P73803

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显示 1-30 共 49 条结果关于 "P73803" 范围论文

P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy.

Pieter Van der Veken et al.

Journal of medicinal chemistry, 55(22), 9856-9867 (2012-11-06)

We have investigated the effect of regiospecifically introducing substituents in the P2 part of the typical dipeptide derived basic structure of PREP inhibitors. This hitherto unexplored modification type can be used to improve target affinity, selectivity, and physicochemical parameters in

An RNA-seq screen of the Drosophila antenna identifies a transporter necessary for ammonia detection.

Karen Menuz et al.

PLoS genetics, 10(11), e1004810-e1004810 (2014-11-21)

Many insect vectors of disease detect their hosts through olfactory cues, and thus it is of great interest to understand better how odors are encoded. However, little is known about the molecular underpinnings that support the unique function of coeloconic

Attractors in Sequence Space: Peptide Morphing by Directed Simulated Evolution.

Jan A Hiss et al.

Molecular informatics, 34(11-12), 709-714 (2016-01-19)

Weak coordination of neutral S- and O-donor proximal ligands to a ferrous porphyrin nitrosyl. Characterization of 6-coordinate complexes at low T.

G G Martirosyan et al.

Journal of inorganic biochemistry, 121, 129-133 (2013-02-05)

The interaction of the S- and O-donor ligands tetrahydrothiophen (THT) and tetrahydrofuran (THF) with the ferrous nitrosyl complex Fe(TTP)(NO) (TTP(2-) is meso-tetra-p-tolyl-porphyrinatodianion) was studied at various temperatures both in solid state and solution using electronic and infrared absorption spectroscopy. Upon

Transition state analogues of Plasmodium falciparum and human orotate phosphoribosyltransferases.

Yong Zhang et al.

The Journal of biological chemistry, 288(48), 34746-34754 (2013-10-26)

The survival and proliferation of Plasmodium falciparum parasites and human cancer cells require de novo pyrimidine synthesis to supply RNA and DNA precursors. Orotate phosphoribosyltransferase (OPRT) is an indispensible component in this metabolic pathway and is a target for antimalarials

Highly enantioselective and recyclable organocatalytic Michael addition of malonates to α,β-unsaturated aldehydes in aqueous media.

Subrata K Ghosh et al.

Organic & biomolecular chemistry, 10(41), 8322-8325 (2012-09-15)

A new type of pyrrolidine-based organocatalyst, which was developed earlier in our lab, has been found to be very effective for the Michael addition reaction in aqueous solvents involving a wide range of α,β-unsaturated aldehydes and malonate derivatives. For the

Palladium catalyzed cyclizations of oxime esters with 1,1-disubstituted alkenes: synthesis of α,α-disubstituted dihydropyrroles and studies towards an asymmetric protocol.

Adele Faulkner et al.

Chemical communications (Cambridge, England), 49(15), 1521-1523 (2013-01-17)

We report efficient Pd-catalyzed cyclizations of oxime esters with 1,1-disubstituted alkenes as the basis of a general entry to α,α-disubstituted pyrrolidine derivatives. We also demonstrate that catalytic asymmetric variants of this chemistry are feasible by employing a suitable chiral ligand.

Synthesis and reduction kinetics of sterically shielded pyrrolidine nitroxides.

Joseph T Paletta et al.

Organic letters, 14(20), 5322-5325 (2012-10-12)

A series of sterically shielded pyrrolidine nitroxides were synthesized, and their reduction by ascorbate (vitamin C) indicate that nitroxide 3, a tetraethyl derivative of 3-carboxy-PROXYL, is reduced at the slowest rate among known nitroxides, i.e., at a 60-fold slower rate

Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.

Michael S Poslusney et al.

Bioorganic & medicinal chemistry letters, 23(6), 1860-1864 (2013-02-19)

This Letter describes the further optimization of an MLPCN probe molecule (ML137) through the introduction of 5- and 6-membered spirocycles in place of the isatin ketone. Interestingly divergent structure-activity relationships, when compared to earlier M1 PAMs, are presented. These novel

Isolation, identification and antimicrobial activities of two secondary metabolites of Talaromyces verruculosus.

Fang Miao et al.

Molecules (Basel, Switzerland), 17(12), 14091-14098 (2012-11-30)

From the ethyl acetate extract of the culture broth of Talaromyces verruculosus, a rhizosphere fungus of Stellera chamaejasme L., (-)-8-hydroxy-3-(4-hydroxypentyl)-3,4-dihydroisocoumarin (1) and (E)-3-(2,5-dioxo-3-(propan-2-ylidene)pyrrolidin-1-yl)acrylic acid (2) were isolated and evaluated for their antimicrobial activities. Their structures were elucidated by UV, IR

Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human.

Raman Sharma et al.

Drug metabolism and disposition: the biological fate of chemicals, 40(11), 2143-2161 (2012-08-17)

The disposition of 3,3-difluoropyrrolidin-1-yl{(2S,4S)-4-[4-(pyrimidin-2-yl)piperazin-1-yl]pyrrolidin-2-yl}methanone (PF-00734200), a dipeptidyl peptidase IV inhibitor that progressed to phase 3 for the treatment of type 2 diabetes, was examined in rats, dogs, and humans after oral administration of a single dose of [(14)C]PF-00734200. Mean recoveries

Spiro-fused pyrrolidine, piperidine, and oxindole scaffolds from lactams.

Christoph Hirschhäuser et al.

Organic letters, 14(18), 4846-4849 (2012-09-06)

Expedient routes to three classes of novel spiro-fused pyrrolidine, piperidine, and indoline heterocycle scaffolds are described. These three-dimensional frameworks, which conform to the "rule of three", are suitably protected to allow for site-selective manipulation and functionalization. Different modes of substrate

The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.

Edwige Lorthiois et al.

Journal of medicinal chemistry, 56(6), 2207-2217 (2013-02-22)

The small-molecule trans-3,4-disubstituted pyrrolidine 6 was identified from in silico three-dimensional (3D) pharmacophore searches based on known X-ray structures of renin-inhibitor complexes and demonstrated to be a weakly active inhibitor of the human enzyme. The unexpected binding mode of the

Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.

Thomas V Magee et al.

Bioorganic & medicinal chemistry letters, 23(6), 1727-1731 (2013-02-19)

A novel series of 3-O-carbamoyl erythromycin A derived analogs, labeled carbamolides, with activity versus resistant bacterial isolates of staphylococci (including macrolide and oxazolidinone resistant strains) and streptococci are reported. An (R)-2-aryl substituent on a pyrrolidine carbamate appeared to be critical

Rescue of notch-1 signaling in antigen-specific CD8+ T cells overcomes tumor-induced T-cell suppression and enhances immunotherapy in cancer.

Rosa A Sierra et al.

Cancer immunology research, 2(8), 800-811 (2014-05-17)

An impaired antitumor immunity is found in patients with cancer and represents a major obstacle in the successful development of different forms of immunotherapy. Signaling through Notch receptors regulates the differentiation and function of many cell types, including immune cells.

Preparation of N-Sulfinyl Aldimines using Pyrrolidine as Catalyst via Iminium Ion Activation

Morales S, et al.

Organic Syntheses, 94, 346-346 (2017)

New directions in thermoresponsive polymers.

Debashish Roy et al.

Chemical Society reviews, 42(17), 7214-7243 (2013-03-02)

Interest in thermoresponsive polymers has steadily grown over many decades, and a great deal of work has been dedicated to developing temperature sensitive macromolecules that can be crafted into new smart materials. However, the overwhelming majority of previously reported temperature-responsive

Electrospray ionization mass spectrometry of non-covalent complexes formed between N-alkylimidazolium-containing zwitterionic sulfonates and protonated bases.

Anton Podjava et al.

European journal of mass spectrometry (Chichester, England), 20(6), 467-475 (2014-01-01)

This paper describes non-covalent complexes between zwitterionic 3-(1-alkyl-3N-imidazolio)- propane-1-sulfonates and different amines. Electrospray ionization (ESI) mass spectrometry and collision- induced dissociation were used to measure the stability of such complexes in solution and in the gas phase. Generally, zwitterionic sulfonates

Virtual screening and QSAR study of some pyrrolidine derivatives as α-mannosidase inhibitors for binding feature analysis.

N S H N Moorthy et al.

Bioorganic & medicinal chemistry, 20(24), 6945-6959 (2012-11-16)

Virtual screening and QSAR analysis were carried out to investigate the binding features of (2R, 3R, 4S)-2-aminomethylpyrrolidine 3,4-diol and the functionalized pyrrolidine derivatives to the α-mannosidase I and II enzymes. The QSAR models (possessed considerable R(2), Q(2) values, etc.) suggested

Metabolic Disposition and Elimination of Cyadox in Pigs, Chickens, Carp, and Rats.

Huang Lingli et al.

Journal of agricultural and food chemistry, 63(22), 5557-5569 (2015-05-15)

The metabolism, distribution, and elimination of cyadox (CYA) is investigated in pigs, chickens, carp, and rats to identify the marker residue and target tissue of CYA in food animals for food safety concerns. Following a single oral gavage of [(3)H]-CYA

Enantioselective construction of a polyhydroxylated pyrrolidine skeleton from 3-vinylaziridine-2-carboxylates: synthesis of (+)-DMDP and a potential common intermediate for (+)-hyacinthacine A1 and (+)-1-epi-australine.

Yukari Kondo et al.

The Journal of organic chemistry, 77(18), 7988-7999 (2012-08-18)

We report an enantioselective synthesis of the polyhydroxylated pyrrolidine alkaloid (+)-DMDP. The key steps in the synthesis were guanidinium ylide mediated asymmetric aziridination, stereospecific ring opening of trans-3-vinylaziridine-2-carboxylate with an oxygen nucleophile, iodine-mediated 5-endo-trig amino cyclization, and Prévost displacement. In

Synthesis and characterization of novel soluble fulleropyrrolidine derivatives and their photovoltaic performance.

Dongbo Mi et al.

Journal of nanoscience and nanotechnology, 13(5), 3474-3479 (2013-07-19)

Currently, [60] fullerene derivatives are the focus of considerable research due to their important roles in many fields, especially material science. In this study, we synthesized the following two novel fulleropyrrolidine derivatives: C60-fused N-methyl-(4-hexyloxybenzen-2-yl) pyrrolidine, (p-HOPF) and C60-fused N-methyl-(2-hexyloxybenzen-2-yl) pyrrolidine

Fulvic acid attenuates homocysteine-induced cyclooxygenase-2 expression in human monocytes.

Shao-Ju Chien et al.

BMC complementary and alternative medicine, 15, 61-61 (2015-04-19)

Homocysteine and pro-inflammatory mediators such as cyclooxygenase-2 (COX-2) have been linked to vascular dysfunction and risks of cardiovascular diseases. Fulvic acid (FA), a class of compounds of humic substances, possesses various pharmacological properties. However, the effect of FA on inflammatory

o-Aminobenzaldehyde, Redox-Neutral Aminal Formation and Synthesis of Deoxyvasicinone

Zhang C, et al.

Organic Syntheses, 89, 274-274 (2012)

Prediction of the chromatographic retention of acid-base compounds in pH buffered methanol-water mobile phases in gradient mode by a simplified model.

Axel Andrés et al.

Journal of chromatography. A, 1385, 42-48 (2015-02-11)

Retention of ionizable analytes under gradient elution depends on the pH of the mobile phase, the pKa of the analyte and their evolution along the programmed gradient. In previous work, a model depending on two fitting parameters was recommended because

Synthesis of 2,5-bis(spirocyclohexane)-substituted nitroxides of pyrroline and pyrrolidine series, including thiol-specific spin label: an analogue of MTSSL with long relaxation time.

Igor A Kirilyuk et al.

The Journal of organic chemistry, 77(18), 8016-8027 (2012-08-25)

The nitroxides of 7-azadispiro[5.1.5.2]pentadecane and 7-azadispiro[5.1.5.2]pentadeca-14-ene series have been prepared, including thiol-specific methane thiosulfonate spin label for site-directed spin labeling. The effect of spirocyclohexane moieties on chemical and spectral properties has been studied. The obtained temperature dependencies of electron spin

Three-dimensional quantitative structure-activity relationship analyses of substrates of the human proton-coupled amino acid transporter 1 (hPAT1).

Iris Thondorf et al.

Bioorganic & medicinal chemistry, 19(21), 6409-6418 (2011-10-01)

The proton-coupled amino acid transporter hPAT1 has recently gained much interest due to its ability to transport small drugs thereby allowing their oral administration. A three-dimensional quantitative structure-activity relationship (3D QSAR) study has been performed on its natural and synthetic

Evaluation of mutagenic and antimutagenic properties of new derivatives of pyrrolidine-2,5-dione with anti-epileptic activity, by use of the Vibrio harveyi mutagenicity test.

Elżbieta Pękala et al.

Mutation research, 758(1-2), 18-22 (2013-09-26)

The Vibrio harveyi test was used to evaluate mutagenic and antimutagenic properties of nineteen new derivatives of pyrrolidine-2,5-dione (compounds 1-19) with antiepileptic activity. Four V. harveyi strains were used: BB7 (wild type) and the genetically modified strains BB7M, BB7X and

Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists.

Aiko Nitta et al.

Bioorganic & medicinal chemistry letters, 22(22), 6876-6881 (2012-10-11)

Optimization starting with our lead compound 1 (IC(50)=4.9 nM) led to the identification of pyrrolidinyl phenylurea derivatives. Further modification toward improvement of the bioavailability provided (R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrrolidin-3-yl)-3-(2-(2-hydroxyethoxy)phenyl)urea 32 (IC(50)=1.7 nM), a potent and orally active CCR3 antagonist.

Pyrrolidine in drug discovery: a versatile scaffold for novel biologically active compounds

Li Petri G, et al.

Topics in Current Chemistry, 379, 1-46 (2021)

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