Diversity-oriented synthesis of spiro-substituted 1,3-thiazine library via a one-pot, two-step, three-component reaction.

abstract：:Yeast surface display empowers selection of protein binding ligands, typically using recombinant soluble antigens. However, ectodomain fragments of transmembrane targets may fail to recapitulate their true, membrane-bound form. Direct selections against adhered mammalian cells empower enrichment of genuine binders yet...

journal_title：ACS combinatorial science

authors： Lown PS,Hackel BJ

更新日期：2020-05-11 00:00:00

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

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

abstract：:We report the first example of venting-while-heating microwave-assisted synthesis of a small library of 3-arylthioindoles. Compounds were prepared in excellent isolated yields (90-98%) within 4 min in a closed vessel by treating indoles with disulfides in the presence of sodium hydride in anhydrous N,N-dimethylformami...

journal_title：ACS combinatorial science

authors： La Regina G,Gatti V,Famiglini V,Piscitelli F,Silvestri R

更新日期：2012-04-09 00:00:00

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

authors： Fujimoto K,Aimi A,Maruyama S

更新日期：2020-12-14 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

authors： Srivastava A,Aggarwal L,Jain N

更新日期：2015-01-12 00:00:00

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

authors： Johnson ID,Loveridge M,Bhagat R,Darr JA

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

authors： Alexandrakis V,Wallisch W,Hamann S,Varvaro G,Fidler J,Ludwig A

更新日期：2015-11-09 00:00:00

abstract：:This work presents the first use of yeast-displayed protein targets for screening mRNA-display libraries of cyclic and linear peptides. The WW domains of Yes-Associated Protein 1 (WW-YAP) and mitochondrial import receptor subunit TOM22 were adopted as protein targets. Yeast cells displaying WW-YAP or TOM22 were magnet...

journal_title：ACS combinatorial science

authors： Bacon K,Bowen J,Reese H,Rao BM,Menegatti S

更新日期：2020-12-14 00:00:00

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

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

更新日期：2015-03-09 00:00:00

abstract：:A one-pot parallel synthesis of N(1)-aryl-N(2)-alkyl-substituted oxamides with 2,2,2-trifluoroethyl chlorooxoacetate was developed. The synthesis of a library of 45 oxamides revealed higher efficiency of this reagent over the known ethyl chlorooxoacetate. The reagent was successfully used to prepare the known oxamide-...

journal_title：ACS combinatorial science

authors： Bogolubsky AV,Moroz YS,Mykhailiuk PK,Pipko SE,Zhemera AV,Konovets AI,Stepaniuk OO,Myronchuk IS,Dmytriv YV,Doroschuk RA,Zaporozhets OA,Tolmachev A

更新日期：2015-10-12 00:00:00

abstract：:A novel parallel medicinal chemistry (PMC)-enabled synthesis of 1H-pyrazolo[3,4-d]pyrimidines employing condensation of easily accessible N-pyrazolylamides and nitriles has been developed. The presented studies describe singleton and library enablements that allowed rapid generation of molecular diversity to examine C...

journal_title：ACS combinatorial science

authors： Shah AA,Chenard LK,Tucker JW,Helal CJ

更新日期：2017-11-13 00:00:00

abstract：:Preparative RP-LCMS is widely used to purify compounds from crude reaction mixtures in drug discovery today. Method development for preparative Liquid Chromatography-Mass Spectrometry (LCMS) consists of finding the right balance between speed and quality, often leading to the use of fast generic gradients (5-95% organ...

journal_title：ACS combinatorial science

authors： Koza P,Gonnot V,Pelleter J

更新日期：2012-04-09 00:00:00

abstract：:A potentiometric Pb(II)-selective sensor was fabricated by a combinatorial screening of electrically conducting polysulfoaminoanthraquinone (PSA) nanoparticles as a solid ionophore, ion exchangers (oleic acid (OA) and NaTPB), plasticizers in a polyvinyl chloride (PVC) matrix, membrane thickness, inner filling ion spec...

journal_title：ACS combinatorial science

authors： Huang MR,Ding YB,Li XG

更新日期：2014-03-10 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

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

abstract：:This paper describes the synthesis of a 300 member library of 3,5-substituted enones. The synthesis starts with 6 different bromoenones that are accessed from the corresponding 1,3 diones. These bromides are then diversified by Suzuki coupling with a variety of aromatic and vinyl boronic acids. Additionally a small se...

journal_title：ACS combinatorial science

authors： Khalaf J,Estrella-Jimenez ME,Shashack MJ,Phatak SS,Zhang S,Gilbertson SR

更新日期：2011-07-11 00:00:00

abstract：:An unprecedented three-component C(sp(3))-H functionalization of 2-alkylazaarenes with aryl aldehydes and 4-hydroxycoumarins was realized, providing azaarene-substituted 3-benzyl-4-hydroxycoumarins in good to excellent yields. These new target compounds displayed broad-spectrum antibacterial activities, providing a ne...

journal_title：ACS combinatorial science

authors： Dong H,Xu L,Li SS,Wang L,Shao CL,Xiao J

更新日期：2016-09-12 00:00:00

abstract：:Combinatorial synthesis of Li-ion batteries has proven extremely powerful in screening complex compositional spaces for next-generation materials. To date, no Na-ion counterpart exists wherein Na-ion cathodes can be synthesized in such a way to be comparable to that obtained in bulk synthesis. Herein, we develop a syn...

journal_title：ACS combinatorial science

authors： Adhikari T,Hebert A,Adamič M,Yao J,Potts K,McCalla E

更新日期：2020-06-08 00:00:00

abstract：:We report the parallel synthesis of a series of novel 4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-3-ium chloride salts, which are analogs to cationic anthraquinones. Three synthetic protocols were examined leading to a convenient and facile library synthesis of the cationic anthraquinone analogs that contain...

journal_title：ACS combinatorial science

authors： Fosso MY,Chan KY,Gregory R,Chang CW

更新日期：2012-03-12 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

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

更新日期：2018-03-12 00:00:00

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

authors： Méndez L,Mata EG

更新日期：2015-02-09 00:00:00

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) an...

journal_title：ACS combinatorial science

authors： Li J,Wang J,Xu Z,Zhu S

更新日期：2014-09-08 00:00:00

abstract：:The possibility of band gap engineering in graphene opens countless new opportunities for application in nanoelectronics. In this work, the energy gaps of 622 computationally optimized graphene nanoflakes were mapped to topological autocorrelation vectors using machine learning techniques. Machine learning modeling re...

journal_title：ACS combinatorial science

authors： Fernandez M,Abreu JI,Shi H,Barnard AS

更新日期：2016-11-14 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

authors： Tapp MJN,Slocik JM,Dennis PB,Naik RR,Milam VT

更新日期：2018-10-08 00:00:00

abstract：:The Au-Al alloy system was investigated via a combinatorial thin film sputtering method for its potential as a plasmonic material. Au xAl1- x combinatorial libraries were cosputtered from Au and Al elemental targets and the composition, phase, and dielectric function of a ∼350 nm film was determined using energy dispe...

journal_title：ACS combinatorial science

authors： Collette R,Wu Y,Olafsson A,Camden JP,Rack PD

更新日期：2018-11-12 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

authors： Xie YJ,Sun J,Yan CG

更新日期：2014-06-09 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

authors： Burlingame MA,Tom CT,Renslo AR

更新日期：2011-05-09 00:00:00

abstract：:A build/couple/pair strategy for the synthesis of complex and densely functionalized small molecules is presented. The strategy relies on synthetically tractable building blocks (build), that is, diversely substituted hydrazides, α-hydroxy aldehydes, and boronic acids, which undergo Petasis 3-component reactions (coup...

journal_title：ACS combinatorial science

authors： Flagstad T,Hansen MR,Le Quement ST,Givskov M,Nielsen TE

更新日期：2015-01-12 00:00:00

abstract：:Ultrasound-assisted synthesis of benzimidazo[2,1-b]quinazolin-1(1H)-ones was achieved via piperidine-catalyzed three-component reaction of 2-aminobenzimidazoles, an aromatic aldehyde, and 1,3-dione in aqueous isopropanol. This mechanism was first suspected following our identification of unusual reaction intermediates...

journal_title：ACS combinatorial science

authors： Chen LH,Chung TW,Narhe BD,Sun CM

更新日期：2016-03-14 00:00:00

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

authors： Bharate JB,Bharate SB,Vishwakarma RA

更新日期：2014-11-10 00:00:00

abstract：:The exploration of new alloys with desirable properties has been a long-standing challenge in materials science because of the complex relationship between composition and microstructure. In this Research Article, we demonstrate a combinatorial strategy for the exploration of composition dependence of microstructure. ...

journal_title：ACS combinatorial science

authors： Li Y,Jensen KE,Liu Y,Liu J,Gong P,Scanley BE,Broadbridge CC,Schroers J

更新日期：2016-10-10 00:00:00