Modulating the development of E. coli biofilms with 2-aminoimidazoles.

abstract：:Several classes of flavonoids (flavones, flavanones, 2'-hydroxychalcones and flavan-4-ols) having a variety of substituents on A ring were investigated for their antiproliferative activity against MCF-7 human breast cancer cells. Structure-activity relationships of these compounds were discussed. 2'-hydroxychalcones a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pouget C,Lauthier F,Simon A,Fagnere C,Basly JP,Delage C,Chulia AJ

更新日期：2001-12-17 00:00:00

abstract：:A series of novel amino acid ester derivatives of 2,3-substituted isoindolinones was synthesized and evaluated for p53-mediated apoptotic activity. The rationale for augmentation of the target activity of 2,3-substituted isoindolinones was based on the introduction of new fragments in the structure of the inhibitor th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Grigoreva TA,Novikova DS,Petukhov AV,Gureev MA,Garabadzhiu AV,Melino G,Barlev NA,Tribulovich VG

更新日期：2017-12-01 00:00:00

abstract：:A concise synthesis of three novel C2-C3 unsaturated pyrrolo[2,1-c][1,4]benzodiazepine analogues (18-20) containing conjugated acrylyl C2-substituents is reported that utilises Heck coupling to install the C2-acrylyl side chains. These analogues possess significant cytotoxicity according to the NCI 60-cell line screen...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen Z,Gregson SJ,Howard PW,Thurston DE

更新日期：2004-03-22 00:00:00

abstract：:A series of 2,2-dimethyl-5-[4-(methylsulfonyl)phenyl]-4-phenyl-3(2H)furanones was prepared and evaluated for their ability to inhibit cyclo-oxygenase-2 (COX-2). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shin SS,Noh MS,Byun YJ,Choi JK,Kim JY,Lim KM,Ha JY,Kim JK,Lee CH,Chung S

更新日期：2001-01-22 00:00:00

abstract：:The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as replacement of the benzylic methylene with sulfones, gem-difluoromethylenes and alcohols in an effort to balance the antiviral potency with reasonable pharmacok...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lynch CL,Willoughby CA,Hale JJ,Holson EJ,Budhu RJ,Gentry AL,Rosauer KG,Caldwell CG,Chen P,Mills SG,MacCoss M,Berk S,Chen L,Chapman KT,Malkowitz L,Springer MS,Gould SL,DeMartino JA,Siciliano SJ,Cascieri MA,Carella

更新日期：2003-01-06 00:00:00

abstract：:To obtain modulators for reducing mitochondrial damage by the inhibition of Aβ oligomer formation, 2-phenylbenzofuran derivatives were designed and prepared. Their inhibitory activity against Aβ fibril formation was screened using ThT fluorescence assay, and the effect of derivatives on mitochondrial function was eval...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee YS,Kim HY,Youn HM,Seo JH,Kim Y,Shin KJ

更新日期：2013-11-01 00:00:00

abstract：:Sulfonate analogues of combretastatin A-4 have been prepared. These compounds compete with colchicine and combretastatin A-4 for the colchicine binding site on tubulin and are potent inhibitors of tubulin polymerization and cell proliferation. Importantly, these compounds also inhibit the proliferation of P-glycoprote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gwaltney SL 2nd,Imade HM,Barr KJ,Li Q,Gehrke L,Credo RB,Warner RB,Lee JY,Kovar P,Wang J,Nukkala MA,Zielinski NA,Frost D,Ng SC,Sham HL

更新日期：2001-04-09 00:00:00

abstract：:Two series of aminosubstituted coumarins were synthesised and evaluated in vitro as inhibitors of DNA gyrase and as potential antibacterials. Novel novobiocin-like coumarins, 4-(dialkylamino)methylcoumarins and 4-((2-alkylamino)ethoxy)coumarins, were discovered as gyrase B inhibitors with promising antibacterial activ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Laurin P,Ferroud D,Schio L,Klich M,Dupuis-Hamelin C,Mauvais P,Lassaigne P,Bonnefoy A,Musicki B

更新日期：1999-10-04 00:00:00

abstract：:The stereochemical effects of the hydrocarbon crosslink on the conformation and cellular uptake of i,i+4 stapled peptides were studied. Compared to its S,S-configurated counterpart, the crosslink bearing the R,R-configuration provided a significantly diminished helix stabilizing effect and conferred less efficient cel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim YW,Verdine GL

更新日期：2009-05-01 00:00:00

abstract：:Mannose-6-phosphate (M6P)-containing N-linked glycans are essential signaling molecules for sorting hydrolases in eukaryotic cells. Their receptors, especially the cation-independent M6P receptors (CI-MPRs), have emerged as promising protein targets for targeted drug delivery for the treatment of lysosomal storage dis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu Y,Marshall J,Li Q,Edwards N,Chen G

更新日期：2013-04-15 00:00:00

abstract：:HIV-1 protease inhibitors (PI) with an N-arylpyrrole moiety in the P(3) position afforded excellent antiviral potency and substantially improved aqueous solubility over previously reported variants. The rapid in vitro clearance of these compounds in human liver microsomes prompted oral coadministration with indinavir ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kevin NJ,Duffy JL,Kirk BA,Chapman KT,Schleif WA,Olsen DB,Stahlhut M,Rutkowski CA,Kuo LC,Jin L,Lin JH,Emini EA,Tata JR

更新日期：2003-11-17 00:00:00

abstract：:The first non-substrate like inhibitors of human cytosolic phosphoenolpyruvate carboxykinase (PEPCK) competitive with GTP are reported. An effort to discover orally active compounds that improve glucose homeostasis in Type 2 diabetics by reversibly inhibiting PEPCK led to the discovery of 1-allyl-3-butyl-8-methylxanth...

journal_title：Bioorganic & medicinal chemistry letters

authors： Foley LH,Wang P,Dunten P,Ramsey G,Gubler ML,Wertheimer SJ

更新日期：2003-10-20 00:00:00

abstract：:A series of diphenyl ethers was prepared and evaluated for androgen receptor antagonist activity in human androgen receptor binding and cellular functional assays. Analogs with potent in vitro activities were evaluated for topical in vivo efficacy in the Golden Syrian Hamster ear model. Several compounds showed reduct...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mitchell LH,Hu LY,Nguyen M,Fakhoury S,Smith Y,Iula D,Kostlan C,Carroll M,Dettling D,Du D,Pocalyko D,Wade K,Lefker B

更新日期：2009-04-15 00:00:00

abstract：:A two-step reaction cascade is applied to the sequence-specific detection of single-stranded DNA, including analyte-triggered re-activation of apo-aldolase by its cofactor Zn(2+) and catalytic conversion of a chromophore. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Graf N,Kassube S,Krämer R

更新日期：2008-09-01 00:00:00

abstract：:A novel class of cyclic nucleotide analogs has shown anti-HCMV activity. The synthesis as well as structure-activity relationship studies are presented. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen-Ba P,Lee N,Mitchell H,Chan L,Quimpère M

更新日期：1998-12-15 00:00:00

abstract：:Retinoid X Receptor (RXR) specific ligands are currently being investigated for the treatment of metabolic diseases such as type II diabetes. We report the synthesis of conformationally locked retinoids, which are potent RXR selective ligands, and the attempted synthesis of 9-cyclopropyl locked analogs of RA and 9-cis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vuligonda V,Garst ME,Chandraratna RA

更新日期：1999-02-22 00:00:00

abstract：:An Mg2+ and ATP dependent beta-lactam synthetase (BLS) catalyses formation of a beta-lactam ring during the biosynthesis of clavulanic acid, an important beta-lactamase inhibitor. An epimeric mixture of a 2-methylated derivative of the natural BLS substrate N2-(2-carboxyethyl)-L-arginine was synthesised and found to b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sleeman MC,MacKinnon CH,Hewitson KS,Schofield CJ

更新日期：2002-02-25 00:00:00

abstract：:Photocleavable linkers are advantageous over the common linkers because they could be cleaved without using reagents. A novel photocleavable linker with an α-thioacetophenone moiety has been developed. This linker, which can be cleaved upon irradiation at 365 nm via the Norrish type II reaction, is applicable to a pro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yonezawa H,Nishiyama Y,Takeo K,Iwatsubo T,Tomita T,Yokoshima S,Fukuyama T

更新日期：2014-07-01 00:00:00

abstract：:This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [(35)S]GTPgammaS to different subtypes of Gi protein. The problem arose from the strong affinity between [(35)S]GTPgammaS and the tested compounds...

journal_title：Bioorganic & medicinal chemistry letters

authors： Manetti D,Di Cesare Mannelli L,Dei S,Guandalini L,Martini E,Banchelli M,Ghelardini C

更新日期：2009-04-15 00:00:00

abstract：:Coxsackievirus and related enteroviruses are important human pathogens that cause various diseases with clinical manifestations ranging from trivial flu-like syndromes to dangerous or even fatal diseases such as myocarditis, meningitis and encephalitis. Here, we report on our continuous SAR study focused on 9-(bicyclo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sála M,De Palma AM,Hřebabecký H,Dejmek M,Dračínský M,Leyssen P,Neyts J,Mertlíková-Kaiserová H,Nencka R

更新日期：2011-07-15 00:00:00

abstract：:A novel series of diphenyl lactam containing calcium channel blockers is described. Extensive SAR studies resulted in compounds with low molar activity and good plasma exposure after oral dosing. Compounds 2, 6 and 7 demonstrated significant efficacy in the capsaicin model of secondary hyperalgesia following oral admi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Doherty GA,Bhatia P,Vortherms TA,Marsh KC,Wetter JM,Mack H,Scott VE,Jarvis MF,Stewart AO

更新日期：2012-02-15 00:00:00

abstract：:Several oximes of triterpenes with a 17-beta hydroxyl and abietane derivatives are inhibitors of pyruvate dehydrogenase kinase (PDK) activity. The oxime 12 and dehydroabietyl amine 2 exhibit a blood glucose lowering effect in the diabetic ob/ob mouse after a single oral dose of 100 micromol/kg. However, the mechanism ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aicher TD,Damon RE,Koletar J,Vinluan CC,Brand LJ,Gao J,Shetty SS,Kaplan EL,Mann WR

更新日期：1999-08-02 00:00:00

abstract：:The synthesis, SAR, pharmacokinetic profile, and modeling studies of both monocyclic and fused pyrazoles containing substituted N-arylpiperidinyl P4 moieties that are potent and selective factor Xa inhibitors will be discussed. Fused pyrazole analog 16a, with a 2'-methylsulfonylphenyl piperidine P4 group, was shown to...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qiao JX,Cheng X,Smallheer JM,Galemmo RA,Drummond S,Pinto DJ,Cheney DL,He K,Wong PC,Luettgen JM,Knabb RM,Wexler RR,Lam PY

更新日期：2007-03-01 00:00:00

abstract：:A series of chiral heterocyclic aminopyrrolidine derivatives was synthesized as novel melatoninergic ligands. Binding affinity assays were performed on cloned human MT(1) and MT(2) receptors, stably expressed in NIH3T3 cells. Compound 16 was identified as an orally bioavailable agonist at MT(1) and MT(2) melatonin rec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun LQ,Chen J,Mattson RJ,Epperson JR,Deskus JA,Li WS,Takaki K,Hodges DB,Iben L,Mahle CD,Ortiz A,Molstad D,Ryan E,Yeleswaram K,Xu C,Luo G

更新日期：2003-12-15 00:00:00

abstract：:Model reactions offer a chemical mechanism by which formation of a sulfenyl amide residue at the active site of the redox-regulated protein tyrosine phosphatase PTP1B protects the cysteine redox switch in this enzyme against irreversible oxidative destruction. The results suggest that 'overoxidation' of the sulfenyl a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sivaramakrishnan S,Cummings AH,Gates KS

更新日期：2010-01-15 00:00:00

abstract：:Symmetrically and asymmetrically substituted 1,2,4,5-tetraoxanes were synthesized by the oxidative system H(2)O(2)/TFE in presence of MeReO(3) as a catalyst. All of the synthesized compounds were characterized spectroscopically, and evaluated for cytotoxicity, and antimalarial activity. Several of these tetraoxanes ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Atheaya H,Khan SI,Mamgain R,Rawat DS

更新日期：2008-02-15 00:00:00

abstract：:In order to obtain rigidity within the sugar moiety of nucleosides, the bicyclic pyrimidine derivatives of N,O-isoxazolidines were designed and synthesized by using 1,3-dipolar cycloaddition of Delta(1)-pyrrolidine-1-oxide and the appropriate vinyl-nucleobases. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Procopio A,Alcaro S,De Nino A,Maiuolo L,Ortuso F,Sindona G

更新日期：2005-02-01 00:00:00

abstract：:ADX88178 (1) has been recently developed as a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4). The aim of this study was to develop [(11)C]1 as a novel positron emission tomography ligand and to evaluate its binding ability for mGluR4. Using stannyl precursor 3, [(11)C]1 was efficie...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujinaga M,Yamasaki T,Nengaki N,Ogawa M,Kumata K,Shimoda Y,Yui J,Xie L,Zhang Y,Kawamura K,Zhang MR

更新日期：2016-01-15 00:00:00

abstract：:Two new γ-lactones, aspergilactones A (1) and B (2), were discovered along with two known compounds, annularin A (3) and pericoterpenoid A (4), from a culture of the sponge-associated fungus Aspergillus sp. LS45. The planar structures of 1-4 were characterized using comprehensive spectroscopic methods and comparison w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang L,Ding L,Li X,Wang N,Yan Y,Yang M,Cui W,Benjamin Naman C,Cheng K,Zhang W,Zhang B,Jin H,He S

更新日期：2019-07-01 00:00:00

abstract：:Docking studies of 4-phenylthiazolinethione on human IDO1 suggest complexation of the heme iron by the exocyclic sulfur atom further reinforced by hydrophobic interactions of the phenyl ring within pocket A of the enzyme. On this basis, chemical modifications were proposed to increase inhibition activity. Synthetic ro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Balti M,Plas A,Meinguet C,Haufroid M,Thémans Q,Efrit ML,Wouters J,Lanners S

更新日期：2017-08-01 00:00:00