Effective syntheses of 2',4'-BNANC monomers bearing adenine, guanine, thymine, and 5-methylcytosine, and the properties of oligonucleotides fully modified with 2',4'-BNANC.

abstract：:Two types of structural variants of D-myo-inositol 1,4,5-trisphosphate [Ins(1,4,5)P3] were prepared by a chemoenzymatic route. These 6-O-substituted analogues retained the biological activity of Ins(1,4,5)P3, and were able to elicit Ca2+ release from porcine brain microsomes. Moreover, these derivatives allowed the pr...

journal_title：Bioorganic & medicinal chemistry

authors： Gou DM,Shieh WR,Lu PJ,Chen CS

更新日期：1994-01-01 00:00:00

abstract：:A series of N-substituted desloratadine analogues were designed and synthesized. They were tested for H1 antihistamine activity by inhibiting histamine-induced contraction of isolated ileum muscles of guinea-pigs in vitro and inhibiting histamine-induced asthmatic reaction in guinea-pigs in vivo. All the evaluated com...

journal_title：Bioorganic & medicinal chemistry

authors： Lin Y,Wang Y,Sima LF,Wang DH,Cao XH,Chen LG,Chen B

更新日期：2013-07-15 00:00:00

abstract：:Four palladium(II) and platinum(II) saccharinate (sac) complexes with 2-(hydroxymethyl)pyridine (2-hmpy) and 2-(2-hydroxyethyl)pyridine (2-hepy), namely trans-[Pd(2-hmpy)2(sac)2]·H2O (1), trans-[Pt(2-hmpy)2(sac)2]·3H2O (2), trans-[Pd(2-hepy)2(sac)2] (3) and trans-[Pt(2-hepy)2(sac)2] (4), have been synthesized and char...

journal_title：Bioorganic & medicinal chemistry

authors： Ari F,Aztopal N,Icsel C,Yilmaz VT,Guney E,Buyukgungor O,Ulukaya E

更新日期：2013-11-01 00:00:00

abstract：:Glycamino acids, a family of sugar amino acids, are derivatives of C-glycosides that possesses a carboxyl group at the C-1 position and an amino group replacing one of the hydroxyl groups at either the C-2, 3, 4, or 6 position. We have prepared a series of glucose-type glycamino acids as monomeric building blocks: the...

journal_title：Bioorganic & medicinal chemistry

authors： Suhara Y,Yamaguchi Y,Collins B,Schnaar RL,Yanagishita M,Hildreth JE,Shimada I,Ichikawa Y

更新日期：2002-06-01 00:00:00

abstract：:The synthesis of a range of 2-amido-3-hydroxypyridin-4-ones as bidentate iron(III) chelators with potential for oral administration is described. The pKa values of the ligands together with the stability constants of their iron(III) complexes have been determined. Results indicate that the introduction of an amido sub...

journal_title：Bioorganic & medicinal chemistry

authors： Liu ZD,Piyamongkol S,Liu DY,Khodr HH,Lu SL,Hider RC

更新日期：2001-03-01 00:00:00

abstract：:Searching for new substances with antileishmanial activity, we synthesized and evaluated a series of α,α-difluorohydrazide and α,α-difluoramides against Leishmania amazonensis arginase (LaArg). Four α,α-difluorohydrazide derivatives showed activity against LaArg with Ki in the range of 1.3-26 μM. The study of the kine...

journal_title：Bioorganic & medicinal chemistry

authors： Crizanto de Lima E,Castelo-Branco FS,Maquiaveli CC,Farias AB,Rennó MN,Boechat N,Silva ER

更新日期：2019-09-01 00:00:00

abstract：:We describe the syntheses, physicochemical properties and biological evaluation of a novel series of complexones containing bis- or biazoles moieties and two iminodiacetic acid units as novel ligands for paramagnetic lanthanides. The complexones were prepared by reaction of the corresponding 1,1'-bishaloethylbi- or bi...

journal_title：Bioorganic & medicinal chemistry

authors： Mayoral EP,García-Amo M,López P,Soriano E,Cerdán S,Ballesteros P

更新日期：2003-12-01 00:00:00

abstract：:A series of 10 novel nitro-analogues of cryptolepine (1) has been synthesised and these compounds were evaluated for their in-vitro cytotoxic properties as well as their potential for reductive activation by the cytosolic reductase enzymes NQO1 and NQO2. Molecular modelling studies suggest that cryptolepine is able to...

journal_title：Bioorganic & medicinal chemistry

authors： Seville S,Phillips RM,Shnyder SD,Wright CW

更新日期：2007-10-01 00:00:00

abstract：:In this study, we disclose the design and synthesis of novel 4-susbtituted nipecotic acid derivatives as inhibitors of the GABA transporter mGAT1. Based on molecular modeling studies the compounds are assumed to adopt a binding pose similar to that of the potent mGAT1 inhibitor nipecotic acid. As substitution in 4-pos...

journal_title：Bioorganic & medicinal chemistry

authors： Hellenbrand T,Höfner G,Wein T,Wanner KT

更新日期：2016-05-01 00:00:00

abstract：:A number of 3,5-bis(benzylidene)-4-piperidones 1 and some N-4-(2-aminoethoxy)phenylcarbonyl analogs 3-6 display excellent in vitro antimycobacterial properties. In particular, 1c and 6d are potent antimycobacterials which are well tolerated in mice and are identified as important lead molecules. The nature of both the...

journal_title：Bioorganic & medicinal chemistry

authors： Das U,Das S,Bandy B,Stables JP,Dimmock JR

更新日期：2008-04-01 00:00:00

abstract：:Oligo/polysialic acids consisting of consecutive α(2,8)-linkages on gangliosides and glycoproteins play a role in cell adhesion and differentiation events in a manner that is dependent on the degree of polymerization (DP). Anti-oligo/polysialic acid antibodies often have DP-dependent antigenic specificity, and such un...

journal_title：Bioorganic & medicinal chemistry

authors： Hanashima S,Sato C,Tanaka H,Takahashi T,Kitajima K,Yamaguchi Y

更新日期：2013-10-01 00:00:00

abstract：:Several N-substituted quindolines were made to further evaluate the role of N-alkylation on the activity of indoloquinolines as antifungal agents. While N-5 substitution is required for these activities, N-10 alkylation alone leads to inactive products but is tolerated in the presence of N-5 alkyl groups. It was also ...

journal_title：Bioorganic & medicinal chemistry

authors： Mardenborough LG,Zhu XY,Fan P,Jacob MR,Khan SI,Walker LA,Ablordeppey SY

更新日期：2005-06-02 00:00:00

abstract：:Modified oligonucleotides, whose ON-OFF switch of hybridization can be controlled by an external stimulus, are important to understanding life phenomena and efficient treatment of diseases. The ON-OFF switch can be completely controlled by chemical modification of the oligonucleotide such as cyclization. However, thei...

journal_title：Bioorganic & medicinal chemistry

authors： Nishizawa S,Ohkubo A

更新日期：2020-12-01 00:00:00

abstract：:A series of potential substrates of gamma-aminobutyric acid aminotransferase (GABA-AT) with lipophilic bioisosteres of the carboxylic acid group (2-7) were synthesized and tested. Most of the synthesized compounds showed substrate activities with GABA-AT; 1H-tetrazole-5-propanamine (6) was the best of those tested. Th...

journal_title：Bioorganic & medicinal chemistry

authors： Yuan H,Silverman RB

更新日期：2006-03-01 00:00:00

abstract：:New 6-[(2'-dialkylamino)ethyl]-4(3H)-pyrimidinones were prepared by a multistep procedure starting from acetone dicarboxylic acid diethyl ester and urea derivatives. These compounds were used as starting materials to obtain 4-N,N-dialkyl-6-vinyl-pyrimidine derivatives by an unprecedented tandem C-6 side chain Hofmann-...

journal_title：Bioorganic & medicinal chemistry

authors： Saladino R,Ciambecchini U,Maga G,Mastromarino P,Conti C,Botta M

更新日期：2002-07-01 00:00:00

abstract：:The discovery of the non-peptide antiplatelet injectable agent FK419 is reported. Based on the beta-turn structure of RGD peptide sequences in the alpha chain of fibrinogen, which binds the glycoprotein IIb/IIIa (GPIIb/IIIa) on the surface of platelets to induce platelet aggregation, the prototype 2 was designed. Afte...

journal_title：Bioorganic & medicinal chemistry

authors： Yamanaka T,Ohkubo M,Kuroda S,Nakamura H,Takahashi F,Aoki T,Mihara K,Seki J,Kato M

更新日期：2005-07-01 00:00:00

abstract：:The indolocarbazole antibiotics staurosporine and rebeccamycin (1) are potent antitumor drugs targeting protein kinase C and topoisomerase I, respectively. To obtain staurosporine analogues from rebeccamycin, different structural modifications were performed: coupling of the sugar moiety to the second indole nitrogen,...

journal_title：Bioorganic & medicinal chemistry

authors： Anizon F,Moreau P,Sancelme M,Voldoire A,Prudhomme M,Ollier M,Sevère D,Riou JF,Bailly C,Fabbro D,Meyer T,Aubertin AM

更新日期：1998-09-01 00:00:00

abstract：:To improve the in vitro potency of the c-Src inhibitor 1a and to address its hERG liability, a structure-activity study was carried out, focusing on two regions of the lead compound. The blockade of the delayed cardiac current rectifier K(+) (I(Kr)) channel was overcome by replacing the ethylenediamino group with an a...

journal_title：Bioorganic & medicinal chemistry

authors： Mukaiyama H,Nishimura T,Kobayashi S,Komatsu Y,Kikuchi S,Ozawa T,Kamada N,Ohnota H

更新日期：2008-01-15 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：:A novel series of homo- and heterodimeric ligands containing κ/μ agonist and μ agonist/antagonist pharmacophores joined by a 10-carbon ester linker chain were synthesized and evaluated for their in vitro binding affinity at κ, μ, and δ opioid receptors, and their functional activities were determined at κ and μ recept...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang B,Zhang T,Sromek AW,Scrimale T,Bidlack JM,Neumeyer JL

更新日期：2011-05-01 00:00:00

abstract：:The discovery of new non-nucleoside antiviral compounds is of significant and growing interest for treating herpes virus infections due to the emergence of nucleoside-resistant strains. Using a whole cell virus-induced cytopathogenic assay, we tested a series of substituted triaryl heterocyclic compounds including acr...

journal_title：Bioorganic & medicinal chemistry

authors： Goodell JR,Madhok AA,Hiasa H,Ferguson DM

更新日期：2006-08-15 00:00:00

abstract：:Janus kinases (JAKs) are considered promising targets for the treatment of autoimmune diseases including rheumatoid arthritis (RA) due to their important role in multiple cytokine receptor signaling pathways. Recently, several JAK inhibitors have been developed for the treatment of RA. Here, we describe the identifica...

journal_title：Bioorganic & medicinal chemistry

authors： Hamaguchi H,Amano Y,Moritomo A,Shirakami S,Nakajima Y,Nakai K,Nomura N,Ito M,Higashi Y,Inoue T

更新日期：2018-10-01 00:00:00

abstract：:Research in recent years has demonstrated that the Trypanosoma cruzi cysteine protease cruzain (TCC) is a valid chemotherapeutic target, since inhibitors of this protease affect the pathology appropriately. By exploring the N-acylhydrazones (NAH) as privileged structures usually present in antiparasitic agents, we inv...

journal_title：Bioorganic & medicinal chemistry

authors： dos Santos Filho JM,Leite AC,de Oliveira BG,Moreira DR,Lima MS,Soares MB,Leite LF

更新日期：2009-09-15 00:00:00

abstract：:In this paper, we describe a short synthesis of N-(phosphonoacetyl)-L-aspartate (PALA) analogues. The mono- and difluorinated thioacetamide precursors were prepared in one step from methyl (diethoxyphosphono)di- and monofluoromethyldithioacetates 8 and 11 as starting materials. Antiproliferating properties on a L1210 ...

journal_title：Bioorganic & medicinal chemistry

authors： Pfund E,Lequeux T,Masson S,Vazeux M,Cordi A,Pierre A,Serre V,Hervé G

更新日期：2005-08-15 00:00:00

abstract：:Aminoglycoside antibiotics have recently emerged as an intriguing family of RNA binding molecules and they became leading structures for the design of novel RNA ligands. The demystification of the aminoglycoside-RNA recognition phenomenon is required for the development of superior binders. To explore the existence of...

journal_title：Bioorganic & medicinal chemistry

authors： Michael K,Wang H,Tor Y

更新日期：1999-07-01 00:00:00

abstract：:Pregnane X receptor (PXR) is a ligand-dependent transcription factor that is considered to be a potential therapeutic target for multiple diseases. Herein, we report the development and structure-activity relationship studies of a new series of hPXR agonists. Focusing on our recently developed silanol-sulfonamide scaf...

journal_title：Bioorganic & medicinal chemistry

authors： Toyama H,Shirakawa H,Komai M,Hashimoto Y,Fujii S

更新日期：2018-08-15 00:00:00

abstract：:The title l-glutathione derivatives, containing acid- and base-labile esters, respectively, were obtained in good overall yields. N-(t)Boc l-glutathione dimethyl ester was prepared via Fischer esterification of l-glutathione disulfide (GSSG) using HCl in dry methanol, protection of the amine with (t)Boc(2)O, and tribu...

journal_title：Bioorganic & medicinal chemistry

authors： Falck JR,Sangras B,Capdevila JH

更新日期：2007-01-15 00:00:00

abstract：:Polyamides consisting of N-methylpyrrole (Py), N-methylimidazole (Im), and N-methyl-3-hydroxypyrrole (Hp) are synthetic ligands that recognize predetermined DNA sequences with affinities and specificities comparable to many DNA-binding proteins. As derivatives of the natural products distamycin and netropsin, Py/Im/Hp...

journal_title：Bioorganic & medicinal chemistry

authors： Bremer RE,Szewczyk JW,Baird EE,Dervan PB

更新日期：2000-08-01 00:00:00

abstract：:Methylation of histone arginine residues is an epigenetic mark related to gene expression that is implicated in a variety of biological processes and can be reversed by small-molecule modulators of protein arginine methyltransferases (PRMTs). A series of symmetrical ureas, designed as analogues of the known PRMT1 inhi...

journal_title：Bioorganic & medicinal chemistry

authors： Fontán N,García-Domínguez P,Álvarez R,de Lera ÁR

更新日期：2013-04-01 00:00:00

abstract：:Twelve thiorhodamine derivatives have been examined for their ability to stimulate the ATPase activity of purified human P-glycoprotein (P-gp)-His(10), to promote uptake of calcein AM and vinblastine into multidrug-resistant, P-gp-overexpressing MDCKII-MDR1 cells, and for their rates of transport in monolayers of mult...

journal_title：Bioorganic & medicinal chemistry

authors： Orchard A,Schamerhorn GA,Calitree BD,Sawada GA,Loo TW,Claire Bartlett M,Clarke DM,Detty MR

更新日期：2012-07-15 00:00:00