Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2).

abstract：:We report the synthesis and properties of two new seminaphthorhodafluor (SNARF) derivatives, SNARF-F and SNARF-Cl. Both these derivatives exhibit typical red shifts of absorption and fluorescence, and higher cell permeability as compared to traditional SNARF, while the pH-dependent dual-emission characteristics are we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nakata E,Nazumi Y,Yukimachi Y,Uto Y,Maezawa H,Hashimoto T,Okamoto Y,Hori H

更新日期：2011-03-15 00:00:00

abstract：:Incorporation of a carboxylic acid into a series of uracil derivatives as hGnRH-R antagonists resulted in a significant reduction of CYP3A4 inhibitory activity. Highly potent hGnRH antagonists with low CYP3A4 inhibitory liability, such as 8a and 8d, were identified. Thus, 8a had a K(i) of 2.2 nM at GnRH-R and an IC(50...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen C,Chen Y,Pontillo J,Guo Z,Huang CQ,Wu D,Madan A,Chen T,Wen J,Xie Q,Tucci FC,Rowbottom M,Zhu YF,Wade W,Saunders J,Bozigian H,Struthers RS

更新日期：2008-06-01 00:00:00

abstract：:The synthesis and biological evaluation of novel cycloheptaquinoline antagonists of the human H(3) receptor are described. Two series of compounds, bearing either an amino substituent or an alkyne linker at the 11-position, were investigated. Modifications of the amino substituents, optimization of chain length and th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Turner SC,Esbenshade TA,Bennani YL,Hancock AA

更新日期：2003-07-07 00:00:00

abstract：:Structure-activity studies on benzamide 1 obtained from library screening led to the discovery of a novel series of potent and selective glycine transporter type-2 inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ho KK,Appell KC,Baldwin JJ,Bohnstedt AC,Dong G,Guo T,Horlick R,Islam KR,Kultgen SG,Masterson CM,McDonald E,McMillan K,Morphy JR,Rankovic Z,Sundaram H,Webb M

更新日期：2004-01-19 00:00:00

abstract：:Ortho-substituted biphenyl moieties are widely used in drug design. We herein report a successful use of the perpendicular conformation of the alpha-substituted phenylcyclopropyl groups to mimic the aplanar, biologically active conformation of the ortho-substituted biphenyl moieties to achieve structural diversity. Th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qiao JX,Cheney DL,Alexander RS,Smallwood AM,King SR,He K,Rendina AR,Luettgen JM,Knabb RM,Wexler RR,Lam PY

更新日期：2008-07-15 00:00:00

abstract：:A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Webster SP,Ward P,Binnie M,Craigie E,McConnell KM,Sooy K,Vinter A,Seckl JR,Walker BR

更新日期：2007-05-15 00:00:00

abstract：:The application of a novel solid-phase synthesis of 2,3-disubstituted indoles utilizing a carbamate indole linker is described resulting in the identification of the novel, high-affinity, selective h5-HT2A antagonist 19. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Smith AL,Stevenson GI,Lewis S,Patel S,Castro JL

更新日期：2000-12-18 00:00:00

abstract：:A series of MT-II related cyclic peptides, based on potent but non-selective hMC4R agonist (Penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2)) was prepared in which His(6) residue was systematically substituted. Two of the most interesting peptides identified in this study are Penta-c[Asp-5-ClAtc-DPhe-Arg-Trp-Lys]-N...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cheung AW,Danho W,Swistok J,Qi L,Kurylko G,Rowan K,Yeon M,Franco L,Chu XJ,Chen L,Yagaloff K

更新日期：2003-04-07 00:00:00

abstract：:Mass-directed isolation of the CH(2)Cl(2)/MeOH extract from the leaves of Cryptocarya obovata resulted in the purification of a new trypanocidal alpha-pyrone, 7',8'-dihydroobolactone (1). The chemical structure of 1 was determined by 1D/2D NMR, MS and CD data analysis. 7',8'-Dihydroobolactone was shown to inhibit Tryp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Davis RA,Demirkiran O,Sykes ML,Avery VM,Suraweera L,Fechner GA,Quinn RJ

更新日期：2010-07-15 00:00:00

abstract：:A series of novel (1S)-(-)-verbenone derivatives was synthesized bearing a 4-styryl scaffold. The synthesized compounds were tested for their anti-oxidant, anti-excitotoxic, and anti-ischemic activities. These derivatives significantly reduced oxygen-glucose deprivation-induced neuronal injury and N-methyl-D-aspartic ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ju C,Song S,Hwang S,Kim C,Kim M,Gu J,Oh YK,Lee K,Kwon J,Lee K,Kim WK,Choi Y

更新日期：2013-10-01 00:00:00

abstract：:A new halicyclamine derivative, tetradehydrohalicyclamine B (1), was isolated from the marine sponge Acanthostrongylophora ingens, along with halicyclamine B (2) as proteasome inhibitors. Compound 1 is the second example found to have a pyridinium ring in the halicyclamine family. Although the relative configuration o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kato H,El-Desoky AH,Takeishi Y,Nehira T,Angkouw ED,Mangindaan REP,de Voogd NJ,Tsukamoto S

更新日期：2019-01-01 00:00:00

abstract：:A series of 114 SIRT inhibitor candidates was assembled using 'click chemistry', by reacting two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in the presence of Cu(I) catalyst. Screening identified two SIRT2-selective inhibitors, which were more SIRT2-selective than AGK2, a known SIRT...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tatum PR,Sawada H,Ota Y,Itoh Y,Zhan P,Ieda N,Nakagawa H,Miyata N,Suzuki T

更新日期：2014-04-15 00:00:00

abstract：:Our process research on OPC-35564 revealed that a mixed borohydride reducing agent (ZrCl4/NaBH4) in DME (Itsuno system) afforded a rapid and direct conversion of N-alkyl-nitroisatin into nitroindole nucleus. Comparison with other reducing agents indicated the superiority of the present system and the key function of Z...

journal_title：Bioorganic & medicinal chemistry letters

authors： Torisawa Y,Nishi T,Minamikawa J

更新日期：2001-03-26 00:00:00

abstract：:A series of 6-alkoxyisoindolin-1-ones with a magic shotgun pharmacological profile are presented as potential antipsychotics. The in vitro pharmacological profile includes D(2) partial agonism (30-55%), 5-HT(1A) partial agonism (60-90%), and 5-HT(2A) antagonism. Selected compounds in this series displayed good in vivo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Favor DA,Powers JJ,White AD,Fitzgerald LW,Groppi V,Serpa KA

更新日期：2010-10-01 00:00:00

abstract：:A group of novel quinoxalinone derivatives (4a-h) were prepared and investigated for their inhibitory activity against ALR2 and antioxidant activity. Most of them were found to be potent aldose reductase inhibitors with IC50 values ranging from 0.019 to 0.982 μM. The most active compound 2-(3-(4-hydroxyphenoxy)-6-fluo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zou Y,Qin X,Hao X,Zhang W,Yang S,Yang Y,Han Z,Ma B,Zhu C

更新日期：2015-09-15 00:00:00

abstract：:Twelve dimeric peptidomimetics 1 were prepared via a divergent-convergent strategy. These peptidomimetics incorporated the same amino acids as i +1 and i + 2 residues in key beta-turns of the neurotrophin NT-3. Cytosensor microphysiometry was used to gauge the effects of the dimers 1 on cells that overexpress the NT-3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang AJ,Khare S,Gokulan K,Linthicum DS,Burgess K

更新日期：2001-01-22 00:00:00

abstract：:To overcome the chemical and metabolic instability of the secondary fatty acyl residues in the AGP class of lipid A mimetics, the secondary ether lipid analogs of the potent TLR4 agonist CRX-527 (2) and TLR4 antagonist CRX-526 (3) were synthesized and evaluated along with their ester counterparts for agonist/antagonis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bazin HG,Murray TJ,Bowen WS,Mozaffarian A,Fling SP,Bess LS,Livesay MT,Arnold JS,Johnson CL,Ryter KT,Cluff CW,Evans JT,Johnson DA

更新日期：2008-10-15 00:00:00

abstract：:Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. To examine the distance between the two ligand binding sites (C1A and C1B) of PKC, we designed and synthesized two series of isobenzofuranone dimers. Peak binding activities were observed for the C3-acyl cha...

journal_title：Bioorganic & medicinal chemistry letters

authors： Baba Y,Mayumi S,Hirai G,Kawasaki H,Ogoshi Y,Yanagisawa T,Hashimoto Y,Sodeoka M

更新日期：2004-06-07 00:00:00

abstract：:The mechanism of edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one) to scavenge DPPH radical is clarified by density functional theory (DFT) calculations. It is revealed that H-atom-abstraction rather than electron-transfer reaction is involved in the radical-scavenging process of edaravone, and H-atom at position 4 is r...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang LF,Zhang HY

更新日期：2003-11-03 00:00:00

abstract：:Series of benzyl-phenoxybenzyl amino-phenyl acid derivatives (8a-q) are reported as non-steroidal GR antagonist. Compound 8g showed excellent h-GR binding and potent antagonistic activity (in vitro). The lead compound 8g exhibited significant oral antidiabetic and antihyperlipidemic effects (in vivo), along with liver...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shah K,Patel D,Jadav P,Sheikh M,Sairam KV,Joharapurkar A,Jain MR,Bahekar R

更新日期：2012-09-15 00:00:00

abstract：:A new family of photonuclease, thiadiazole-naphthalimide were synthesized and evaluated. Thiadiazole group was incorporated for the first time. These compounds intercalated into DNA efficiently and damaged DNA as low as 10 microM photochemically. Mechanism experiment showed that electron transfer and radicals were inv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Y,Xu Y,Qian X,Qu B

更新日期：2003-10-20 00:00:00

abstract：:In continuation of our efforts to find new antimicrobial compounds, series of fatty N-acyldiamines were prepared from fatty methyl esters and 1,2-ethylenediamine, 1,3-propanediamine or 1,4-butanediamine. The synthesized compounds were screened for their antibacterial activity against Gram-positive bacteria (Staphyloco...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ferreira BDS,de Almeida AM,Nascimento TC,de Castro PP,Silva VL,Diniz CG,Le Hyaric M

更新日期：2014-10-01 00:00:00

abstract：:A versatile route for the synthesis of homochiral alpha-ketoamide analogues of amino acids is described. Incorporation of this functionality into peptide sequences using either solution or solid-phase chemistry resulted in potent inhibitors of the Hepatitis C Virus NS3 proteinase. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Beevers R,Carr MG,Jones PS,Jordan S,Kay PB,Lazell RC,Raynham TM

更新日期：2002-02-25 00:00:00

abstract：:A series of glutathione derivatives 1-4, modified at the N,S and/or COOH sites, with in vitro antitrypanosomal activity were tested against bloodstream form Trypanosoma brucei 247 wild type and a T. b. brucei 247 strain over-expressing the multiple drug resistance protein (MRPA) by 50-100x to assess the susceptibility...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alibu VP,Daunes S,D'Silva C

更新日期：2013-08-01 00:00:00

abstract：:As a continuation of our efforts to discover and develop the apoptosis inducing 4-aryl-4H-chromenes as novel anticancer agents, we explored the SAR of 4-aryl-4H-chromenes with modifications at the 7- and 5-, 6-, 8-positions. It was found that a small hydrophobic group, such as NMe2, NH2, NHEt, and OMe, is preferred at...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kemnitzer W,Kasibhatla S,Jiang S,Zhang H,Zhao J,Jia S,Xu L,Crogan-Grundy C,Denis R,Barriault N,Vaillancourt L,Charron S,Dodd J,Attardo G,Labrecque D,Lamothe S,Gourdeau H,Tseng B,Drewe J,Cai SX

更新日期：2005-11-01 00:00:00

abstract：:A series of anthranilodinitrile-based biaryls were synthesized and evaluated in vitro against extracellular promastigotes and intracellular amastigotes of Leishmania donovani. Among various screened compounds, a biaryl with trifluoromethyl group 5f showed 83% inhibition against promastigotes and 70% inhibition against...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh FV,Vatsyayan R,Roy U,Goel A

更新日期：2006-05-15 00:00:00

abstract：:A benzopyranopyridine inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MK2) is prepared rapidly and efficiently in one step using microwave dielectric heating, whereas a substrate-selective p38 MAPK inhibitor was prepared using conventional heating techniques. The former had MK2 inhibitory act...

journal_title：Bioorganic & medicinal chemistry letters

authors： Davis T,Bagley MC,Dix MC,Murziani PG,Rokicki MJ,Widdowson CS,Zayed JM,Bachler MA,Kipling D

更新日期：2007-12-15 00:00:00

abstract：:A quantitative structure-activity relationship (QSAR) modeling of the antimold activity of cinnamaldehyde analogues against of Aspergillus niger and Paecilomyces variotii was presented. The molecular descriptors of cinnamaldehyde analogues were calculated by the CODESSA program, and these descriptors were selected by ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Y,Li S,Kong X

更新日期：2013-03-01 00:00:00

abstract：:A novel fluorescein-based fluorescent probe for nitroxyl (HNO) based on the reductive Staudinger ligation of HNO with an aromatic phosphine was prepared. This probe reacts with HNO derived from Angeli's salt and 4-bromo Piloty's acid under physiological conditions without interference by other biological redox species...

journal_title：Bioorganic & medicinal chemistry letters

authors： Miao Z,Reisz JA,Mitroka SM,Pan J,Xian M,King SB

更新日期：2015-01-01 00:00:00

abstract：:In the modification of the fibrinogen fragment related sequences ARPAK, QRPAK GRPAK and KRPAK, the corresponding cyclo-ARPAK, cyclo-QRPAK, cyclo-GRPAK, and cyclo-KRPAK were prepared in the diluted solution. The bioassay in vivo indicated that the thrombolytic potencies of cyclo-ARPAK, cyclo-GRPAK, cyclo-QRPAK, and cyc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao M,Lin N,Wang C,Peng S

更新日期：2003-03-10 00:00:00