M,Nemenyi A,Dal Santo V,Psaro R,Ostinelli L,Monticelli D,Dossi C,Recchia S

    更新日期：2016-01-11 00:00:00

  • Compositionally Dependent Nonlinear Optical Bandgap Behavior of Mixed Anodic Oxides in Niobium-Titanium System.

    abstract：:Optical bandgap mapping of Nb-Ti mixed oxides anodically grown on a thin film parent metallic combinatorial library was performed via variable angle spectroscopic ellipsometry (VASE). A wide Nb-Ti compositional spread ranging from Nb-90 at.% Ti to Nb-15 at.% Ti deposited by cosputtering was used for this purpose. The ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.6b00162

    authors： Bleckenwegner P,Mardare CC,Cobet C,Kollender JP,Hassel AW,Mardare AI

    更新日期：2017-02-13 00:00:00

  • Exploring the First High-Entropy Thin Film Libraries: Composition Spread-Controlled Crystalline Structure.

    abstract：:Thin films of two types of high-entropy oxides (HEOs) have been deposited on 76.2 mm Si wafers using combinatorial sputter deposition. In one type of the oxides, (MgZnMnCoNi)O x , all the metals have a stable divalent oxidation state and similar cationic radii. In the second...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.0c00159

    authors： Nguyen TX,Su YH,Hattrick-Simpers J,Joress H,Nagata T,Chang KS,Sarker S,Mehta A,Ting JM

    更新日期：2020-12-14 00:00:00

  • Metal-free, ionic liquid-mediated synthesis of functionalized quinolines.

    abstract：:An expedient and metal-free synthetic protocol for construction of substituted quinolines has been developed from anilines and phenylacetaldehydes using imidazolium cation-based ionic liquids as the reaction medium. Mechanistic analysis indicated that the reaction occurs through C-C and C-N bond formation to produce i...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co500047w

    authors： Bharate JB,Bharate SB,Vishwakarma RA

    更新日期：2014-11-10 00:00:00

  • Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface.

    abstract：:Protein-protein interactions are generally challenging to target by small molecules. To address the challenge, we have used a multidisciplinary approach to identify small-molecule disruptors of protein-protein interactions that are mediated by SUMO (small ubiquitin-like modifier) proteins. SUMO modifications have emer...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co500181b

    authors： Alontaga AY,Li Y,Chen CH,Ma CT,Malany S,Key DE,Sergienko E,Sun Q,Whipple DA,Matharu DS,Li B,Vega R,Li YJ,Schoenen FJ,Blagg BS,Chung TD,Chen Y

    更新日期：2015-04-13 00:00:00

  • Screening Yeast Display Libraries against Magnetized Yeast Cell Targets Enables Efficient Isolation of Membrane Protein Binders.

    abstract：:When isolating binders from yeast displayed combinatorial libraries, a soluble, recombinantly expressed form of the target protein is typically utilized. As an alternative, we describe the use of target proteins displayed as surface fusions on magnetized yeast cells. In our strategy, the target protein is coexpressed ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.9b00147

    authors： Bacon K,Burroughs M,Blain A,Menegatti S,Rao BM

    更新日期：2019-12-09 00:00:00

  • Diversity-oriented synthesis of chromenes via metal-free domino reactions from ketones and phenols.

    abstract：:Functionalized chromenes have been synthesized via highly selective metal-free domino reactions from ketones and phenols. 2H-Chromenes, 4H-chromenes, spiran and benzocyclopentane can be respectively prepared starting from the corresponding cyclic ketones, aryl methyl ketones, acetone, and 3-pentanone. ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co3000506

    authors： Xue WJ,Li Q,Gao FF,Zhu YP,Wang JG,Zhang W,Wu AX

    更新日期：2012-08-13 00:00:00

  • Combinatorial Investigations of High Temperature CuNb Oxide Phases for Photoelectrochemical Water Splitting.

    abstract：:High-throughput combinatorial methods have been useful in identifying new oxide semiconductors with the potential to be applied to solar water splitting. Most of these techniques have been limited to producing and screening oxide phases formed at temperatures below approximately 550 °C. We report the development of a ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.5b00142

    authors： Skorupska K,Maggard PA,Eichberger R,Schwarzburg K,Shahbazi P,Zoellner B,Parkinson BA

    更新日期：2015-12-14 00:00:00

  • Regio- and stereoselective synthesis of a library of bioactive dispiro-oxindolo/acenaphthoquino andrographolides via 1,3-dipolar cycloaddition reaction under microwave irradiation.

    abstract：:Dispiro-pyrrolidino/pyrrolizidino fused oxindoles/acenaphthoquinones have been derived from andrographolide via azomethine ylide cycloaddition to the conjugated double-bond under microwave (MW) irradiation. The reactions are chemo-, stereo-, and regioselective in nature. Change in amino acid from sarcosine/N-benzyl gl...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co3001154

    authors： Hazra A,Bharitkar YP,Chakraborty D,Mondal SK,Singal N,Mondal S,Maity A,Paira R,Banerjee S,Mondal NB

    更新日期：2013-01-14 00:00:00

  • One-pot, three-component reaction using modified Julia reagents: a facile synthesis of 4,5-disubstituted 1,2,3-(NH)-triazoles in a wet organic solvent.

    abstract：:A new one-pot, three component reaction involving the use of Julia reagent, aldehyde, and sodium azide was developed for the efficient synthesis of N-unsubstituted 1,2,3-triazoles. This reaction could be carried out under mild reaction conditions without any precaution, and broad scope of substrates, both respect to J...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co5001597

    authors： Chai H,Guo R,Yin W,Cheng L,Liu R,Chu C

    更新日期：2015-03-09 00:00:00

  • Structural and Functional Properties of the Thin Film System Ti-Ni-Si.

    abstract：:The thin film system Ti-Ni-Si was investigated using methods of combinatorial materials science. A thin film composition spread library of the system was fabricated using combinatorial magnetron sputtering. The functional properties Seebeck coefficient, electrical resistivity, and luminance were determined using high-...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.8b00181

    authors： Wambach M,Ziolkowski P,Müller E,Ludwig A

    更新日期：2019-05-13 00:00:00

  • Geometrical Properties Can Predict CO2 and N2 Adsorption Performance of Metal-Organic Frameworks (MOFs) at Low Pressure.

    abstract：:Metal-organic frameworks (MOFs) are nanoporous materials with exceptional host-guest properties poised for groundbreaking innovations in gas separation applications according to high-throughput (HT) screening data. However, MOF structural libraries are nearly infinite in practice and so statistical and information tec...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.5b00188

    authors： Fernandez M,Barnard AS

    更新日期：2016-05-09 00:00:00

  • Dielectrophoretic Manipulation of Cancer Cells and Their Electrical Characterization.

    abstract：:Electromanipulation and electrical characterization of cancerous cells is becoming a topic of high interest as the results reported to date demonstrate a good differentiation among various types of cells from an electrical viewpoint. Dielectrophoresis and broadband dielectric spectroscopy are complementary tools for s...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.0c00109

    authors： Turcan I,Olariu MA

    更新日期：2020-11-09 00:00:00

  • Bi Alloying into Rare Earth Double Perovskites Enhances Synthesizability and Visible Light Absorption.

    abstract：:A high throughput combinatorial synthesis utilizing inkjet printing of precursor inks was used to rapidly evaluate Bi-alloying into double perovskite oxides for enhanced visible light absorption. The fast visual screening of photo image scans of the library plates identifies 4-metal oxide compositions displaying an in...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.0c00177

    authors： Newhouse PF,Zhou L,Umehara M,Boyd DA,Soedarmadji E,Haber JA,Gregoire JM

    更新日期：2020-12-14 00:00:00

  • Facile (triazolyl)methylation of MACOS-derived benzofused sultams utilizing ROMP-derived OTP reagents.

    abstract：:A combination of MACOS scale-out and ROMP-derived oligomeric triazole phosphates (OTP(n)) have been successfully utilized for the preparation of a 106-member library of triazole containing benzothiaoxazepine-1,1-dioxides. This report demonstrates the utilization of a suite of soluble OTP(n) reagents for facile (triazo...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/co2001839

    authors： Faisal S,Ullah F,Maity PK,Rolfe A,Samarakoon TB,Porubsky P,Neuenswander B,Lushington GH,Basha FZ,Organ MG,Hanson PR

    更新日期：2012-04-09 00:00:00

  • Synthesis of Aminofuran-Linked Benzimidazoles and Cyanopyrrole-Fused Benzimidazoles by Condition-Based Skeletal Divergence.

    abstract：:A condition-based skeletal divergent synthesis was explored to achieve skeletal diversity in two component condensation reaction. Cyanomethyl benzimidazole was reacted with α-bromoketone under thermal conditions to furnish 2-aminofuranyl-benzimidazoles, while the same reaction afforded 3-cyano-benzopyrrolo-imidazoles ...

    journal_title：ACS combinatorial science

    pub_type： 杂志文章

    doi：10.1021/acscombsci.7b00052

    authors： Hsu WS,Tsai MH,Barve IJ,Yellol GS,Sun CM

    更新日期：2017-07-10 00:00:00