Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.

abstract：:Based on the findings that cholest-4-en-3-one, an intestinal metabolite of cholesterol, has an anti-obesity effect on animals, the structure-effect relationship of its 3-oxo derivatives and related compounds were investigated. Cholesten-3-ones, which possesses an enone structure with a carbonyl group at C3, markedly i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suzuki K,Shimizu T,Nakata T

更新日期：1998-08-18 00:00:00

abstract：:A series of 2,2-dimethyl-5-[4-(methylsulfonyl)phenyl]-4-phenyl-3(2H)furanones was prepared and evaluated for their ability to inhibit cyclo-oxygenase-2 (COX-2). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shin SS,Noh MS,Byun YJ,Choi JK,Kim JY,Lim KM,Ha JY,Kim JK,Lee CH,Chung S

更新日期：2001-01-22 00:00:00

abstract：:Cyclic and linear lipopeptides, burkholdine analogues, were synthesized by conventional Fmoc-SPPS and cyclisation with DIPC/HOBt in the solution phase. Synthesized peptides were evaluated for antifungal activities with MIC values against Saccharomyces cerevisiae and Aspergillus oryzae. As a result, the stereochemistry...

journal_title：Bioorganic & medicinal chemistry letters

authors： Konno H,Abumi K,Sasaki Y,Yano S,Nosaka K

更新日期：2015-08-15 00:00:00

abstract：:In order to investigate the relationship between tyrosine phosphorylation of β-catenin and transcriptional activity of β-catenin in Hela and Bcap-37 cells, genistein (a tyrosine kinase inhibitor) was used to inhibit tyrosine phosphorylation in cells. Our results showed the total β-catenin protein levels were mainly eq...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qian HY,Zhang DG,Wang HW,Pei DS,Zheng JN

更新日期：2014-06-01 00:00:00

abstract：:A series of novel 1-acetyl-3-(3,4-dimethoxypheny)-5-(4-(3-(arylureido/arylthioureido/arylsulfonamido) phenyl)-4,5-dihydropyrazole derivatives of biological interest have been prepared by sequential cyclization of 1-(4-nitrophenyl)-3-(3,4-dimethoxyphenyl)-pro-2-ene-1 with hydrazine hydrate, reduction followed by reacti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Keche AP,Hatnapure GD,Tale RH,Rodge AH,Kamble VM

更新日期：2012-11-01 00:00:00

abstract：:The first inhibitors of fungal protein: mannosyl transferase 1 (PMT1) are described. They are based upon rhodanine-3-acetic acid and several compounds have been identified, for example, 5-[[3-(1-phenylethoxy)-4-(2-phenylethoxy)phenyl]methylene]-4-oxo-2-thioxo-3-thiazolidineacetic acid (5a), which inhibit Candida albic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Orchard MG,Neuss JC,Galley CM,Carr A,Porter DW,Smith P,Scopes DI,Haydon D,Vousden K,Stubberfield CR,Young K,Page M

更新日期：2004-08-02 00:00:00

abstract：:Based on a screening lead from a yeast-based assay to identify Src family kinase inhibitors, a series of 4-anilino-7-thienyl-3-quinolinecarbonitriles was prepared. When the thiophene ring was substituted with a water-solubilizing group in a 2,5-, 3,5- or 2,4-pattern, potent inhibition of Src kinase activity was observ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Boschelli DH,Wang DY,Ye F,Yamashita A,Zhang N,Powell D,Weber J,Boschelli F

更新日期：2002-08-05 00:00:00

abstract：:A computer-aided drug design strategy leads to the identification of a new class of p38 inhibitors based on the 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) scaffold. The tolyl triazole amides provided a potent platform amenable to optimization. Further exploration leads to compounds with greater than 100-fold improveme...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cogan DA,Aungst R,Breinlinger EC,Fadra T,Goldberg DR,Hao MH,Kroe R,Moss N,Pargellis C,Qian KC,Swinamer AD

更新日期：2008-06-01 00:00:00

abstract：:Hippuristanol is a natural product that has recently been shown to inhibit eukaryotic translation initiation and tumor cell proliferation. To investigate the structure and activity relationship of hippuristanol, we synthesized a series of analogs by expanding the size of its F ring and determined their effects on the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li W,Dang Y,Liu JO,Yu B

更新日期：2010-05-15 00:00:00

abstract：:Hypoxia is a characteristic feature of solid tumors. Herein, we have developed novel hypoxia-sensitive probes (IM-ACs) for Raman spectroscopic analysis, consisting of nitroimidazole as a hypoxia-targeting unit and acetylene group as the signal-emitting unit. Among IM-ACs synthesized in this study, IM-AC possessing a d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kurihara R,Ikemura Y,Tanabe K

更新日期：2016-10-15 00:00:00

abstract：:Chimeric molecules which effect intracellular degradation of target proteins via E3 ligase-mediated ubiquitination (e.g., PROTACs) are currently of high interest in medicinal chemistry. However, these entities are relatively large compounds that often possess molecular characteristics which may compromise oral bioavai...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dragovich PS,Adhikari P,Blake RA,Blaquiere N,Chen J,Cheng YX,den Besten W,Han J,Hartman SJ,He J,He M,Rei Ingalla E,Kamath AV,Kleinheinz T,Lai T,Leipold DD,Li CS,Liu Q,Lu J,Lu Y,Meng F,Meng L,Ng C,Peng K,Le

更新日期：2020-02-15 00:00:00

abstract：:The steroidogenic enzyme 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) is a therapeutic target in the management of androgen-sensitive diseases such as prostate cancer and benign prostate hyperplasia. In this Letter, we designed and synthesized the first fluorescent inhibitor of this enzyme by combining a fluorog...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kenmogne LC,Maltais R,Poirier D

更新日期：2016-05-01 00:00:00

abstract：:Cocaine binds into beta-cyclodextrin, but not detectably into alpha- or gamma-cyclodextrin, in water solution. NMR studies indicate the geometry of the complex, which is confirmed by molecular mechanics calculations and binding studies on cocaine analogues and cyclodextrin dimers. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nesna N,Lou J,Breslow R

更新日期：2000-09-04 00:00:00

abstract：:The inhibition of ribonuclease Bi by 3'-N-hydroxyurea-3'-deoxythymidine 5'-phosphate is enhanced by 30-fold in the presence of Zn(2+). Thus, an N-hydroxyurea nucleotide can recruit Zn(2+) to inhibit the enzymatic activity of a ribonuclease. This result engenders a general strategy for the inhibition of non-metalloenzy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Higgin JJ,Yakovlev GI,Mitkevich VA,Makarov AA,Raines RT

更新日期：2003-02-10 00:00:00

abstract：:Currently, there is an ongoing interest in the synthesis of nucleoside diphosphate analogs as important regulators in catabolism/anabolism, and their potential applications as mechanistic probes and chemical tools for bioassays. However, the pyrophosphate bond formation step remains as the bottleneck. In this Digest, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu Z

更新日期：2015-09-15 00:00:00

abstract：:The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is disclosed. Compound 10i was identified as lead compound with a promising overall profile. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Belanger DB,Curran PJ,Hruza A,Voigt J,Meng Z,Mandal AK,Siddiqui MA,Basso AD,Gray K

更新日期：2010-09-01 00:00:00

abstract：:To make full use both of optical properties of quantum dots (QDs) and of specific interactions between aptamers and their ligands of interest, we employed QD-conjugated RNA aptamer interactions with histidine tag. QDs offer revolutionary fluorescence performance due to their long-term photostability, brilliant colors,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shin S,Kim IH,Kang W,Yang JK,Hah SS

更新日期：2010-06-01 00:00:00

abstract：:Retinoid X receptor (RXR) and Histone deacetylase (HDAC) are considered important targets for anti-cancer therapy due to their crucial roles in genetic or epigenetic regulations of cancer development and progression. Here, we have designed and synthesized a novel compound which targets both RXR and HADC. This dual-tar...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen GL,Wang LH,Wang J,Chen K,Zhao M,Sun ZZ,Wang S,Zheng HL,Yang JY,Wu CF

更新日期：2013-07-01 00:00:00

abstract：:A polyphemusin peptide analogue, T22 ([Tyr(5,12), Lys7]-polyphemusin II), and its shortened potent analogues, T134 (des-[Cys(8,13), Tyr(9,12)]-[D-Lys10, Pro11, L-citrulline16]-T22 without C-terminal amide) and T140 [[L-3-(2-naphthyl)alanine3]-T134], strongly inhibit the T-cell line-tropic (T-tropic) HIV-1 infection th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamamura H,Omagari A,Oishi S,Kanamoto T,Yamamoto N,Peiper SC,Nakashima H,Otaka A,Fujii N

更新日期：2000-12-04 00:00:00

abstract：:Incorporation of a 4-hydroxy-N-acetylprolinol nucleotide analogue at the 3'-terminus of DNA or 2-5A-DNA sequences resulted in a significantly enhanced 3'-exonuclease resistance while the affinity for complementary RNA was only slightly decreased. Furthermore, the binding to and activation of human RNase L by thus modi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Verheijen JC,van Roon AM,Meeuwenoord NJ,Stuivenberg HR,Bayly SF,Chen L,van der Marel GA,Torrence PF,van Boom JH

更新日期：2000-04-17 00:00:00

abstract：:We proposed a novel QSAR (quantitative structure-activity relationship) procedure called LERE (linear expression by representative energy terms)-QSAR involving molecular calculations such as ab initio fragment molecular orbital and generalized Born/surface area ones. We applied LERE-QSAR to two datasets for the free-e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Munei Y,Shimamoto K,Harada M,Yoshida T,Chuman H

更新日期：2011-01-01 00:00:00

abstract：:Bis(mu-hydroxo)diiron(III) complex, [Fe2III(mu-OH)2(NE)2](NO3)2 x 3H2O (3) (N-(4-nitro-2-hydroxy)phenylmethyl-N-(2-pyridylethyl)-N-(2-pyridylmethyl)amine = HNE, where H denotes a dissociable proton of the p-nitrophenol group), has been prepared and characterized by X-ray crystallography, electronic and magnetic spectr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kurosaki H,Yoshida H,Ito M,Koike H,Higuchi E,Goto M

更新日期：2001-03-26 00:00:00

abstract：:A novel class of 2,3-diaminopyridine bradykinin B1 receptor antagonists is disclosed. Structure-activity relationship studies (SARs) that led to compounds with significantly improved potency and pharmacokinetic properties relative to the lead compound are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng DM,Wai JM,Kuduk SD,Ng C,Murphy KL,Ransom RW,Reiss D,Chang RS,Harrell CM,MacNeil T,Tang C,Prueksaritanont T,Freidinger RM,Pettibone DJ,Bock MG

更新日期：2005-05-02 00:00:00

abstract：:A series of 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues were synthesized and evaluated for cytotoxic activity against eight human cancer cell lines. Compounds 18, 21, 28, 29, 30 and 31 showed cytotoxic activity with GI(50) values in the range of 2.1-8.1 microM concentration. Among these, compounds 21...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharma VM,Adi Seshu KV,Vamsee Krishna C,Prasanna P,Chandra Sekhar V,Venkateswarlu A,Rajagopal S,Ajaykumar R,Deevi DS,Rao Mamidi NV,Rajagopalan R

更新日期：2003-05-19 00:00:00

abstract：:Utilizing mefloquine as a scaffold, a next generation quinoline methanol (NGQM) library was constructed to identify early lead compounds that possess biological properties consistent with the target product profile for malaria chemoprophylaxis while reducing permeability across the blood-brain barrier. The library of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Milner E,McCalmont W,Bhonsle J,Caridha D,Carroll D,Gardner S,Gerena L,Gettayacamin M,Lanteri C,Luong T,Melendez V,Moon J,Roncal N,Sousa J,Tungtaeng A,Wipf P,Dow G

更新日期：2010-02-15 00:00:00

abstract：:We have developed versatile methods toward the synthesis of a variety of piperidine/piperazine bridged isosteres of pridopidine. The compounds were assessed against the D2 receptor in agonist and antagonist modes and against the D4 receptor in agonist mode. hERG Binding and the ADME profiles were studied. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Maertens G,Saavedra OM,Vece V,Reyes MAV,Hocine S,Öney E,Goument B,Mirguet O,Le Tiran A,Gloanec P,Hanessian S

更新日期：2018-08-15 00:00:00

abstract：:Oxygen dependent degradation of hypoxia-inducible factor (HIF)-1α is triggered with hydroxylation by proline hydroxylase domain 2 (PHD2) under normoxic conditions. Some of previously developed PHD2 inhibitors show a considerable potency against factor inhibiting HIF (FIH), the HIF asparagine hydroxylase. For specific ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kwon HS,Choi YK,Kim JW,Park YK,Yang EG,Ahn DR

更新日期：2011-07-15 00:00:00

abstract：:Benzothiazole benzimidazole (S)-isothiazolidinone ((S)-IZD) derivatives 5 were discovered through a peptidomimetic modification of the tripeptide (S)-IZD protein tyrosine phosphatase 1B (PTP1B) inhibitor 1. These derivatives are potent, competitive, and reversible inhibitors of PTP1B with improved caco-2 permeability....

journal_title：Bioorganic & medicinal chemistry letters

authors： Sparks RB,Polam P,Zhu W,Crawley ML,Takvorian A,McLaughlin E,Wei M,Ala PJ,Gonneville L,Taylor N,Li Y,Wynn R,Burn TC,Liu PC,Combs AP

更新日期：2007-02-01 00:00:00

abstract：:The design and synthesis of new 1alpha,25-dihydroxy-19-norvitamin D(3) analogues 3a-c, which have an amide bond in the molecule instead of the diene, are described. The A-ring moiety was constructed by a (3S,5S)-3,5-dihydroxypiperidine derivative (9, 11, or 13) prepared from D-mannose, and a CD-ring carboxylic acid 16...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suhara Y,Kittaka A,Ono K,Kurihara M,Fujishima T,Yoshida A,Takayama H

更新日期：2002-12-16 00:00:00

abstract：:The tertiary amide delta opioid agonist 2 is a potent antinociceptive agent. Compound 2 was metabolized in vitro and in vivo to secondary amide 3, a potent and selective micro opioid agonist. The SAR of a series of N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides was examined. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Carson JR,Coats SJ,Codd EE,Dax SL,Lee J,Martinez RP,McKown LA,Anne Neilson L,Pitis PM,Wu WN,Zhang SP

更新日期：2004-05-03 00:00:00