Synthesis and antibacterial activity of N-[2-[5-(methylthio)thiophen-2-yl]-2-oxoethyl] and N-[2-[5-(methylthio)thiophen-2-yl]-2-(oxyimino)ethyl]piperazinylquinolone derivatives.

abstract：:A series of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker was synthesized for antitumor evaluation. The carbamate or carbonate linker is able to lower the reactivity of the phenyl N-mustard pharmacophore and thus, these conjugates are rather chemically stable. The in vitro studies r...

journal_title：Bioorganic & medicinal chemistry

authors： Kapuriya N,Kapuriya K,Dong H,Zhang X,Chou TC,Chen YT,Lee TC,Lee WC,Tsai TH,Naliapara Y,Su TL

更新日期：2009-02-01 00:00:00

abstract：:Protein geranylgeranylation reactions are dependent on the availability of geranylgeranyl diphosphate (GGDP), which serves as the isoprenoid donor. Inhibition of GGDP synthase (GGDPS) is of interest from a drug development perspective as GGDPS inhibition results in impaired protein geranylgeranylation, which in multip...

journal_title：Bioorganic & medicinal chemistry

authors： Wills VS,Metzger JI,Allen C,Varney ML,Wiemer DF,Holstein SA

更新日期：2017-04-15 00:00:00

abstract：:Avermectin B1a (1) is a potent anthelmintic, insecticide, miticide and chloride channel activator on interaction with a specific nerve membrane site analyzed by binding assays with [3H]1. Candidate photoaffinity probes were prepared replacing the dioleandrosyl substituent with potential isosteric esters and ethers app...

journal_title：Bioorganic & medicinal chemistry

authors： Tsukamoto Y,Cole LM,Casida JE

更新日期：2000-01-01 00:00:00

abstract：:Enantiomerically pure (S)-atenolol was prepared by using (R,R) salen Co(III) complex for the resolution of terminal epoxide. This process was carried out at room temperature in excellent enantio selectivity. The method can be applied for large-scale preparation of (S)-atenolol without any problem. ...

journal_title：Bioorganic & medicinal chemistry

authors： Bose DS,Venkat Narsaiah A

更新日期：2005-02-01 00:00:00

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

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

abstract：:A library of 1,4-benzodiazepines has been synthesised and evaluated for activity against Trypanosoma brucei, a causative parasite of Human African Trypanosomiasis (HAT). The most potent of these derivatives has an MIC value of 0.97 μM. Herein we report the design, synthesis and biological evaluation of the abovementio...

journal_title：Bioorganic & medicinal chemistry

authors： Clark RL,Clements CJ,Barrett MP,Mackay SP,Rathnam RP,Owusu-Dapaah G,Spencer J,Huggan JK

更新日期：2012-10-15 00:00:00

abstract：:Flaviviruses, such as Dengue (DENV) and Zika (ZIKV) viruses, represent a severe health burden. There are currently no FDA-approved treatments, and vaccines against most flaviviruses are still lacking. We have developed several flexible analogues ("fleximers") of the FDA-approved nucleoside Acyclovir that exhibit activ...

journal_title：Bioorganic & medicinal chemistry

authors： Thames JE,Waters CD 3rd,Valle C,Bassetto M,Aouadi W,Martin B,Selisko B,Falat A,Coutard B,Brancale A,Canard B,Decroly E,Seley-Radtke KL

更新日期：2020-08-31 00:00:00

abstract：:The multi-step ligand action to a target protein is an important aspect when understanding mechanisms of ligand binding and discovering new drugs. However, structurally capturing such complex mechanisms is challenging. This is particularly true for interactions between large membrane proteins and small molecules. One ...

journal_title：Bioorganic & medicinal chemistry

authors： Niitsu A,Egawa A,Ikeda K,Tachibana K,Fujiwara T

更新日期：2018-11-15 00:00:00

abstract：:In search of potent beta(3)-adrenergic receptor agonists, a series of novel substituted 1,2,3,4-tetrahydroquinolin-6-yloxypropanes has been synthesized and evaluated for their beta(3)-adrenergic receptor agonistic activity (ranging from -17.73% to 90.64% inhibition at 10 microM) using well established Human SK-N-MC ne...

journal_title：Bioorganic & medicinal chemistry

authors： Shakya N,Roy KK,Saxena AK

更新日期：2009-01-15 00:00:00

abstract：:Histone deacetylases (HDACs) have been found to be biomarkers of cancers and the corresponding inhibitors have attracted much attention these years. Herein we reported a near-infrared fluorescent HDAC inhibitor based on vorinostat (SAHA) and a NIR fluorophore. This newly designed inhibitor showed similar inhibitory ac...

journal_title：Bioorganic & medicinal chemistry

authors： Huang Y,Ru HB,Bao B,Yu JH,Li J,Zang Y,Lu W

更新日期：2020-09-01 00:00:00

abstract：:Bacterial chemotactic responses are initiated when certain small molecules (i.e., carbohydrates, amino acids) interact with bacterial chemoreceptors. Although bacterial chemotaxis has been the subject of intense investigations, few have explored the influence of attractant structure on signal generation and chemotaxis...

journal_title：Bioorganic & medicinal chemistry

authors： Gestwicki JE,Strong LE,Borchardt SL,Cairo CW,Schnoes AM,Kiessling LL

更新日期：2001-09-01 00:00:00

abstract：:Twelve optically pure enantiomers were obtained using either crystallization or chiral high performance liquid chromatography (HPLC) separation methodologies to resolve six racemic sigma-1 (σ1) receptor ligands. The in vitro binding affinities of each enantiomer for σ1, σ2 receptors and vesicular acetylcholine transpo...

journal_title：Bioorganic & medicinal chemistry

authors： Yue X,Jin H,Luo Z,Liu H,Zhang X,McSpadden ED,Tian L,Flores HP,Perlmutter JS,Parsons SM,Tu Z

更新日期：2017-02-15 00:00:00

abstract：:Radioligand therapy (RLT) using prostate-specific membrane antigen (PSMA) targeting ligands is an attractive option for the treatment of Prostate cancer (PCa) and its metastases. We report herein a series of radioiodinated glutamate-urea-lysine-phenylalanine derivatives as new PSMA ligands in which l-tyrosine and l-gl...

journal_title：Bioorganic & medicinal chemistry

authors： Yao X,Zha Z,Ploessl K,Choi SR,Zhao R,Alexoff D,Zhu L,Kung HF

更新日期：2020-03-01 00:00:00

abstract：:The synthesis of 7-oxo and 7-hydroxy trifluoroallocolchicinoids was achieved through the intramolecular cyclization of o-phenyl-β-phenylalanines. The resulting compounds were evaluated for their cytotoxic activity against KB cells and their inhibitory effect towards the polymerization of tubulin. The results yielded s...

journal_title：Bioorganic & medicinal chemistry

authors： Chosson E,Santoro F,Rochais C,Santos JS,Legay R,Thoret S,Cresteil T,Sinicropi MS,Besson T,Dallemagne P

更新日期：2012-04-15 00:00:00

abstract：:An analogue 2 of coenzyme A (CoA) has been prepared in which the geminal methyl groups are replaced with hydrogens. An NMR titration study was conducted and shifts in frequency of protons in the pantetheine portion of the molecule upon titration of the adenine base were observed as has been previously reported with Co...

journal_title：Bioorganic & medicinal chemistry

authors： Vogel KW,Stark LM,Mishra PK,Yang W,Drueckhammer DG

更新日期：2000-10-01 00:00:00

abstract：:Therapeutic development of a targeted agent involves a series of decisions over additional activities that may be ignored, eliminated or pursued. This paper details the concurrent application of two methods that provide a spectrum of information about the biological activity of a compound: biochemical profiling on a l...

journal_title：Bioorganic & medicinal chemistry

authors： Ross-Macdonald P,de Silva H,Patel V,Truong A,He A,Neuhaus I,Tilford C,Ji R,Siemers N,Greer A,Carboni J,Gottardis M,Menard K,Lee F,Dodier M,Frennesson D,Sampognaro A,Saulnier M,Trainor G,Vyas D,Zimmermann K,Wittm

更新日期：2012-03-15 00:00:00

abstract：:Three fluoroalkylated derivatives (1-3) of the selective estrogen receptor modulator (SERM), raloxifene, have been synthesized. The key step in the synthesis is the C-C bond formation of benzo[b]thiophene and a substituted phenyl group (ring C) using a Stille reaction. The in vitro binding affinities of the substitute...

journal_title：Bioorganic & medicinal chemistry

authors： Lee KC,Moon BS,Lee JH,Chung KH,Katzenellenbogen JA,Chi DY

更新日期：2003-08-15 00:00:00

abstract：:Even number fatty acid residues-docosanoyl (behenoyl) and stearoyl were selected for introduction to the N(4)-position of (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine) (HPMPC, cidofovir), and its 5-azacytosine counterpart, (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine) (HPMP-5-azaC) with the aim to prep...

journal_title：Bioorganic & medicinal chemistry

authors： Krečmerová M,Pohl R,Masojídková M,Balzarini J,Snoeck R,Andrei G

更新日期：2014-05-15 00:00:00

abstract：:Antioxidant activity in α- and β-chitosan at a wide range of molecular weight (Mw) and chitosan concentration (CS) was determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, reducing ability, chelating ability, and hydroxyl radical scavenging activity. The form of chitosan (FC) had significant...

journal_title：Bioorganic & medicinal chemistry

authors： Jung J,Zhao Y

更新日期：2012-05-01 00:00:00

abstract：:The trans-2,3-disubstituted piperidine, quinazolinone-containing natural product febrifugine (also known as dichroine B) and its synthetic analogue, halofuginone, possess antimalarial activity. More recently studies have also shown that halofuginone acts as an agent capable of reducing fibrosis, an indication with cli...

journal_title：Bioorganic & medicinal chemistry

authors： McLaughlin NP,Evans P,Pines M

更新日期：2014-04-01 00:00:00

abstract：:3-Amino-2-hydroxy-propionaldehydes [H2NCH(R)CHOHCHO with R = H, i-Bu, CH2Ph] were designed as metallo-aminopeptidase inhibitors based on the metal active site chelation concept. These compounds were found to be micromolar inhibitors of aminopeptidase-M (AP-M, EC 3.4.11.2) with potencies similar to bestatin (Ki = 3.5 m...

journal_title：Bioorganic & medicinal chemistry

authors： Tarnus C,Rémy JM,d'Orchymont H

更新日期：1996-08-01 00:00:00

abstract：:The preparation and biological evaluation of a novel series of dimeric epothilone A derivatives (1-6) are described. Two types of diacyl spacers were introduced to establish the various dimeric epothilone A constructs. The effect of these compounds on tubulin polymerization and their cytotoxicity against four differen...

journal_title：Bioorganic & medicinal chemistry

authors： Passarella D,Comi D,Cappelletti G,Cartelli D,Gertsch J,Quesada AR,Borlak J,Altmann KH

更新日期：2009-11-01 00:00:00

abstract：:8-Chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide, monohydrochloride (1, SC-51089) is a functional PGE2 antagonist selective for the EP1 receptor subtype with antinociceptive activity. Analogues of SC-51089, in which the diacylhydrazine moiety has been replaced with 2,...

journal_title：Bioorganic & medicinal chemistry

authors： Hallinan EA,Hagen TJ,Tsymbalov S,Stapelfeld A,Savage MA

更新日期：2001-01-01 00:00:00

abstract：:The first committed step in lipid A biosynthesis is catalyzed by uridine diphosphate-(3-O-(R-3-hydroxymyristoyl))-N-acetylglucosamine deacetylase (LpxC), a zinc-dependent deacetylase, and inhibitors of LpxC may be useful in the development of antibacterial agents targeting a broad spectrum of Gram-negative bacteria. H...

journal_title：Bioorganic & medicinal chemistry

authors： Shin H,Gennadios HA,Whittington DA,Christianson DW

更新日期：2007-04-01 00:00:00

abstract：:3-(4-Piperidinyl)-5-arylpyrazoles, such as 1, were selective for the cloned human dopamine D4 receptor (hD4), but also showed affinity at voltage sensitive calcium, sodium and potassium ion channels. A combination of substituent changes to reduce the basicity of the piperidine nitrogen and conformational restriction t...

journal_title：Bioorganic & medicinal chemistry

authors： Collins I,Rowley M,Davey WB,Emms F,Marwood R,Patel S,Patel S,Fletcher A,Ragan IC,Leeson PD,Scott AL,Broten T

更新日期：1998-06-01 00:00:00

abstract：:Dicationic 2,6-diphenylpyrazines, aza-analogues and prodrugs were synthesized; evaluated for DNA affinity, activity against Trypanosoma brucei rhodesiense (T. b. r.) and Plasmodium falciparum (P. f.) in vitro, efficacy in T. b. r. STIB900 acute and T. b. brucei GVR35 CNS mouse models. Most diamidines gave poly(dA-dT)2...

journal_title：Bioorganic & medicinal chemistry

authors： Hu L,Patel A,Bondada L,Yang S,Wang MZ,Munde M,Wilson WD,Wenzler T,Brun R,Boykin DW

更新日期：2013-11-01 00:00:00

abstract：:A series of fifteen N4-benzyl substituted 5-nitroisatin-3-thiosemicarbazones 5a-o was synthesized and evaluated for urease inhibitory, phytotoxic and cytotoxic influences. All the compounds proved to be highly potent inhibitors of the enzyme, showing inhibitory activity (IC50=0.87±0.25-8.09±0.23μM) much better than th...

journal_title：Bioorganic & medicinal chemistry

authors： Pervez H,Khan N,Zaib S,Yaqub M,Naseer MM,Tahir MN,Iqbal J

更新日期：2017-02-01 00:00:00

abstract：:An amine group was synthesized starting from an optically active bicyclo[2.2.1]heptane compound, which was then used to build the 5 atoms ring of a key 6-chloropurine intermediate. This was then reacted with ammonia and selected amines obtaining new adenine- and 6-substituted adenine conformationally constrained carbo...

journal_title：Bioorganic & medicinal chemistry

authors： Tănase CI,Drăghici C,Căproiu MT,Shova S,Mathe C,Cocu FG,Enache C,Maganu M

更新日期：2014-01-01 00:00:00

abstract：:Fluorinated derivatives of 1,4-naphthoquinones are highly potent inhibitors of Cdc25A and Cdc25B phosphatases and growth of tumor cells. Eight new derivatives of polyfluoro-1,4-naphthoquinone were synthesized and their cytotoxicity in human myeloma, human mammary adenocarcinoma, mouse fibroblasts and primary mouse fib...

journal_title：Bioorganic & medicinal chemistry

authors： Zakharova OD,Ovchinnikova LP,Goryunov LI,Troshkova NM,Shteingarts VD,Nevinsky GA

更新日期：2011-01-01 00:00:00

abstract：:Filamenting temperature-sensitive mutant Z (FtsZ) is recognized as a promising target for new antibiotics development because of its high conservatism and pivotal role in the bacteria cell division. The aromatic heterocyclic scaffold of indole is known showing merit medical functions in antiviral and antimicrobial. In...

journal_title：Bioorganic & medicinal chemistry

authors： Cai S,Yuan W,Li Y,Huang X,Guo Q,Tang Z,Fang Z,Lin H,Wong WL,Wong KY,Lu YJ,Sun N

更新日期：2019-04-01 00:00:00