Preparation, antimicrobial evaluation, and mutagenicity of [2-hydroxyaryl]-[1-methyl-5-nitro-1H-2-imidazolyl]methanols , [5-tert-butyl-2-methylaminophenyl]-[1-methyl-5-nitro-1H-2-imidazo lyl]me thanol, and [2-hydroxyaryl]-[1-methyl-5-nitro-1H-2-imidazolyl

abstract：:A series of novel hybrids of metronidazole and berberine as new type of antimicrobial agents were synthesized and characterized by (1)H NMR, (13)C NMR, IR, MS and HRMS spectra. Bioactive assay manifested that most of the prepared compounds exhibited effective antibacterial and antifungal activities and some showed com...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang L,Chang JJ,Zhang SL,Damu GL,Geng RX,Zhou CH

更新日期：2013-07-15 00:00:00

abstract：:Herpes Simplex Virus (HSV) infections are among the most common human diseases. In this work, we assess the structural features and electronic properties of a series of ten 1-hydroxyacridone derivatives (1a-j) recently described as a new class of non-nucleoside inhibitors of Herpes Simplex Virus-1 (HSV-1). Based on th...

journal_title：Bioorganic & medicinal chemistry

authors： Bernardino AM,Castro HC,Frugulhetti IC,Loureiro NI,Azevedo AR,Pinheiro LC,Souza TM,Giongo V,Passamani F,Magalhães UO,Albuquerque MG,Cabral LM,Rodrigues CR

更新日期：2008-01-01 00:00:00

abstract：:The farnesoid X receptor (FXR) belonging to the metabolic subfamily of nuclear receptors is a ligand-induced transcriptional activator. Its central function is the physiological maintenance of bile acid homeostasis including the regulation of glucose and lipid metabolism. Accessible structural information about its li...

journal_title：Bioorganic & medicinal chemistry

authors： Grienke U,Mihály-Bison J,Schuster D,Afonyushkin T,Binder M,Guan SH,Cheng CR,Wolber G,Stuppner H,Guo DA,Bochkov VN,Rollinger JM

更新日期：2011-11-15 00:00:00

abstract：:Microsomal prostaglandin E(2) synthase-1 (mPGES-1) has been recognized as novel, promising drug target for anti-inflammatory and anticancer drugs. mPGES-1 catalyzes the synthesis of the inducible prostaglandin E(2) in response to pro-inflammatory stimuli, rendering this enzyme extremely interesting in drug discovery p...

journal_title：Bioorganic & medicinal chemistry

authors： De Simone R,Bruno I,Riccio R,Stadler K,Bauer J,Schaible AM,Laufer S,Werz O

更新日期：2012-08-15 00:00:00

abstract：:An efficient and modular one-pot synthesis of polysubstituted aromatic amines by a mild reductive amination procedure is described and the biological potential of these nitrogen-centered compounds is demonstrated by growth inhibition of murine connective tissue cells and microscopy-based morphological studies. ...

journal_title：Bioorganic & medicinal chemistry

authors： Menche D,Arikan F,Li J,Rudolph S,Sasse F

更新日期：2007-12-01 00:00:00

abstract：:A series of benzazolone compounds were synthesized utilizing benzoxazolinonic and benzothiazolinonic heterocycles as the building unit. The antioxidant activity of these compounds was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO(4) or 2,2'-azobis(2-amidinopro...

journal_title：Bioorganic & medicinal chemistry

authors： Yekini I,Hammoudi F,Martin-Nizard F,Yous S,Lebegue N,Berthelot P,Carato P

更新日期：2009-11-15 00:00:00

abstract：:Soluble epoxide hydrolase (sEH) is a component of the arachidonic acid cascade and is a candidate target for therapies for hypertension or inflammation. Although many sEH inhibitors are available, their scaffolds are not structurally diverse, and knowledge of their specific interactions with sEH is limited. To obtain ...

journal_title：Bioorganic & medicinal chemistry

authors： Amano Y,Yamaguchi T,Tanabe E

更新日期：2014-04-15 00:00:00

abstract：:Thirteen anthraquinone derivatives 5-17 including two 3-(3-alkylaminopropoxy)-9,10-anthraquinone (NHA) derivatives 5 and 6, and 11 1-hydroxy-3-(3-alkylaminopropoxy)-9,10-anthraquinone (MHA) derivatives 7-17 were synthesized, evaluated for cytotoxicities against two cancer cell lines, and assayed the generation of reac...

journal_title：Bioorganic & medicinal chemistry

authors： Tu HY,Huang AM,Teng CH,Hour TC,Yang SC,Pu YS,Lin CN

更新日期：2011-09-15 00:00:00

abstract：:The intestinal absorption of an intact oligopeptide was investigated in rats using a synthetic cationic peptide, 001-C8 (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH2). The peptide was coupled with 4-nitrobenzo-2-oxa-1,3-diazole (NBD) to prepare a fluorescence-labeled derivative 001-C8-NBD (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH-NB...

journal_title：Bioorganic & medicinal chemistry

authors： Sai Y,Kajita M,Tamai I,Kamata M,Wakama J,Wakamiya T,Tsuji A

更新日期：1998-06-01 00:00:00

abstract：:We recently reported that 4-epi-jaspine B exhibits potent inhibitory activity towards sphingosine kinases (SphKs). In this study, we investigated the effects of modifying the 2-alkyl group, as well as the functional groups on the THF ring of 4-epi-jaspine B using a diversity-oriented synthesis approach based on a late...

journal_title：Bioorganic & medicinal chemistry

authors： Ohno H,Honda M,Hamada N,Miyagaki J,Iwata A,Otsuki K,Maruyama T,Nakamura S,Nakanishi I,Inuki S,Fujii N,Oishi S

更新日期：2017-06-15 00:00:00

abstract：:A series of 3-(pyrazolyl)-1,2,5,6-tetrahydropyridine derivatives (B) was synthesized and tested for muscarinic activity in receptor binding assays using [3H]-oxotremorine-M (3H-OXO-M) and [3H]-pirenzepine (3H-PZ) as ligands. Potential muscarinic agonistic or antagonistic properties of the compounds were determined usi...

journal_title：Bioorganic & medicinal chemistry

authors： Plate R,Plaum MJ,de Boer T,Andrews JS,Rae DR,Gibson S

更新日期：1996-02-01 00:00:00

abstract：:We designed, synthesized and evaluated 13 novel tricyclic indeno[2,1-d]pyrimidines as RTK inhibitors. These analogues were synthesized via a Dieckmann condensation of 1,2-phenylenediacetonitrile followed by cyclocondensation with guanidine carbonate to afford the 2-amino-3,9-dihydro-indeno[2,1-d]pyrimidin-4-one. Sulfo...

journal_title：Bioorganic & medicinal chemistry

authors： Gangjee A,Zhao Y,Ihnat MA,Thorpe JE,Bailey-Downs LC,Kisliuk RL

更新日期：2012-07-15 00:00:00

abstract：:In continuing our screening program of naphthoquinone activity against Trypanosoma cruzi, the aetiological agent of Chagas' disease, new beta-lapachone-based 1,2,3-triazoles, 3-arylamino-nor-beta-lapachones, 3-alkoxy-nor-beta-lapachones and imidazole anthraquinones were synthesised and evaluated against bloodstream tr...

journal_title：Bioorganic & medicinal chemistry

authors： da Silva EN Jr,Guimarães TT,Menna-Barreto RF,Pinto Mdo C,de Simone CA,Pessoa C,Cavalcanti BC,Sabino JR,Andrade CK,Goulart MO,de Castro SL,Pinto AV

更新日期：2010-05-01 00:00:00

abstract：:The expression and function of endothelin (ET) receptors is abnormal in cardiovascular diseases, tumor progression, and tumor metastasis. In this study, we prepared two [(18)F]-fluorinated derivatives of the non-peptide ET(A) receptor antagonist PD 156707 and evaluated their ET receptor binding potencies. Ex vivo as w...

journal_title：Bioorganic & medicinal chemistry

authors： Höltke C,Law MP,Wagner S,Kopka K,Faust A,Breyholz HJ,Schober O,Bremer C,Riemann B,Schäfers M

更新日期：2009-10-15 00:00:00

abstract：:Both histone deacetylase (HDAC) and fibroblast growth factor receptor (FGFR) are important targets for cancer therapy. Although combining dual HDAC pharmacophore with tyrosine kinase inhibitors (TKIs) had achieved a successful progress, dual HDAC/FGFR1 inhibitors haven't been reported yet. Herein, we designed a series...

journal_title：Bioorganic & medicinal chemistry

authors： Liu J,Qian C,Zhu Y,Cai J,He Y,Li J,Wang T,Zhu H,Li Z,Li W,Hu L

更新日期：2018-02-01 00:00:00

abstract：:Several rationally designed analogs of 3-fluoro-2-oxo-3-phenylpropionic acid were chemically synthesized, and the reactions of the hydrate form of these compounds with 4-hydroxyphenylpyruvate dioxygenase from pig liver as inhibitors were examined. Compounds 14a and 14b were found to be potent competitive inhibitors of...

journal_title：Bioorganic & medicinal chemistry

authors： Ling TS,Shiu S,Yang DY

更新日期：1999-07-01 00:00:00

abstract：:In our previous study on discovering novel types of CCR3 antagonists, we found a fluoronaphthalene derivative (1) that exhibited potent CCR3 inhibitory activity with an IC(50) value of 20 nM. However, compound 1 also inhibited human cytochrome P450 2D6 (CYP2D6) with an IC(50) value of 400 nM. In order to reduce its CY...

journal_title：Bioorganic & medicinal chemistry

authors： Sato I,Morihira K,Inami H,Kubota H,Morokata T,Suzuki K,Iura Y,Nitta A,Imaoka T,Takahashi T,Takeuchi M,Ohta M,Tsukamoto S

更新日期：2008-09-15 00:00:00

abstract：:Caffeic acid esters, one of the components of propolis, are known to show a variety of biological effects such as anti-tumor, anti-oxidant, and anti-inflammatory activities. Although, the anti-inflammatory activities of caffeic acid esters have been studied by analyzing their structure, the detailed mechanisms of thei...

journal_title：Bioorganic & medicinal chemistry

authors： Uwai K,Osanai Y,Imaizumi T,Kanno S,Takeshita M,Ishikawa M

更新日期：2008-08-15 00:00:00

abstract：:A novel 7,6 fused bicyclic scaffold, pyrimido[4,5-b]azepine was designed to fit into the ATP binding site of the HER2/EGFR proteins. The synthesis of this scaffold was accomplished by an intramolecular Claisen-type condensation. As the results of optimization lead us to 4-anilino and 6-functional groups, we discovered...

journal_title：Bioorganic & medicinal chemistry

authors： Kawakita Y,Seto M,Ohashi T,Tamura T,Yusa T,Miki H,Iwata H,Kamiguchi H,Tanaka T,Sogabe S,Ohta Y,Ishikawa T

更新日期：2013-04-15 00:00:00

abstract：:Previously, bioassay-guided separation led us to isolate eleven novel steroidal alkaloids named cortistatins from the marine sponge Corticium simplex. These cortistatins were classified into three types based on the chemical structure of the side chain part, that is, isoquinoline, N-methyl piperidine or 3-methylpyridi...

journal_title：Bioorganic & medicinal chemistry

authors： Aoki S,Watanabe Y,Tanabe D,Arai M,Suna H,Miyamoto K,Tsujibo H,Tsujikawa K,Yamamoto H,Kobayashi M

更新日期：2007-11-01 00:00:00

abstract：:Lipoxygenases (LOXs) and cyclooxygenases (COXs) metabolize poly-unsaturated fatty acids into inflammatory signaling molecules. Modulation of the activity of these enzymes may provide new approaches for therapy of inflammatory diseases. In this study, we screened novel anacardic acid derivatives as modulators of human ...

journal_title：Bioorganic & medicinal chemistry

authors： Wisastra R,Kok PA,Eleftheriadis N,Baumgartner MP,Camacho CJ,Haisma HJ,Dekker FJ

更新日期：2013-12-15 00:00:00

abstract：:Cell invasion and migration are required for the parent solid tumor cells to metastasize to distant organs. Microtubules form a polarized network, enabling organelle and protein movement throughout the cell. Cytoskeletal elements coordinately regulate cell's motility, adhesion, migration, exocytosis, endocytosis, and ...

journal_title：Bioorganic & medicinal chemistry

authors： Abdel Bar FM,Khanfar MA,Elnagar AY,Badria FA,Zaghloul AM,Ahmad KF,Sylvester PW,El Sayed KA

更新日期：2010-01-15 00:00:00

abstract：:In an effort to expand the spectrum of activity of the oxazolidinone class of antibacterial agents to include Gram-negative bacteria, a series of new carbon-carbon linked pyrazolylphenyl analogues has been prepared. The alpha-N-substituted methyl pyrazole (10alpha) in the C3-linked series exhibited very good Gram-posi...

journal_title：Bioorganic & medicinal chemistry

authors： Lee CS,Allwine DA,Barbachyn MR,Grega KC,Dolak LA,Ford CW,Jensen RM,Seest EP,Hamel JC,Schaadt RD,Stapert D,Yagi BH,Zurenko GE,Genin MJ

更新日期：2001-12-01 00:00:00

abstract：:1,11-Didechloro-6-methyl-4'-O-demethyl rebeccamycin (JDC-108), a rebeccamycin analog possessing potent anti-tumor activities, was prepared via a concise one-pot strategy in good yield. The interaction between JDC-108 and human serum albumin (HSA) was studied by spectroscopic methods including fluorescence spectroscopy...

journal_title：Bioorganic & medicinal chemistry

authors： Cui F,Qin L,Zhang G,Liu X,Yao X,Lei B

更新日期：2008-08-15 00:00:00

abstract：:The over-expression of aminopeptidase N on diverse malignant cells is associated with the tumor angiogenesis and metastasis. In this report, one new series of leucine ureido derivatives containing the triazole moiety was designed, synthesized and evaluated as APN inhibitors. Among them, compound 13v showed the best AP...

journal_title：Bioorganic & medicinal chemistry

authors： Cao J,Ma C,Zang J,Gao S,Gao Q,Kong X,Yan Y,Liang X,Ding Q,Zhao C,Wang B,Xu W,Zhang Y

更新日期：2018-07-23 00:00:00

abstract：:Three potent antidepressants, (R)-nisoxetine, lortalamine, and oxaprotiline, with high affinity and high selectivity for the norepinephrine transporter (NET) were synthesized and radiolabeled with C-11 via [11C]methylation. The reference compounds and their corresponding normethyl precursors were synthesized via multi...

journal_title：Bioorganic & medicinal chemistry

authors： Lin KS,Ding YS

更新日期：2005-08-01 00:00:00

abstract：:The ability as P-glycoprotein (P-gp, ABCB1) modulators of thirty (1-30) triterpenoids of the cucurbitane-type was evaluated on human L5178 mouse T-lymphoma cell line transfected with the human MDR1 gene, through the rhodamine-123 exclusion assay. Compounds (1-26, and 29, 30) were previously obtained from the African m...

journal_title：Bioorganic & medicinal chemistry

authors： Ramalhete C,Mulhovo S,Molnar J,Ferreira MU

更新日期：2016-11-01 00:00:00

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：:The role of novel triazine derivatives against oxidative stress exerted by hydrogen peroxide on differentiated rat pheochromocytoma (PC12) cell line was examined and a consistent protection from H(2)O(2)-induced cell death, associated with a marked reduction in caspase-3 activation, was observed. Moreover, activation ...

journal_title：Bioorganic & medicinal chemistry

authors： Irannejad H,Amini M,Khodagholi F,Ansari N,Tusi SK,Sharifzadeh M,Shafiee A

更新日期：2010-06-15 00:00:00

abstract：:A series of thiosugar derivatives (thiolevomannosans) derived from mannose were synthesized and their inhibitory activity was tested against alpha-mannosidase (jack bean). These inhibitors were found to be more potent than the well-known inhibitors like kifunensine and deoxymannojirimycin based on docking and biochemi...

journal_title：Bioorganic & medicinal chemistry

authors： Sivapriya K,Hariharaputran S,Suhas VL,Chandra N,Chandrasekaran S

更新日期：2007-09-01 00:00:00