The chemical synthesis and antibiotic activity of a diverse library of 2-aminobenzimidazole small molecules against MRSA and multidrug-resistant A. baumannii.

abstract：:We are investigating compounds that could be useful in the treatment of neoplastic lesions of the cervix by acting on the oncoprotein E6 of human papillomavirus-16. The E6 protein contains two potential zinc-binding domains that are required for most of its functions. We have published tests that measure (i) the relea...

journal_title：Bioorganic & medicinal chemistry

authors： Beerheide W,Sim MM,Tan YJ,Bernard HU,Ting AE

更新日期：2000-11-01 00:00:00

abstract：:The synthesis of a series of new isothiazol-3(2H)-one 1,1-dioxides with halogenated (mostly fluorinated) pyridinyl and pentafluorophenyl substituents at 2-position is reported. These compounds (18-24) became easily accessible from 2-thiocyanato-1-carboxaldehydes and aminopyridines, pentafluoroaniline, respectively, by...

journal_title：Bioorganic & medicinal chemistry

authors： Eilfeld A,González Tanarro CM,Frizler M,Sieler J,Schulze B,Gütschow M

更新日期：2008-09-01 00:00:00

abstract：:3- And 4-imidazol-1-yl-methyl substituted biphenyl compounds (named as meta- and para-substituted compounds) were synthesized bearing additional substituents in 3'-/4'-position as inhibitors of P450 17 (17alpha-hydroxylase-C17,20-lyase). P450 17 is the key enzyme of androgen biosynthesis. Its inhibition is a novel the...

journal_title：Bioorganic & medicinal chemistry

authors： Wachall BG,Hector M,Zhuang Y,Hartmann RW

更新日期：1999-09-01 00:00:00

abstract：:Both the enantiomeric forms of DAU 5750, a novel muscarinic receptor antagonist, have been synthesized in order to assess the relevance of configurational/conformational features for high affinity binding to muscarinic receptor subtypes. The attribution of absolute stereochemistry and conformational analysis by means ...

journal_title：Bioorganic & medicinal chemistry

authors： Turconi M,Gozzo A,Schiavi G,Fronza G,Mele A,Bravo P

更新日期：1994-12-01 00:00:00

abstract：:This study aimed to investigate the relationships between structures of gene carrier molecules and their activities for gene delivery into cells. We compared 2 types of poly(L-lysine) as carriers, that is, dendritic poly(L-lysine) (KG6) and linear poly(L-lysine) (PLL). KG6 formed a neutral DNA complex, and its DNA com...

journal_title：Bioorganic & medicinal chemistry

authors： Yamagata M,Kawano T,Shiba K,Mori T,Katayama Y,Niidome T

更新日期：2007-01-01 00:00:00

abstract：:A series of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives (Ia-Il) were synthesized and biologically evaluated. It was found that Ig, the most active compound, antagonized both Ang II AT(1) and endothelin ET(A) receptors (AT(1) IC(50)=8.5, ET(A) IC(50)=8.9 nM), and was more potent than losartan in R...

journal_title：Bioorganic & medicinal chemistry

authors： Bai R,Wei Z,Liu J,Xie W,Yao H,Wu X,Jiang J,Wang Q,Xu J

更新日期：2012-08-01 00:00:00

abstract：:Novel 2-phenyl-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones (PQs) endowed with high affinity for central benzodiazepine receptor (BzR) were synthesized. In particular, 9-fluoro-2-(2-fluorophenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one (2(2)) showed binding affinity in the subnanomolar concentration range and p...

journal_title：Bioorganic & medicinal chemistry

authors： Carotti A,Altomare C,Savini L,Chiasserini L,Pellerano C,Mascia MP,Maciocco E,Busonero F,Mameli M,Biggio G,Sanna E

更新日期：2003-11-17 00:00:00

abstract：:Since overactivation of NMDA receptors is associated with neurodegenerative disorders, the design and development of subunit-selective NMDA receptor antagonists are of great interest. In order to avoid the formation of quinone-like intermediates as starting point for degradation the benzylic OH group of the lead compo...

journal_title：Bioorganic & medicinal chemistry

authors： Rath S,Schepmann D,Wünsch B

更新日期：2017-10-15 00:00:00

abstract：:Activity-based probes (ABPs) have found increasing use in functional proteomics studies. Recently, ABPs that can be employed in combination with click chemistry gained particular attention due to their flexible application in vitro and in vivo. Moreover, there is a continuous need for new ABPs that target small subset...

journal_title：Bioorganic & medicinal chemistry

authors： Haedke U,Götz M,Baer P,Verhelst SH

更新日期：2012-01-15 00:00:00

abstract：:We disclose herein our efforts aimed at discovery of selective PARP-1 and PARP-2 inhibitors. We have recently discovered several novel classes of quinazolinones, quinazolidinones, and quinoxalines as potent PARP-1 inhibitors, which may represent attractive therapeutic candidates. In PARP enzyme assays using recombinan...

journal_title：Bioorganic & medicinal chemistry

authors： Ishida J,Yamamoto H,Kido Y,Kamijo K,Murano K,Miyake H,Ohkubo M,Kinoshita T,Warizaya M,Iwashita A,Mihara K,Matsuoka N,Hattori K

更新日期：2006-03-01 00:00:00

abstract：:It was envisaged to combine high antipyretic activity of paracetamol into commonly used NSAIDs. To achieve this goal new chemical entities were synthesized by chemically combining paracetamol and NSAIDs, and biologically evaluated for their antipyretic, analgesic, anti-inflammatory and ulcerogenic potential. The acid ...

journal_title：Bioorganic & medicinal chemistry

authors： Yadav MR,Nimekar DM,Ananthakrishnan A,Brahmkshatriya PS,Shirude ST,Giridhar R,Parmar A,Balaraman R

更新日期：2006-12-15 00:00:00

abstract：:Several analogues of cirazoline (2), a selective alpha1-adrenoreceptor agonist, were prepared and their pharmacological profiles studied. Although at the alpha1-adrenoreceptor all the compounds displayed a significant agonist activity, at the alpha2-adrenoreceptor they showed either agonist or antagonist activity depe...

journal_title：Bioorganic & medicinal chemistry

authors： Pigini M,Quaglia W,Gentili F,Marucci G,Cantalamessa F,Franchini S,Sorbi C,Brasili L

更新日期：2000-05-01 00:00:00

abstract：:We investigated the carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the clinically used antitumor agent bortezomib, a marketed proteasome inhibitor, against all the catalytically active mammalian isoforms CA I-VII, IX, XII-XV. Bortezomib effectively inhibited all these CAs in the micromolar range. hCA II, t...

journal_title：Bioorganic & medicinal chemistry

authors： Supuran CT

更新日期：2017-10-01 00:00:00

abstract：:In recent years, special attention has been paid to the A3 adenosine receptor (A3AR) as a possible pharmacological target to treat intestinal inflammation. In this work, it was set up a novel method to quantify the concentration of a promising anti-inflammatory agent inside and outside of intestinal barrier using the ...

journal_title：Bioorganic & medicinal chemistry

authors： Buccioni M,Dal Ben D,Lambertucci C,Martí Navia A,Ricciutelli M,Spinaci A,Volpini R,Marucci G

更新日期：2019-08-01 00:00:00

abstract：:Previously, we reported the structural requirements of the cinnamic acid relatives for inhibition of snake venom hemorrhagic action. In the present study, we examined the effect of benzenepolycarboxylic acids and substituted benzoic acids against Protobothropsflavoviridis venom-induced hemorrhage. Pyromellitic acid (1...

journal_title：Bioorganic & medicinal chemistry

authors： Aung HT,Nikai T,Niwa M,Takaya Y

更新日期：2011-12-01 00:00:00

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

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

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

authors： Van der Walt MM,Terre'Blanche G

更新日期：2015-10-15 00:00:00

abstract：:V-RAF murine sarcoma viral oncogene homolog B1 (BRAF) is a serine/threonine-specific protein kinase that is mutated with high frequency in cutaneous melanoma, and many other cancers. Inhibition of mutant BRAF is an attractive therapeutic approach for the treatment of melanoma. A triarylimidazole BRAF inhibitor bearing...

journal_title：Bioorganic & medicinal chemistry

authors： Niculescu-Duvaz D,Niculescu-Duvaz I,Suijkerbuijk BM,Ménard D,Zambon A,Nourry A,Davies L,Manne HA,Friedlos F,Ogilvie L,Hedley D,Takle AK,Wilson DM,Pons JF,Coulter T,Kirk R,Cantarino N,Whittaker S,Marais R,Springer CJ

更新日期：2010-09-15 00:00:00

abstract：:Human urotensin II (hU-II; H-Glu-Thr-Pro-Asp-cyclo[Cys-Phe-Trp-Lys-Tyr-Cys]-Val-OH) is a disulfide bridged undecapeptide recently identified as the ligand of an orphan G protein-coupled receptor. hU-II has been described as the most potent vasoconstrictor compound identified to date. With the aim of replacing the disu...

journal_title：Bioorganic & medicinal chemistry

authors： Grieco P,Carotenuto A,Patacchini R,Maggi CA,Novellino E,Rovero P

更新日期：2002-12-01 00:00:00

abstract：:This paper reports the synthesis of new derivatives (formed by two indole systems separated by a central moiety) analogous of potent antitumor agents previously described. The activity of the bis-indoles bearing a pyridine core confirms the good result described in the previous paper and compound 4c was chosen for the...

journal_title：Bioorganic & medicinal chemistry

authors： Andreani A,Burnelli S,Granaiola M,Leoni A,Locatelli A,Morigi R,Rambaldi M,Varoli L,Landi L,Prata C,Dalla Sega FV,Caliceti C,Shoemaker RH

更新日期：2010-05-01 00:00:00

abstract：:The crystal structure of ABT-378 (lopinavir), bound to the active site of HIV-1 protease is described. A comparison with crystal structures of ritonavir, A-78791, and BILA-2450 shows some analogous features with previous reported compounds. A cyclic urea unit in the P(2) position of ABT-378 is novel and makes two bide...

journal_title：Bioorganic & medicinal chemistry

authors： Stoll V,Qin W,Stewart KD,Jakob C,Park C,Walter K,Simmer RL,Helfrich R,Bussiere D,Kao J,Kempf D,Sham HL,Norbeck DW

更新日期：2002-08-01 00:00:00

abstract：:A series of N'-substituted-2-(5-nitrofuran or 5-nitrothiophen-2-yl)-3H-benzo[d]imidazole-5-carbohydrazide derivatives were synthesized and investigated for their abilities to inhibit β-hematin formation, hemoglobin hydrolysis and in vivo for their antimalarial efficacy in rodent Plasmodium berghei. Selected analogues ...

journal_title：Bioorganic & medicinal chemistry

authors： Camacho J,Barazarte A,Gamboa N,Rodrigues J,Rojas R,Vaisberg A,Gilman R,Charris J

更新日期：2011-03-15 00:00:00

abstract：:Over the last several years we have synthesized and studied the in vitro and in vivo nAChR pharmacological properties of epibatidine (4) analogs. In this study we report the synthesis, nAChR in vitro and in vivo pharmacological properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs (5a-e and 6a-e). All ...

journal_title：Bioorganic & medicinal chemistry

authors： Ondachi PW,Ye Z,Castro AH,Luetje CW,Damaj MI,Mascarella SW,Navarro HA,Carroll FI

更新日期：2015-09-01 00:00:00

abstract：:A novel series of arylsulfonamide derivatives of (aryloxy)propyl piperidines was designed to obtain potent 5-HT7R antagonists. Among the compounds evaluated herein, 3-chloro-N-{1-[3-(1,1-biphenyl-2-yloxy)2-hydroxypropyl]piperidin-4-yl}benzenesulfonamide (25) exhibited antagonistic properties at 5-HT7R and showed selec...

journal_title：Bioorganic & medicinal chemistry

authors： Canale V,Partyka A,Kurczab R,Krawczyk M,Kos T,Satała G,Kubica B,Jastrzębska-Więsek M,Wesołowska A,Bojarski AJ,Popik P,Zajdel P

更新日期：2017-05-15 00:00:00

abstract：:In radiation therapy, adverse side effects are often induced due to the excessive cell death that occurs in radiosensitive normal cells. The radiation-induced cell death of normal cells is caused, at least in part, by apoptosis, which undergoes via activation of p53 and increase in the p53 protein, a zinc-containing t...

journal_title：Bioorganic & medicinal chemistry

authors： Ariyasu S,Sawa A,Morita A,Hanaya K,Hoshi M,Takahashi I,Wang B,Aoki S

更新日期：2014-08-01 00:00:00

abstract：:A continuous flow process is presented that enables the efficient synthesis and derivatization of 1,2,4-thiadiazole heterocycles. Special attention was given to the safe handling of the versatile yet hazardous trichloromethane sulfenylchloride reagent including its in-line quenching in order to eliminate malodourous a...

journal_title：Bioorganic & medicinal chemistry

authors： Baumann M,Baxendale IR

更新日期：2017-12-01 00:00:00

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

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

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

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

abstract：:Germanicane-type triterpenes allobetulin (3) and 28-oxoallobetulin (4) can be obtained by the Wagner-Meerwein rearrangement of the more available lupane-type triterpenes betulin (1) and betulinic acid (2), respectively. The medical uses of betulinic acid (2) and its derivatives are limited because of their poor hydros...

journal_title：Bioorganic & medicinal chemistry

authors： Thibeault D,Gauthier C,Legault J,Bouchard J,Dufour P,Pichette A

更新日期：2007-09-15 00:00:00

abstract：:The toxicity of the molecules currently used in the treatment of human cytomegalovirus (HCMV) in immunocompromised hosts often causes interruption of the therapy. Cyclodextrins (Cds), oligosaccharides possessing a hydrophobic cavity, have the property of forming inclusion complexes with a great number of molecules, im...

journal_title：Bioorganic & medicinal chemistry

authors： Nicolazzi C,Abdou S,Collomb J,Marsura A,Finance C

更新日期：2001-02-01 00:00:00