BIOORGANIC & MEDICINAL CHEMISTRY文献大全第8页

Substituted quinolines as noncovalent proteasome inhibitors.
abstract：:Screening of a library of diverse heterocyclic scaffolds identified substituted quinolines as inhibitors of the human proteasome. The heterocyclic library was prepared via a novel titanium-catalyzed multicomponent coupling reaction, which rendered a diverse set of isoxazoles, pyrimidines, pyrroles, pyrazoles and quino...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.04.005

authors： McDaniel TJ,Lansdell TA,Dissanayake AA,Azevedo LM,Claes J,Odom AL,Tepe JJ

更新日期：2016-06-01 00:00:00
Synergistic reduction of HIV-1 infectivity by 5-azacytidine and inhibitors of ribonucleotide reductase.
abstract：:Although many compounds have been approved for the treatment of human immunodeficiency type-1 (HIV-1) infection, additional anti-HIV-1 drugs (particularly those belonging to new drug classes) are still needed due to issues such as long-term drug-associated toxicities, transmission of drug-resistant variants, and devel...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.03.052

authors： Rawson JM,Roth ME,Xie J,Daly MB,Clouser CL,Landman SR,Reilly CS,Bonnac L,Kim B,Patterson SE,Mansky LM

更新日期：2016-06-01 00:00:00
Studies on phenothiazines: New microtubule-interacting compounds with phenothiazine A-ring as potent antineoplastic agents.
abstract：:New phenothiazine derivatives 6-20 have been designed, synthesized and evaluated in vitro for their ability to inhibit tubulin polymerization and antiproliferative activity against 60 cancer cell lines, including several multi-drug resistant (MDR) tumor cell lines. The phenothiazine unit may successfully replace the c...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.04.001

authors： Ghinet A,Moise IM,Rigo B,Homerin G,Farce A,Dubois J,Bîcu E

更新日期：2016-05-15 00:00:00
Tetrahydroprotoberberine alkaloids with dopamine and σ receptor affinity.
abstract：:Two series of analogues of the tetrahydroprotoberberine (THPB) alkaloid (±)-stepholidine that (a) contain various alkoxy substituents at the C10 position and, (b) were de-rigidified with respect to (±)-stepholidine, were synthesized and evaluated for affinity at dopamine and σ receptors in order to evaluate effects on...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.03.037

authors： Gadhiya S,Madapa S,Kurtzman T,Alberts IL,Ramsey S,Pillarsetty NK,Kalidindi T,Harding WW

更新日期：2016-05-01 00:00:00
Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors.
abstract：:In this study, we disclose the design and synthesis of novel 4-susbtituted nipecotic acid derivatives as inhibitors of the GABA transporter mGAT1. Based on molecular modeling studies the compounds are assumed to adopt a binding pose similar to that of the potent mGAT1 inhibitor nipecotic acid. As substitution in 4-pos...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.03.038

authors： Hellenbrand T,Höfner G,Wein T,Wanner KT

更新日期：2016-05-01 00:00:00
Design, synthesis and biological evaluation of N,N-3-phenyl-3-benzylaminopropanamide derivatives as novel cholesteryl ester transfer protein inhibitor.
abstract：:A series of N,N-3-phenyl-3-benzylaminopropanamide derivatives were identified as novel CETP (cholesteryl ester transfer protein) inhibitors. In our previous study, lead compound L10 was discovered by pharmacophore-based virtual screening (Dong-Mei Zhao et al., 2014). Based on L10 (IC50 8.06 μM), compound HL6 (IC50 10....

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.12.010

authors： Zhao D,Xie H,Bai C,Liu C,Hao C,Zhao S,Yuan H,Luo C,Wang J,Lin B,Zheng J,Cheng M

更新日期：2016-04-15 00:00:00
Novel squaramides with in vitro liver stage antiplasmodial activity.
abstract：:A structure-activity relationship study was performed with ten 8-aminoquinoline-squaramides compounds active against liver stage malaria parasites, using human hepatoma cells (Huh7) infected by Plasmodium berghei parasites. In addition, their blood-schizontocidal activity was assessed against chloroquine-resistant W2 ...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.03.005

authors： Ribeiro CJ,Espadinha M,Machado M,Gut J,Gonçalves LM,Rosenthal PJ,Prudêncio M,Moreira R,Santos MM

更新日期：2016-04-15 00:00:00
Development of a potent 2-oxoamide inhibitor of secreted phospholipase A2 guided by molecular docking calculations and molecular dynamics simulations.
abstract：:Inhibition of group IIA secreted phospholipase A2 (GIIA sPLA2) has been an important objective for medicinal chemists. We have previously shown that inhibitors incorporating the 2-oxoamide functionality may inhibit human and mouse GIIA sPLA2s. Herein, the development of new potent inhibitors by molecular docking calcu...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.02.040

authors： Vasilakaki S,Barbayianni E,Leonis G,Papadopoulos MG,Mavromoustakos T,Gelb MH,Kokotos G

更新日期：2016-04-15 00:00:00
Rational design, synthesis and biological evaluation of 1,3,4-oxadiazole pyrimidine derivatives as novel pyruvate dehydrogenase complex E1 inhibitors.
abstract：:On the basis of previous study on 2-methylpyrimidine-4-ylamine derivatives I, further synthetic optimization was done to find potent PDHc-E1 inhibitors with antibacterial activity. Three series of novel pyrimidine derivatives 6, 11 and 14 were designed and synthesized as potential Escherichia coli PDHc-E1 inhibitors b...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.03.011

authors： He H,Wang W,Zhou Y,Xia Q,Ren Y,Feng J,Peng H,He H,Feng L

更新日期：2016-04-15 00:00:00
Synthesis of 3-acyloxyxanthone derivatives as α-glucosidase inhibitors: A further insight into the 3-substituents' effect.
abstract：:Considerable interest has been attracted in xanthone and its derivatives because of their important biological activities. In this paper, a series of novel 3-arylacyloxyxanthone derivatives 2a-p were synthesized and evaluated for their biological activities toward α-glucosidase. In comparison to the parent 1,3-dihydro...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.01.022

authors： Li GL,Cai CY,He JY,Rao L,Ma L,Liu Y,Wang B

更新日期：2016-04-01 00:00:00
Emerging targets and new small molecule therapies in Parkinson's disease treatment.
abstract：:Parkinson's disease (PD) is a common chronic degenerative disease of the central nervous system. Due to a rapidly aging society worldwide, PD morbidity is on the rise; however, the treatment of PD with conventional drugs carries serious adverse reactions and cannot fix the root cause of PD, the degeneration of dopamin...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.bmc.2016.02.030

authors： Zhang H,Tong R,Bai L,Shi J,Ouyang L

更新日期：2016-04-01 00:00:00
Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors.
abstract：:In continuing our efforts to identify small molecules able to inhibit c-Met kinase, three series of novel 6,7-disubstituted-4-phenoxyquinoline derivatives (23a-w, 26a-d and 30a-d) bearing (thio)semicarbazone scaffold were designed, synthesized and evaluated for their cytotoxicity. The biological data revealed that mos...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.02.003

authors： Zhai X,Bao G,Wang L,Cheng M,Zhao M,Zhao S,Zhou H,Gong P

更新日期：2016-03-15 00:00:00
Discovery of novel phenoxazinone derivatives as DKK1/LRP6 interaction inhibitors: Synthesis, biological evaluation and structure-activity relationships.
abstract：:Amino derivatives of NCI8642 were synthesized and evaluated as inhibitors of DKK1/LRP6 interactions. The new inhibitors were able to activate the Wnt signaling pathway as indicated by the increased levels of β-catenin, and decrease the DKK1-induced Tau phosphorylation at serine 396. ...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.01.025

authors： Thysiadis S,Mpousis S,Avramidis N,Katsamakas S,Balomenos A,Remelli R,Efthimiopoulos S,Sarli V

更新日期：2016-03-01 00:00:00
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
abstract：:Targeting tumor vasculature represents an intriguing therapeutic strategy in the treatment of cancer. In an effort to discover new vascular disrupting agents with improved water solubility and potentially greater bioavailability, various amino acid prodrug conjugates (AAPCs) of potent amino combretastatin, amino dihyd...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.01.007

authors： Devkota L,Lin CM,Strecker TE,Wang Y,Tidmore JK,Chen Z,Guddneppanavar R,Jelinek CJ,Lopez R,Liu L,Hamel E,Mason RP,Chaplin DJ,Trawick ML,Pinney KG

更新日期：2016-03-01 00:00:00
A novel library of saccharin and acesulfame derivatives as potent and selective inhibitors of carbonic anhydrase IX and XII isoforms.
abstract：:Small libraries of N-substituted saccharin and N-/O-substituted acesulfame derivatives were synthesized and tested as atypical and selective inhibitors of four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). Most of them inhibited hCA XII in the low nanomolar range, hCA IX with KIs ...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.01.038

authors： Carradori S,Secci D,De Monte C,Mollica A,Ceruso M,Akdemir A,Sobolev AP,Codispoti R,De Cosmi F,Guglielmi P,Supuran CT

更新日期：2016-03-01 00:00:00
Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors.
abstract：:A series of 31 N,N-disubstituted 2-amino-5-halomethyl-2-thiazolines was designed, synthesized, and evaluated for inhibitory potential against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and carboxylesterase (CaE). The compounds did not inhibit AChE; the most active compounds inhibited BChE and CaE with I...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2016.01.031

authors： Makhaeva GF,Boltneva NP,Lushchekina SV,Serebryakova OG,Stupina TS,Terentiev AA,Serkov IV,Proshin AN,Bachurin SO,Richardson RJ

更新日期：2016-03-01 00:00:00
Discovery of pyridine-based agrochemicals by using Intermediate Derivatization Methods.
abstract：:Pyridine-based compounds have been playing a crucial role as agrochemicals or pesticides including fungicides, insecticides/acaricides and herbicides, etc. Since most of the agrochemicals listed in the Pesticide Manual were discovered through screening programs that relied on trial-and-error testing and new agrochemic...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.bmc.2015.09.031

authors： Guan AY,Liu CL,Sun XF,Xie Y,Wang MA

更新日期：2016-02-01 00:00:00
Synthesis and anti-oomycete activity of novel quinazolin- and benzothiazol-6-yloxyacetamides: Potent aza-analogs and five-ring analogs of quinoline fungicides.
abstract：:Novel quinazolin- and benzothiazol-6-yloxyacetamides show excellent in vivo activity against the three economically most important Oomycete pathogens Phytophthora infestans, Plasmopara viticola and Pythium ultimum. They are polar analogs of known quinolin-6-yloxyacetamides, which are not active against the soil-borne ...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.08.009

authors： Beaudegnies R,Quaranta L,Murphy Kessabi F,Lamberth C,Knauf-Beiter G,Fraser T

更新日期：2016-02-01 00:00:00
Use of cytokinins as agrochemicals.
abstract：:Plant hormones cytokinins regulate various aspects of plant growth and development. For their positive effects on branching, delaying of senescence, nutrient remobilisation, flower and seed set control they became interesting substances in search for potential agrochemicals. From the 1970' of the last century exogenou...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.bmc.2015.12.022

authors： Koprna R,De Diego N,Dundálková L,Spíchal L

更新日期：2016-02-01 00:00:00
Actin-binding doliculide causes premature senescence in p53 wild type cells.
abstract：:Addressing the actin cytoskeleton as future anticancer target can be an innovative chemotherapeutic approach to combat malignancies. Doliculide is a potent stabilizer of actin filaments and can be used as tool and therapeutic lead in cancer research. Though a variety of molecules are known to bind to actin and lead to...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.11.042

authors： Foerster F,Chen T,Altmann KH,Vollmar AM

更新日期：2016-01-15 00:00:00
Synthesis of tetravalent LacNAc-glycoclusters as high-affinity cross-linker against Erythrina cristagalli agglutinin.
abstract：:Four kinds of tetravalent double-headed glycoclusters [(LacNAc)4-DHGs] were designed with linkers of varying lengths consisting of alkanedioic carboxyamido groups (C6, C12, C18 and C24) between two bi-antennary LacNAc-glycosides. These glycoclusters served as high-affinity cross-linking ligands for the LacNAc-binding ...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.11.026

authors： Ogata M,Chuma Y,Yasumoto Y,Onoda T,Umemura M,Usui T,Park EY

更新日期：2016-01-01 00:00:00
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.
abstract：:We described the synthesis of a new congener series of 1,2,3-triazolyl-4-oxoquinolines and evaluated their ability to inhibit oseltamivir (OST)-resistant influenza strains. Oxoquinoline derivative 1i was the most potent compound within this series, inhibiting 94% of wild-type (WT) influenza neuraminidase (NA) activity...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.11.028

authors： Boechat Fda C,Sacramento CQ,Cunha AC,Sagrillo FS,Nogueira CM,Fintelman-Rodrigues N,Santos-Filho O,Riscado CS,Forezi Lda S,Faro LV,Brozeguini L,Marques IP,Ferreira VF,Souza TM,de Souza MC

更新日期：2015-12-15 00:00:00
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.
abstract：:A series of quinoline derivatives featuring the novelty of introducing intra-molecular hydrogen bonding scaffold (iMHBS) were designed, synthesized and biologically evaluated for their mTOR inhibitory activity, as well as anti-proliferative efficacies against HCT-116, PC-3 and MCF-7 cell lines. As a result, six compou...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.11.003

authors： Ma X,Lv X,Qiu N,Yang B,He Q,Hu Y

更新日期：2015-12-15 00:00:00
Structural interrogation of benzosuberene-based inhibitors of tubulin polymerization.
abstract：:The discovery of 3-methoxy-9-(30,40,50-trimethoxyphenyl)-6,7-dihydro-5H-benzo[7]annulen-4-ol (a benzosuberene-based analogue referred to as KGP18) was originally inspired by the natural products colchicine and combretastatin A-4 (CA4). The relative structural simplicity and ease of synthesis of KGP18, coupled with its...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.10.012

authors： Herdman CA,Devkota L,Lin CM,Niu H,Strecker TE,Lopez R,Liu L,George CS,Tanpure RP,Hamel E,Chaplin DJ,Mason RP,Trawick ML,Pinney KG

更新日期：2015-12-15 00:00:00
Phenolic group on A-ring is key for dracoflavan B as a selective noncompetitive inhibitor of α-amylase.
abstract：:A high throughput assay was applied to guide the isolation of a new pancreatic α-amylase inhibitor, dracoflavan B, from the dragon's blood resin from Daemonorops draco. Applying C18 column, we successfully isolated both diastereomers and their structures verified by (1)H NMR spectra in comparison with the literature v...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.11.008

authors： Toh ZS,Wang H,Yip YM,Lu Y,Lim BJ,Zhang D,Huang D

更新日期：2015-12-15 00:00:00
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
abstract：:Chagas disease is an infection caused by protozoan Trypanosoma cruzi, which affects approximately 8-10million people worldwide. Benznidazole is the only drug approved for treatment during the acute and asymptomatic chronic phases of Chagas disease; however, it has poor efficacy during the symptomatic chronic phase. Th...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.10.048

authors： de Oliveira Filho GB,de Oliveira Cardoso MV,Espíndola JW,Ferreira LF,de Simone CA,Ferreira RS,Coelho PL,Meira CS,Magalhaes Moreira DR,Soares MB,Lima Leite AC

更新日期：2015-12-01 00:00:00
Carbonic anhydrase inhibitors: Design, synthesis, kinetic, docking and molecular dynamics analysis of novel glycine and phenylalanine sulfonamide derivatives.
abstract：:The inhibition of two human cytosolic carbonic anhydrase isozymes I and II, with some novel glycine and phenylalanine sulfonamide derivatives were investigated. Newly synthesized compounds G1-4 and P1-4 showed effective inhibition profiles with KI values in the range of 14.66-315μM for hCA I and of 18.31-143.8μM again...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.10.009

authors： Fidan İ,Salmas RE,Arslan M,Şentürk M,Durdagi S,Ekinci D,Şentürk E,Coşgun S,Supuran CT

更新日期：2015-12-01 00:00:00
Fine tuning of agonistic/antagonistic activity for vitamin D receptor by 22-alkyl chain length of ligands: 22S-Hexyl compound unexpectedly restored agonistic activity.
abstract：:1α,25-Dihydroxyvitamin D3 exerts its actions by binding to vitamin D receptor (VDR). We are continuing the study related to the alteration of pocket structure of VDR by 22-alkyl substituent of ligands and the relationships between the alteration and agonistic/antagonistic activity. Previously we reported that compound...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.10.026

authors： Anami Y,Sakamaki Y,Itoh T,Inaba Y,Nakabayashi M,Ikura T,Ito N,Yamamoto K

更新日期：2015-11-15 00:00:00
Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
abstract：:The free fatty acid receptor 1 (FFA1) is a novel antidiabetic target for the treatment of type 2 diabetes based on particular mechanism in amplifying glucose-stimulated insulin secretion. We have previously identified a series of phenoxyacetic acid derivatives. Herein, we describe the further chemical modification of ...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.10.011

authors： Li Z,Wang X,Xu X,Yang J,Xia W,Zhou X,Huang W,Qian H

更新日期：2015-11-15 00:00:00
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.
abstract：:Inhibition of receptor tyrosine kinases (RTKs) continued to be a successful approach for the treatment of many types of human cancers and many potent small molecules kinase inhibitors have been discovered the last decade. In the present study, we describe the synthesis of thienopyrimidine derivatives and their pharmac...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.10.035

authors： Ravez S,Arsenlis S,Barczyk A,Dupont A,Frédérick R,Hesse S,Kirsch G,Depreux P,Goossens L

更新日期：2015-11-15 00:00:00
Structure-activity relationships of amide-phosphonate derivatives as inhibitors of the human soluble epoxide hydrolase.
abstract：:Structure-activity relationships of amide-phosphonate derivatives as inhibitors of the human soluble epoxide hydrolase (sEH) were investigated. First, a series of alkyl or aryl groups were substituted on the carbon alpha to the phosphonate function in amide compounds to see whether substituted phosphonates can act as ...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.10.016

authors： Kim IH,Park YK,Nishiwaki H,Hammock BD,Nishi K

更新日期：2015-11-15 00:00:00
A novel assay revealed that ribonucleotide reductase is functionally important for interstrand DNA crosslink repair.
abstract：:Cells have evolved complex biochemical pathways for DNA interstrand crosslink (ICL) removal. Despite the chemotherapeutic importance of ICL repair, there have been few attempts to identify which mechanistic DNA repair inhibitor actually inhibits ICL repair. To identify such compounds, a new and robust ICL repair assay...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.09.045

authors： Fujii N,Evison BJ,Actis ML,Inoue A

更新日期：2015-11-01 00:00:00
Toward the discovery of dual HCMV-VZV inhibitors: Synthesis, structure activity relationship analysis, and cytotoxicity studies of long chained 2-uracil-3-yl-N-(4-phenoxyphenyl)acetamides.
abstract：:The need for novel therapeutic options to fight herpesvirus infections still persists. Herein we report the design, synthesis and antiviral evaluation of a new family of non-nucleoside antivirals, derived from 1-[ω-(4-bromophenoxy)alkyl]uracil derivatives--previously reported inhibitors of human cytomegalovirus (HCMV)...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.09.033

authors： Babkov DA,Khandazhinskaya AL,Chizhov AO,Andrei G,Snoeck R,Seley-Radtke KL,Novikov MS

更新日期：2015-11-01 00:00:00
Design, synthesis and antibacterial study of new potent and selective coumarin-chalcone derivatives for the treatment of tenacibaculosis.
abstract：:With the aim of finding new chemical entities selective for fish pathogens to avoid drug resistance in humans, a series of coumarin-chalcone hybrid compounds with different patterns of substitution were designed and synthesized. Their antibacterial activity was evaluated against important types of human bacteria strai...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.09.028

authors： Vazquez-Rodriguez S,Lama López R,Matos MJ,Armesto-Quintas G,Serra S,Uriarte E,Santana L,Borges F,Muñoz Crego A,Santos Y

更新日期：2015-11-01 00:00:00
Design, synthesis, and biological evaluation of amide imidazole derivatives as novel metabolic enzyme CYP26A1 inhibitors.
abstract：:All-trans-retinoic acid (ATRA) as a physiological metabolite of vitamin A is widely applied in the treatment of cancer, skin, neurodegenerative and autoimmune diseases. CYP26A1 enzyme, induced by ATRA in liver and target tissues, metabolizes ATRA into 4-hydroxyl-RA. Inhibition of CYP26A1 metabolic enzyme represents a ...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.08.019

authors： Sun B,Liu K,Han J,Zhao LY,Su X,Lin B,Zhao DM,Cheng MS

更新日期：2015-10-15 00:00:00
Elaboration of a fragment library hit produces potent and selective aspartate semialdehyde dehydrogenase inhibitors.
abstract：:Aspartate-β-semialdehyde dehydrogenase (ASADH) lies at the first branch point in the aspartate metabolic pathway which leads to the biosynthesis of several essential amino acids and some important metabolites. This pathway is crucial for many metabolic processes in plants and microbes like bacteria and fungi, but is a...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.09.017

authors： Thangavelu B,Bhansali P,Viola RE

更新日期：2015-10-15 00:00:00
1,3,7-Triethyl-substituted xanthines--possess nanomolar affinity for the adenosine A1 receptor.
abstract：:Adenosine A1 receptors are attracting great interest as drug targets for their role in cognitive deficits. Antagonism of the adenosine A1 receptor may offer therapeutic benefits in complex neurological diseases, such as Alzheimer's and Parkinson's disease. The aim of this study was to discover potential selective aden...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.09.012

authors： Van der Walt MM,Terre'Blanche G

更新日期：2015-10-15 00:00:00
Effect of alkyl group on transnitrosation of N-nitrosothiazolidine thiocarboxamides.
abstract：:S-Nitrosoglutathione (GSNO) relaxes vascular smooth muscles, prevents platelet aggregation, and acts as a potential in vivo nitric oxide donor. 3-Nitroso-1,3-thiazolidine-4-thiocarboxamide (1), a N-nitrosothio-proline analogue, exhibited a high GSNO formation activity. In this study, two compounds (2 and 3) based on c...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.09.008

authors： Inami K,Ono Y,Kondo S,Nakanishi I,Ohkubo K,Fukuzumi S,Mochizuki M

更新日期：2015-10-15 00:00:00
Synthesis, electronic properties, antioxidant and antibacterial activity of some new benzimidazoles.
abstract：:Two groups of benzimidazole derivatives were synthesized using as precursors 5(6)-substituted 2-mercapto-benzimidazol-thiols and their antioxidant activity was investigated using TBA-MDA test. In the group of 1,3-disubstituted-benzimidazol-2-imines the highest lipid peroxidation inhibition effect 74.04% (IC₅₀=141.89 μ...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.08.029

authors： Mavrova ATs,Yancheva D,Anastassova N,Anichina K,Zvezdanovic J,Djordjevic A,Markovic D,Smelcerovic A

更新日期：2015-10-01 00:00:00
Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation.
abstract：:Protein phosphatase magnesium-dependent 1δ (PPM1D, Wip1) is a p53 inducible serine/threonine phosphatase. PPM1D is a promising target protein in cancer therapy since overexpression, missense mutations, truncating mutations, and gene amplification of PPM1D are reported in many tumors, including breast cancer and neurob...

journal_title：Bioorganic & medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.bmc.2015.08.042

authors： Ogasawara S,Kiyota Y,Chuman Y,Kowata A,Yoshimura F,Tanino K,Kamada R,Sakaguchi K

更新日期：2015-10-01 00:00:00

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