Recent progresses on synthesized LuxS inhibitors: A mini-review.

abstract：:A number of N-substituted piperazinylquinolone derivatives were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria. Preliminary results indicated that most compounds tested in this study demonstrated comparable or better activity against Staphylococcus aureus and Stap...

journal_title：Bioorganic & medicinal chemistry

authors： Foroumadi A,Oboudiat M,Emami S,Karimollah A,Saghaee L,Moshafi MH,Shafiee A

更新日期：2006-05-15 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：:Karavilagenin C (1), a cucurbitane-type triterpenoid, previously isolated from the aerial parts of Momordica balsamina, was acylated with different alkanoyl, aroyl and cinnamoyl chlorides/anydrides, yielding ten new mono or diesters, karavoates F (7) and H-P (8-16). Furthermore, the new compound cucurbalsaminol C (17)...

journal_title：Bioorganic & medicinal chemistry

authors： Ramalhete C,Lopes D,Molnár J,Mulhovo S,Rosário VE,Ferreira MJ

更新日期：2011-01-01 00:00:00

abstract：:The emergence of multidrug-resistant bacteria has created an urgent need for antibiotics with a novel mechanism of action. The bacterial cell division protein FtsZ is an attractive target for the development of novel antibiotics. The benzo[c]phenanthridinium sanguinarine and the dibenzo[a,g]quinolizin-7-ium berberine ...

journal_title：Bioorganic & medicinal chemistry

authors： Kelley C,Zhang Y,Parhi A,Kaul M,Pilch DS,LaVoie EJ

更新日期：2012-12-15 00:00:00

abstract：:There is still a need for additional scaffolds to further explore tissue selectivity and improving efficacy of selective estrogen receptor modulators (SERMs). A series of hydroxyl substituted diphenylnaphthyl alkene ligands for the two estrogen receptors are described that arose from an initial de novo designed diphen...

journal_title：Bioorganic & medicinal chemistry

authors： Schmidt JM,Tremblay GB,Plastina MA,Ma F,Bhal neé Basra S,Feher M,Dunn-Dufault R,Redden PR

更新日期：2005-03-01 00:00:00

abstract：:We have recently reported the discovery of numerous new compounds that are selective inhibitors of all of the subtypes of the adenosine receptor family via a pharmacophore database searching and screening strategy. During the course of this work we made the unexpected discovery of a potent A(2B) receptor antagonist, 4...

journal_title：Bioorganic & medicinal chemistry

authors： Webb TR,Lvovskiy D,Kim SA,Ji Xd,Melman N,Linden J,Jacobson KA

更新日期：2003-01-02 00:00:00

abstract：:This paper describes our recent efforts to design and synthesise potent and selective PDE5 inhibitors and the use of in vitro predictors of clearance, absorption and permeability to maximise the potential for dose-proportional pharmacokinetics and good oral bioavailability in man. Optimisation of the preclinical profi...

journal_title：Bioorganic & medicinal chemistry

authors： Rawson DJ,Ballard S,Barber C,Barker L,Beaumont K,Bunnage M,Cole S,Corless M,Denton S,Ellis D,Floc'h M,Foster L,Gosset J,Holmwood F,Lane C,Leahy D,Mathias J,Maw G,Million W,Poinsard C,Price J,Russel R,Street S

更新日期：2012-01-01 00:00:00

abstract：:Semiempirical quantum mechanical and molecular mechanics calculations were carried out to identify and characterize the steric and electronic properties that modulate ligand recognition and activation of the cerebellar GABAA/benzodiazepine (BDZ) receptor. For this hypothesis development, thirteen compounds belonging t...

journal_title：Bioorganic & medicinal chemistry

authors： Schove LT,Perez JJ,Loew GH

更新日期：1994-10-01 00:00:00

abstract：:High specificity has been an important feature in affinity labeling for target profiling. Especially, to label targets via rapidly progressing reactions with consumption of ligand (probe), high specificity of reaction with common functional groups of target protein should be achieved without reactions with similar gro...

journal_title：Bioorganic & medicinal chemistry

authors： Tomohiro T,Nakabayashi M,Sugita Y,Morimoto S

更新日期：2016-08-01 00:00:00

abstract：:Because the activation of matrix metalloproteinases (MMP) is a key factor in the metastatic process, compounds with the ability to inhibit MMP activity have a potential in the treatment of tumor. From the examination of 2000 plant extracts, obovatal isolated from the extract of the leaves of Magnolia obovata THUNB was...

journal_title：Bioorganic & medicinal chemistry

authors： Lee SK,Chun HK,Yang JY,Han DC,Son KH,Kwon BM

更新日期：2007-06-15 00:00:00

abstract：:One of the grand challenges in chemical biology is identifying a small-molecule modulator for each individual function of all human proteins. Instead of targeting one protein at a time, an efficient approach to address this challenge is to target entire protein families by taking advantage of the relatively high level...

journal_title：Bioorganic & medicinal chemistry

authors： Areias FM,Brea J,Gregori-Puigjané E,Zaki ME,Carvalho MA,Domínguez E,Gutiérrez-de-Terán H,Proença MF,Loza MI,Mestres J

更新日期：2010-05-01 00:00:00

abstract：:Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field. ...

journal_title：Bioorganic & medicinal chemistry

authors： Arredondo Y,Moreno-Mañas M,Pleixats R,Palacín C,Raga MM,Castelló JM,Ortiz JA

更新日期：1997-10-01 00:00:00

abstract：:Selenium-incorporated fucoses (seleno-fucoses) differing in the position of the seleno-substituent were synthesized and applied to the X-ray structural determination of a carbohydrate-lectin complex using single/multi-wavelength anomalous dispersion (SAD/MAD) phasing. The hydroxyl groups at the C-1, -2, -3 and -4 posi...

journal_title：Bioorganic & medicinal chemistry

authors： Shimabukuro J,Makyio H,Suzuki T,Nishikawa Y,Kawasaki M,Imamura A,Ishida H,Ando H,Kato R,Kiso M

更新日期：2017-02-01 00:00:00

abstract：:Bioassay-directed fractionation of the leaf and root extracts of the antiproliferative Madagascar plant Stuhlmannia moavi afforded 6-acetyl-5,8-dihydroxy-2-methoxy-7-methyl-1,4-naphthoquinone (stuhlmoavin, 1) as the most active compound, with an IC50 value of 8.1 μM against the A2780 human ovarian cancer cell line, as...

journal_title：Bioorganic & medicinal chemistry

authors： Liu Y,Harinantenaina L,Brodie PJ,Bowman JD,Cassera MB,Slebodnick C,Callmander MW,Randrianaivo R,Rakotobe E,Rasamison VE,Applequist W,Birkinshaw C,Lewis GP,Kingston DG

更新日期：2013-12-15 00:00:00

abstract：:A novel artificial peptide named HPH-Pep, comprising a pyridine and two histidine units, was synthesized. The HPH-Pep-CuII complex had unique pentacoordinated structure as shown by X-ray crystallography and exhibited superoxide-scavenging activity as indicated by ESR spectroscopy. The superoxide-quenching profile of H...

journal_title：Bioorganic & medicinal chemistry

authors： Otsuka M,Satake H,Murakami S,Doi M,Ishida T,Shibasaki M,Sugiura Y

更新日期：1996-10-01 00:00:00

abstract：:Anthraquinone-based compounds are attractive target for the design of new anticancer drugs. We have previously described a series of 1,5- and 1,4-difunctionalized anthraquinones, which exhibit different spectra of potency, together with human telomerase evaluation. The present study details the preparation of further,...

journal_title：Bioorganic & medicinal chemistry

authors： Huang HS,Chiu HF,Lee AL,Guo CL,Yuan CL

更新日期：2004-12-01 00:00:00

abstract：:We report the synthesis and properties of oligonucleotides incorporating N(6)-[N-(pyren-1-ylmethyl)carbamoyl]-deoxyadenosine (dA(pymcm)). We designed the ODN which incorporated two consecutive dA(pymcm) residues. It was revealed that on hybridization with the target DNA and RNA oligomers, the fluorescence spectra of O...

journal_title：Bioorganic & medicinal chemistry

authors： Seio K,Mizuta M,Tasaki K,Tamaki K,Ohkubo A,Sekine M

更新日期：2008-09-01 00:00:00

abstract：:BMS-986120 is a PAR4 antagonist that is being investigated as an antiplatelet agent in phase I clinical trial. An improved synthesis of BMS-986120 has been developed. Based on the novel synthetic approach to BMS-986120, a series of deuterated derivatives of BMS-986120 have been synthesized and biologically evaluated t...

journal_title：Bioorganic & medicinal chemistry

authors： Chen P,Ren S,Song H,Chen C,Chen F,Xu Q,Kong Y,Sun H

更新日期：2019-01-01 00:00:00

abstract：:A series of novel tetrahydropyrazolopyridone derivatives containing 1,3,4-triazole, triazolylmethyl, and partially saturated heterocyclic moieties as P2 binding element was designed, synthesized, and evaluated in vitro for anticoagulant activity in human and rabbit plasma. All compounds showed moderate to significant ...

journal_title：Bioorganic & medicinal chemistry

authors： Sun X,Hong Z,Liu M,Guo S,Yang D,Wang Y,Lan T,Gao L,Qi H,Gong P,Liu Y

更新日期：2017-05-15 00:00:00

abstract：:Ionophoric properties of dipyrazolic crowns and podands containing a 1,3-bis(1H-pyrazol-1-yl)propane unit in their structure are described. They show selectivity of ammonium vs alkali cations and interesting norepinephrine transport rates. A molecular modelling study has been used to elucidate the superstructures of t...

journal_title：Bioorganic & medicinal chemistry

authors： Rodríguez-Franco MI,Fierros M,Martínez A,Navarro P,Conde S

更新日期：1997-02-01 00:00:00

abstract：:The dysfunction and mutual compensatory activation of RAF-MEK-ERK and PI3K-PDK1-AKT pathways have been demonstrated as the hallmarks in several primary and recurrent cancers. The strategy of concurrent blocking of these two pathways shows clinical merits on effective cancer therapy, such as combinatory treatments and ...

journal_title：Bioorganic & medicinal chemistry

authors： Yu Z,Chen Z,Su Q,Ye S,Yuan H,Kuai M,Lv M,Tu Z,Yang X,Liu R,Hu G,Li Q

更新日期：2019-03-15 00:00:00

abstract：:The photoeffect of new proflavine derivatives with DNA-binding and antitumour activities, 3,6-bis((1-alkyl-5-oxo-imidazolidin-2-yliden)imino)acridine hydrochlorides (AcrDIMs), was studied to evaluate them as potential photosensitizers for photodynamic antitumor therapy. EPR measurements showed that superoxide radical ...

journal_title：Bioorganic & medicinal chemistry

authors： Cižeková L,Grolmusová A,Ipóthová Z,Barbieriková Z,Brezová V,Hunáková L,Imrich J,Janovec L,Dovinová I,Paulíková H

更新日期：2014-09-01 00:00:00

abstract：:Geranylgeranyl diphosphate synthase (GGDPS) inhibitors are of potential therapeutic interest as a consequence of their activity against the bone marrow cancer multiple myeloma. A series of bisphosphonates linked to an isoprenoid tail through an amide linkage has been prepared and tested for the ability to inhibit GGDP...

journal_title：Bioorganic & medicinal chemistry

authors： Goetz DB,Varney ML,Wiemer DF,Holstein SA

更新日期：2020-08-15 00:00:00

abstract：:Non-viral gene therapy is based on the development of efficient and safe gene carrier systems able to transfer DNA into cells. Polyethylenimine (PEI), the most promising non-viral vector, with its high cationic-charge-density potential is able (1) to compact DNA in complexes (polyplexes) smaller than those formed by l...

journal_title：Bioorganic & medicinal chemistry

authors： Masotti A,Moretti F,Mancini F,Russo G,Di Lauro N,Checchia P,Marianecci C,Carafa M,Santucci E,Ortaggi G

更新日期：2007-02-01 00:00:00

abstract：:Bioactive compounds present in grapefruit juice are known to increase the bioavailability of certain medications by acting as potent CYP 3A4 inhibitors. An efficient technique has been developed for isolation and purification of three furocoumarins. The isolated compounds have been tested for the inhibition of human C...

journal_title：Bioorganic & medicinal chemistry

authors： Girennavar B,Poulose SM,Jayaprakasha GK,Bhat NG,Patil BS

更新日期：2006-04-15 00:00:00

abstract：:The effect of 7,8-diacetoxy-4-methylcoumarin (DAMC) has been studied on hepatic NADPH cytochrome C reductase-- an enzyme participating in the microsomal electron transport. The preincubation of liver microsomes with DAMC resulted in a time-dependent activation of NADPH cytochrome C reductase. The catalytic activity of...

journal_title：Bioorganic & medicinal chemistry

authors： Raj HG,Parmar VS,Jain SC,Goel S,Singh A,Tyagi YK,Jha HN,Olsen CE,Wengel J

更新日期：1999-02-01 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：:Here we describe the design, synthesis, and pharmacological evaluation of a set of compounds structurally related to the high affinity serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide (6, LP-211). Specific structural modifications were performed in order to maintain affini...

journal_title：Bioorganic & medicinal chemistry

authors： Lacivita E,Niso M,Hansen HD,Di Pilato P,Herth MM,Lehel S,Ettrup A,Montenegro L,Perrone R,Berardi F,Colabufo NA,Leopoldo M,Knudsen GM

更新日期：2014-03-01 00:00:00

abstract：:Synthesis and pharmacological evaluation of a new series of cannabinoid receptor antagonists of indazole ether derivatives have been performed. Pharmacological evaluation includes radioligand binding assays with [3H]-CP55940 for CB1 and CB2 receptors and functional activity for cannabinoid receptors on isolated tissue...

journal_title：Bioorganic & medicinal chemistry

authors： González-Naranjo P,Pérez C,Girón R,Sánchez-Robles EM,Martín-Fontelles MI,Carrillo-López N,Martín-Vírgala J,Naves M,Campillo NE,Páez JA

更新日期：2020-10-01 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