Design, synthesis, and in vitro antibacterial activity of fluoroquinolone derivatives containing a chiral 3-(alkoxyimino)-2-(aminomethyl)azetidine moiety.

abstract：:The natural product acivicin inhibits the glutaminase activity of cytidine triphosphate (CTP) synthetase and is a potent lead compound for drug discovery in the area of neglected tropical diseases, specifically trypanosomaisis. A 2.1-Å-resolution crystal structure of the acivicin adduct with the glutaminase domain fro...

journal_title：ChemMedChem

authors： Oliveira de Souza J,Dawson A,Hunter WN

更新日期：2017-04-20 00:00:00

abstract：:Meridional rhodium(III) polypyridyl complexes of the type mer-[RhX(3)(DMSO)(pp)] (X=Cl, pp=phen 1, dpq 2, dppz 3; X=Br, pp=phen 4) represent a promising class of potent cytostatic agents for the treatment of lymphoma and leukemia. Exposure of their DMSO solutions to light leads to slow isomerization to mixtures of the...

journal_title：ChemMedChem

authors： Dobroschke M,Geldmacher Y,Ott I,Harlos M,Kater L,Wagner L,Gust R,Sheldrick WS,Prokop A

更新日期：2009-02-01 00:00:00

abstract：:A severe limitation in cancer therapy is the often insufficient differentiation between malign and benign tissue using known chemotherapeutics. One approach to decrease side effects is antibody-directed enzyme prodrug therapy (ADEPT). We have developed new glycosidic prodrugs such as (-)-(1S)-26 b based on the antibio...

journal_title：ChemMedChem

authors： Tietze LF,von Hof JM,Krewer B,Müller M,Major F,Schuster HJ,Schuberth I,Alves F

更新日期：2008-12-01 00:00:00

abstract：:Intraoperative imaging technologies recently entered the operating room, and their implementation is revolutionizing how physicians plan, monitor, and perform surgical interventions. In this work, we present a novel surgical imaging reporter system: intraoperative chemiluminescence imaging (ICI). To this end, we have ...

journal_title：ChemMedChem

authors： Büchel GE,Carney B,Shaffer TM,Tang J,Austin C,Arora M,Zeglis BM,Grimm J,Eppinger J,Reiner T

更新日期：2016-09-20 00:00:00

abstract：:Human African trypanosomiasis (HAT), Chagas disease, and leishmaniasis belong to a group of infectious diseases known as neglected tropical diseases and are induced by infection with protozoan parasites named trypanosomatids. Drugs in current use have several limitations, and therefore new candidate drugs are required...

journal_title：ChemMedChem

authors： Dichiara M,Marrazzo A,Prezzavento O,Collina S,Rescifina A,Amata E

更新日期：2017-08-22 00:00:00

abstract：:Targeting the tumor cell mitochondrion could produce novel anticancer agents. We designed an aryl-urea fatty acid (1 g; 16({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)hexadecanoic acid) that disrupted the mitochondrion and decreased MDA-MB-231 breast cancer cell viability. To optimize the aryl-ureas the prese...

journal_title：ChemMedChem

authors： Murray M,Roseblade A,Chen Y,Bourget K,Rawling T

更新日期：2020-01-17 00:00:00

abstract：:Serine- and metallo-β-lactamases present a threat to the clinical use of nearly all β-lactam antibiotics, including penicillins, cephalosporins, and carbapenems. Efforts to develop metallo-β-lactamase (MBL) inhibitors require suitable screening platforms to allow the rapid determination of β-lactamase activity and eff...

journal_title：ChemMedChem

authors： Makena A,van Berkel SS,Lejeune C,Owens RJ,Verma A,Salimraj R,Spencer J,Brem J,Schofield CJ

更新日期：2013-12-01 00:00:00

abstract：:The integrated stress response comprises multiple signaling pathways for detecting and responding to cellular stress that converge at a single event-the phosphorylation of Ser51 on the α-subunit of eukaryotic translation initiation factor 2 (eIF2α). Phosphorylation of eIF2α (eIF2α-P) results in attenuation of global p...

journal_title：ChemMedChem

authors： Hearn BR,Jaishankar P,Sidrauski C,Tsai JC,Vedantham P,Fontaine SD,Walter P,Renslo AR

更新日期：2016-04-19 00:00:00

abstract：:Dihydropyrimidine-based compounds belong to the first discovered inhibitors of the human mitotic kinesin Eg5. Although they are used by many research groups as model compounds for chemical genetics, considerably less emphasis has been placed on the improvement of this type of inhibitor, with the exception of two recen...

journal_title：ChemMedChem

authors： Prokopcová H,Dallinger D,Uray G,Kaan HY,Ulaganathan V,Kozielski F,Laggner C,Kappe CO

更新日期：2010-10-04 00:00:00

abstract：:The histone deacetylase (HDAC) family is a promising drug target class owing to the importance of these enzymes in a variety of cellular processes. Docking studies were conducted to identify novel HDAC inhibitors. Subtle modifications in the recognition domain were introduced into a series of chlamydocin analogues, an...

journal_title：ChemMedChem

authors： Wang S,Li X,Wei Y,Xiu Z,Nishino N

更新日期：2014-03-01 00:00:00

abstract：:A series of 1,3,3,4-tetrasubstituted pyrrolidine containing CCR5 receptor antagonists were designed, which were elaborated either by condensation of a lithium salt of 3-(N,N-dibenzyl)aminopropionic acid methyl ester with ethyl benzoformate or by Baylis-Hillman reaction of ethyl acrylate with ethyl benzoformate and sub...

journal_title：ChemMedChem

authors： Ma D,Yu S,Li B,Chen L,Chen R,Yu K,Zhang L,Chen Z,Zhong D,Gong Z,Wang R,Jiang H,Pei G

更新日期：2007-02-01 00:00:00

abstract：:N-Acylethanolamine acid amidase (NAAA) is a cysteine hydrolase that catalyzes the hydrolysis of endogenous lipid mediators such as palmitoylethanolamide (PEA). PEA has been shown to exert anti-inflammatory and antinociceptive effects in animals by engaging peroxisome proliferator-activated receptor α (PPAR-α). Thus, p...

journal_title：ChemMedChem

authors： Fiasella A,Nuzzi A,Summa M,Armirotti A,Tarozzo G,Tarzia G,Mor M,Bertozzi F,Bandiera T,Piomelli D

更新日期：2014-07-01 00:00:00

abstract：:Compound 11 (3-(benzyloxy)-1'-methyl-1'-azonia-4H-1'-azaspiro[isoxazole-5,3'-bicyclo[2.2.2]octane] iodide) was selected from a previous set of nicotinic ligands as a suitable model compound for the design of new silent agonists of α7 nicotinic acetylcholine receptors (nAChRs). Silent agonists evoke little or no channe...

journal_title：ChemMedChem

authors： Quadri M,Matera C,Silnović A,Pismataro MC,Horenstein NA,Stokes C,Papke RL,Dallanoce C

更新日期：2017-08-22 00:00:00

abstract：:Over the years, a number of dimensionality reduction techniques have been proposed and used in chemoinformatics to perform nonlinear mappings. In this study, four representatives of nonlinear dimensionality reduction methods related to two different families were analyzed: distance-based approaches (Isomap and Diffusi...

journal_title：ChemMedChem

authors： Kireeva NV,Ovchinnikova SI,Tetko IV,Asiri AM,Balakin KV,Tsivadze AY

更新日期：2014-05-01 00:00:00

abstract：:We recently reported the synthesis and biological evaluation of a novel series of 5-alkyl-2-(N,N-disubstituted)amino-6-(2,6-difluorophenylalkyl)-3,4-dihydropyrimidin-4(3H)-ones (F(2)-N,N-DABOs). These compounds are highly active against both wild-type HIV-1 and the K103N, Y181C, and Y188L mutant strains. Herein we pre...

journal_title：ChemMedChem

authors： Samuele A,Facchini M,Rotili D,Mai A,Artico M,Armand-Ugón M,Esté JA,Maga G

更新日期：2008-09-01 00:00:00

abstract：:A group of acidic nucleosides were synthesized to develop a new class of ribonuclease A (RNase A) inhibitors. Our recent study on carboxymethylsulfonyl-modified nucleosides revealed some interesting results in RNase A inhibition. This positive outcome triggered an investigation of the role played by secondary sugar hy...

journal_title：ChemMedChem

authors： Datta D,Dasgupta S,Pathak T

更新日期：2014-09-01 00:00:00

abstract：:(±)-6-Alkyl-2,4-diaminopyrimidine-based inhibitors of bacterial dihydrofolate reductase (DHFR) have been prepared and evaluated for biological potency against Bacillus anthracis and Staphylococcus aureus. Biological studies revealed attenuated activity relative to earlier structures lacking substitution at C6 of the d...

journal_title：ChemMedChem

authors： Nammalwar B,Bourne CR,Bunce RA,Wakeham N,Bourne PC,Ramnarayan K,Mylvaganam S,Berlin KD,Barrow EW,Barrow WW

更新日期：2012-11-01 00:00:00

abstract：:The Eph-ephrin system, including the EphA2 receptor and the ephrinA1 ligand, plays a critical role in tumor and vascular functions during carcinogenesis. We previously identified (3α,5β)-3-hydroxycholan-24-oic acid (lithocholic acid) as an Eph-ephrin antagonist that is able to inhibit EphA2 receptor activation; it is ...

journal_title：ChemMedChem

authors： Tognolini M,Incerti M,Hassan-Mohamed I,Giorgio C,Russo S,Bruni R,Lelli B,Bracci L,Noberini R,Pasquale EB,Barocelli E,Vicini P,Mor M,Lodola A

更新日期：2012-06-01 00:00:00

abstract：:The emergence and dissemination of multidrug resistant (MDR) pathogens resistant to nearly all available antibiotics poses a significant threat in clinical therapy. Among them, Klebsiella pneumoniae clinical isolates overexpressing KPC-2 carbapenemase are the most worrisome, extending bacterial resistance to last-reso...

journal_title：ChemMedChem

authors： Celenza G,Vicario M,Bellio P,Linciano P,Perilli M,Oliver A,Blazquez J,Cendron L,Tondi D

更新日期：2018-04-06 00:00:00

abstract：:Because only a few studies have investigated the affinity and functional activity of NMDA receptor open channel blockers under the same assay conditions, a comparative study of common open channel blockers is of major interest. The pharmacological activities of MK-801, phencyclidine (PCP), dexoxadrol, etoxadrol, (S)- ...

journal_title：ChemMedChem

authors： Temme L,Schepmann D,Schreiber JA,Frehland B,Wünsch B

更新日期：2018-03-06 00:00:00

abstract：:A novel class of isochroman dopamine analogues, originally reported by Abbott Laboratories, have >100-fold selectivity for D₁-like over D₂-like receptors. We synthesized a parallel series of chroman compounds and showed that repositioning the oxygen atom in the heterocyclic ring decreases potency and confers D₂-like r...

journal_title：ChemMedChem

authors： Bonner LA,Laban U,Chemel BR,Juncosa JI,Lill MA,Watts VJ,Nichols DE

更新日期：2011-06-06 00:00:00

abstract：:The Pathogen Box is a 400-strong collection of drug-like compounds, selected for their potential against several of the world's most important neglected tropical diseases, including trypanosomiasis, leishmaniasis, cryptosporidiosis, toxoplasmosis, filariasis, schistosomiasis, dengue virus and trichuriasis, in addition...

journal_title：ChemMedChem

authors： Veale CGL

更新日期：2019-02-19 00:00:00

abstract：:Over the past few years, the number of people diagnosed with type 2 diabetes has increased owing to an unhealthy diet, a limited amount of exercise, and obesity. The search for novel and efficient antidiabetes agents has become an urgent task for scientists. Among the antidiabetes drugs, α-glucosidase inhibitor drugs ...

journal_title：ChemMedChem

authors： Liu Z,Ma S

更新日期：2017-06-07 00:00:00

abstract：:Loperamide (1a), an opioid receptor agonist, is in clinical use as an antidiarrheal agent. Carbon/silicon exchange (sila-substitution) at the 4-position of the piperidine ring of 1a (R3 COH→R3 SiOH) leads to sila-loperamide (1b). Sila-loperamide was synthesized in a multistep procedure, starting from triethoxyvinylsil...

journal_title：ChemMedChem

authors： Geyer M,Wellner E,Jurva U,Saloman S,Armstrong D,Tacke R

更新日期：2015-05-01 00:00:00

abstract：:It has been 25 years since the development of the first efficient HIV-1/AIDS treatment. Scientists now know more about the HIV-1 infection life cycle, and more than 30 antiretroviral drugs have been developed, including HIV-1 fusion inhibitors. Fundamental work was begun in the early 1990s and led to the development o...

journal_title：ChemMedChem

authors： Cai L,Jiang S

更新日期：2010-11-08 00:00:00

abstract：:The NLRP3 inflammasome is an important regulator of the sterile inflammatory response, and its activation by host-derived sterile molecules leads to the intracellular activation of caspase-1, processing of the pro-inflammatory cytokines interleukin-1β (IL-1β)/IL-18, and pyroptotic cell death. Inappropriate activation ...

journal_title：ChemMedChem

authors： Baldwin AG,Tapia VS,Swanton T,White CS,Beswick JA,Brough D,Freeman S

更新日期：2018-02-20 00:00:00

abstract：:N-Acylethanolamine acid amidase (NAAA) is a cysteine amidase that preferentially hydrolyzes saturated or monounsaturated fatty acid ethanolamides (FAEs), such as palmitoylethanolamide (PEA) and oleoylethanolamide (OEA), which are endogenous agonists of nuclear peroxisome proliferator-activated receptor-α (PPAR-α). Com...

journal_title：ChemMedChem

authors： Vitale R,Ottonello G,Petracca R,Bertozzi SM,Ponzano S,Armirotti A,Berteotti A,Dionisi M,Cavalli A,Piomelli D,Bandiera T,Bertozzi F

更新日期：2014-02-01 00:00:00

abstract：:Members of the Eph receptor tyrosine kinase family play essential roles in the pathogenesis of cancer and are therefore promising candidates for molecular imaging by positron emission tomography (PET), for example. In this regard, radiochemical access to novel PET radiotracers derived from potent inhibitors that targe...

journal_title：ChemMedChem

authors： Mamat C,Mosch B,Neuber C,Köckerling M,Bergmann R,Pietzsch J

更新日期：2012-11-01 00:00:00

abstract：:S100B contributes to cell proliferation by binding the C terminus of p53 and inhibiting its tumor suppressor function. The use of multiple computational approaches to screen fragment libraries targeting the human S100B-p53 interaction site is reported. This in silico screening led to the identification of 280 novel pr...

journal_title：ChemMedChem

authors： Agamennone M,Cesari L,Lalli D,Turlizzi E,Del Conte R,Turano P,Mangani S,Padova A

更新日期：2010-03-01 00:00:00

abstract：:alpha,beta-Unsaturated carbonyl compounds as potential drug candidates is a controversial topic since their potential Michael acceptor activity can lead to cell damage and cytotoxicity. Nevertheless, the alpha,beta-unsaturated carbonyl functionality can be employed as a tool to fine tune biological activity by directl...

journal_title：ChemMedChem

authors： Amslinger S

更新日期：2010-03-01 00:00:00