Abstract:
:A series of diverse polycyclic heterocycles containing spirooxindole, pyridine/thiophene, and pyrrolidine/pyrrolizidine/pyrrolothiazole rings have been synthesized through the 1,3-dipolar cycloaddition of azomethine ylides generated in situ by the condensation of dicarbonyl compounds (isatin or acenaphthenequinone) and secondary amino acids with dipolarophiles. The method is simple and provides diverse and biologically interesting products with excellent yields.
journal_name
ACS Comb Scijournal_title
ACS combinatorial scienceauthors
Li J,Wang J,Xu Z,Zhu Sdoi
10.1021/co500085tsubject
Has Abstractpub_date
2014-09-08 00:00:00pages
506-12issue
9eissn
2156-8952issn
2156-8944journal_volume
16pub_type
杂志文章abstract::A series of LiMn1-x-yFexVyPO4 (LMFVP) nanomaterials have been synthesized using a pilot-scale continuous hydrothermal synthesis process (CHFS) and evaluated as high voltage cathodes in Li-ion batteries at a production rate of 0.25 kg h-1. The rapid synthesis and screening approach has allowed the specific capacity of ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00035
更新日期:2016-11-14 00:00:00
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
更新日期:2019-12-09 00:00:00
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
更新日期:2017-07-10 00:00:00
abstract::Individually, benzoxazole and triazole moieties are of significant biological interest owing to their importance in drugs and pharmaceuticals. To assess their combined biological impact when woven into one molecule, we designed a novel, regioselective, multicomponent, one-pot (MCOP) approach for the construction of be...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500135z
更新日期:2015-01-12 00:00:00
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
更新日期:2019-12-09 00:00:00
abstract::A novel method of evaluating the enantioselectivity of chiral receptors is investigated. It involves extraction of an ionic guest in racemic form from an ion-exchange resin to the organic solvent, where it is bound by a chiral receptor. The enantioselectivity of the examined receptor is determined simply by measuring ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.5b00075
更新日期:2015-09-14 00:00:00
abstract::Retinoic acid (RA) is a key metabolite necessary for embryonic development and differentiation in vertebrates. We demonstrate the utility of genetically encoded, ligand-activatable single-chain bioluminescence probes for detecting RAs from different biological sources. We examined 13 different molecular designs to ide...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.9b00035
更新日期:2019-06-10 00:00:00
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
更新日期:2012-08-13 00:00:00
abstract::A build/couple/pair (B/C/P) strategy was employed to generate a library of 7936 stereochemically diverse 12-membered macrolactams. All 8 stereoisomers of a common linear amine precursor were elaborated to form the corresponding 8 stereoisomers of two regioisomeric macrocyclic scaffolds via head-to-tail cyclization. Su...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co200161z
更新日期:2012-02-13 00:00:00
abstract::High-throughput experimentation provides efficient mapping of composition-property relationships, and its implementation for the discovery of optical materials enables advancements in solar energy and other technologies. In a high throughput pipeline, automated data processing algorithms are often required to match ex...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00053
更新日期:2016-11-14 00:00:00
abstract::A Fe-Co-Nb thin film materials library was deposited by combinatorial magnetron sputtering and investigated by high-throughput methods to identify new noncubic ferromagnetic phases, indicating that combinatorial experimentation is an efficient method to discover new ferromagnetic phases adequate for permanent magnet a...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.5b00116
更新日期:2015-11-09 00:00:00
abstract::An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido[2,3-b][1,4]benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460TaxR (EC50 < 1.0 μ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00010
更新日期:2016-05-09 00:00:00
abstract::Under the acidic conditions, substituted furans were constructed from γ-alkynyl ketones through corresponding allene intermediates in one-pot. The methodology was also tailored to a series of the Ugi reaction products for the synthesis of 6-methylpyrazin-2(1 H)-one derivatives. The current method offered significant a...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.8b00005
更新日期:2018-05-14 00:00:00
abstract::A one-pot, three-component synthesis of benzimidazole-linked thiazolidines from 2-cyanomethyl benzimidazole, iso-, isothio-, or isoselenocyanates and 1,2-dichloroethane is reported. Isolation of the key intermediate formed during the course of the reaction validates its mechanistic pathway. Under the same reaction con...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.9b00161
更新日期:2020-01-13 00:00:00
abstract::The reactions of vinyl malononitriles with 3-phenacylideneoxindoles in ethanol in the presence of DBU as base resulted in the functionalized spirocyclic oxindoles through the domino Michael addition and intramolecular nucleophilic addition to cyano group. On the other hand, the similar reaction in the presence of pipe...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500006c
更新日期:2014-06-09 00:00:00
abstract::Parallel solution-phase synthesis of combinatorial libraries of dihydroindenoisoquinolines employing a sequential Cu(I)/Pd(0)-catalyzed multicomponent coupling and annulation protocol was realized. The scope and limitations of the protocol with respect to the substitution pattern in the aryl ring of the indene core, a...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co200027c
更新日期:2011-09-12 00:00:00
abstract::Competition-enhanced ligand screening (CompELS) was employed to rapidly screen through large DNA libraries to identify single-stranded, oligonucleotide-based ligands called aptamers that bind to a nonbiological target. This previously unreported aptamer screening approach involves the repeated introduction of unenrich...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.8b00048
更新日期:2018-10-08 00:00:00
abstract::A novel immobilized N-chlorosuccinimide resin was developed for peptide disulfide bond formation in combinatorial libraries. The resin is prepared in a simple two-step process from commercial starting materials. Disulfide formation is initiated by adding a peptide solution to the resin, and excess reagent is removed b...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500003p
更新日期:2014-04-14 00:00:00
abstract::A novel three-component, two-step, one-pot nucleophilic aromatic substitution (SNAr)-intramolecular cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). On the basis of the new efficiently convergent synthetic route, a library of Torin analogs was synth...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.7b00119
更新日期:2017-12-11 00:00:00
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
更新日期:2019-05-13 00:00:00
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
更新日期:2016-05-09 00:00:00
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
更新日期:2020-12-14 00:00:00
abstract::3-Substituted 4-quinolones were synthesized using a one-pot metal-free strategy in moderate to quantitative yields. Carried out in dimethylsulfoxide (DMSO) via a sequential addition of materials, the methodology is tolerant of a wide range of functional groups and applicable to library synthesis. ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co1000103
更新日期:2011-01-10 00:00:00
abstract::DNA-encoded synthesis is rekindling interest in combinatorial compound libraries for drug discovery and in technology for automated and quantitative library screening. Here, we disclose a microfluidic circuit that enables functional screens of DNA-encoded compound beads. The device carries out library bead distributio...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00192
更新日期:2017-03-13 00:00:00
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
更新日期:2011-05-09 00:00:00
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
更新日期:2020-12-14 00:00:00
abstract::A microgradient-heater (MGH) was developed, and its feasibility as a tool for high-throughput materials science experimentation was tested. The MGH is derived from microhot plate (MHP) systems and allows combinatorial thermal processing on the micronano scale. The temperature gradient is adjustable by the substrate ma...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co3000488
更新日期:2012-10-08 00:00:00
abstract::We have achieved an efficient solution-phase parallel synthesis of a library of natural piper-amide-like compounds from the bifunctional β-phosphono-N-hydroxy-succinimidyl ester intermediate. The primary important feature in our study is the construction of natural-product-like molecules through the adaptation of soph...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co400003d
更新日期:2013-04-08 00:00:00
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
更新日期:2018-03-12 00:00:00
abstract::Acetylenic tertiary alcohols are well-known to be compounds that are biologically more stable than their corresponding secondary alcohols. The linkage of an acetylenic compound to a polymer support and further introduction of molecular diversity was found to be an interesting way to generate libraries of hydroxy acety...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co300034y
更新日期:2012-06-11 00:00:00