Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.

abstract：:Aminoglycoside antibiotics act by binding to 16S rRNA. Resistance to these antibiotics occurs via drug modifications by enzymes such as aminoglycoside 6'-N-acetyltransferases (AAC(6')s). We report here the regioselective and efficient synthesis of N-6'-acylated aminoglycosides and their use as probes to study AAC(6')-...

journal_title：Bioorganic & medicinal chemistry

authors： Yan X,Gao F,Yotphan S,Bakirtzian P,Auclair K

更新日期：2007-04-15 00:00:00

abstract：:Cyanocobalamin (vitamin B12) is an essential nutrient as well as a very useful carrier in drug delivery. Conjugates of vitamin B12 are investigated due to their wide range of therapeutic applications. We report the synthesis of six vitamin B12 conjugates, and the effect of conjugation on their solubilities and stabili...

journal_title：Bioorganic & medicinal chemistry

authors： Wang X,Wei L,Kotra LP

更新日期：2007-02-15 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

abstract：:Following our studies on structure-activity relationships of anti-rhinovirus chromene and chroman derivatives, we designed and synthesized new series of 3-phenylalkyl-2H-chromenes and -chromans bearing differently sized, aliphatic linker chains between the two cycles. The cytotoxicity and the antiviral activity of the...

journal_title：Bioorganic & medicinal chemistry

authors： Conti C,Proietti Monaco L,Desideri N

更新日期：2017-04-01 00:00:00

abstract：:A group of racemic 4-aryl(heteroaryl)-1,4-dihydro-2,6-dimethyl-3-nitropyridines possessing nitric oxide donor O(2)-acetoxymethyl-1-(N-ethyl-N-methylamino, or 4-ethylpiperazin-1-yl)diazen-1-ium-1,2-diolate, C-5 ester substituents were synthesized by coupling the respective 4-aryl(heteroaryl)-1,4-dihydro-2,6-dimethyl-3-...

journal_title：Bioorganic & medicinal chemistry

authors： Velázquez C,Knaus EE

更新日期：2004-07-15 00:00:00

abstract：:A series of 27 salicylanilide diethyl phosphates was prepared as a part of our on-going search for new antimicrobial active drugs. All compounds exhibited in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium strains, with minimum inhibitory concentration (MIC) values of ...

journal_title：Bioorganic & medicinal chemistry

authors： Vinšová J,Kozic J,Krátký M,Stolaříková J,Mandíková J,Trejtnar F,Buchta V

更新日期：2014-01-15 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：:Cancer cells reprogram their metabolism due to genetic alteration to compensate for increased energy demand and enhanced anabolism, cell proliferation, and protection from oxidative damage. Here, we assessed the cytotoxicity of three dimeric naphthoquinones against the glycolytic MCF-7 versus the oxidative MDA-453 bre...

journal_title：Bioorganic & medicinal chemistry

authors： Emadi A,Le A,Harwood CJ,Stagliano KW,Kamangar F,Ross AE,Cooper CR,Dang CV,Karp JE,Vuica-Ross M

更新日期：2011-12-01 00:00:00

abstract：:The peptides DRPVPY and MDWNMHAA, which were identified as mimics of the cell-surface polysaccharides of Streptococcus Group A and Shigella flexneri Y, respectively, were used in this study to develop experimental vaccines directed against these two bacteria. Both oligopeptides were synthesized employing the Fmoc soli...

journal_title：Bioorganic & medicinal chemistry

authors： Hossany RB,Johnson MA,Eniade AA,Pinto BM

更新日期：2004-07-01 00:00:00

abstract：:Chronic hepatitis C virus (HCV) infections are a significant medical problem worldwide. The NS5B Polymerase of HCV plays a central role in virus replication and is a prime target for the discovery of new treatment options. We recently disclosed 1H-benzo[de]isoquinoline-1,3(2H)-diones as allosteric inhibitors of NS5B P...

journal_title：Bioorganic & medicinal chemistry

authors： Malancona S,Donghi M,Ferrara M,Martin Hernando JI,Pompei M,Pesci S,Ontoria JM,Koch U,Rowley M,Summa V

更新日期：2010-04-15 00:00:00

abstract：:The synthesis of novel melatonin analogues 3a and 4a-c designed as melatonin receptor ligands is described. Among the newly synthesized ligands, 2-((S)-2-hydroxymethylindolin-1-ylmethyl)-melatonin 4b displayed the highest affinity for MT(1) receptors (K(i)=9.8 nM) and for MT(2) subtype (K(i)=7.8 nM), whereas the rigid...

journal_title：Bioorganic & medicinal chemistry

authors： Attia MI,Witt-Enderby PA,Julius J

更新日期：2008-08-15 00:00:00

abstract：:A series of nitrogen-based 20S-hydroxyl camptothecin ester derivatives were prepared. 3-Aminopropionate of camptothecin was found more cytotoxic in vitro on several human tumor cell lines than 3-amidopropionate of camptothecin. Ester 16 showed best antitumor activity in vivo and in vitro in all esters we prepared. ...

journal_title：Bioorganic & medicinal chemistry

authors： Wang CY,Pan XD,Liu HY,Fu ZD,Wei XY,Yang LX

更新日期：2004-07-01 00:00:00

abstract：:We report the synthesis and the functional studies of multiple crown alpha-helical peptides designed to form artificial ion channels. The approach combines the versatility of solid phase peptide synthesis, the conformational predictability of peptidic molecules, and the solution synthesis of crown ethers with engineer...

journal_title：Bioorganic & medicinal chemistry

authors： Biron E,Otis F,Meillon JC,Robitaille M,Lamothe J,Van Hove P,Cormier ME,Voyer N

更新日期：2004-03-15 00:00:00

abstract：:A series of novel pyrimidinylthioacetanilides were designed, synthesized, and evaluated for their biological activity as potent HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Most of the tested compounds were proved to be effective in inhibiting HIV-1 (IIIB) replication with EC50 ranging from 0.15 μM ...

journal_title：Bioorganic & medicinal chemistry

authors： Li X,Lu X,Chen W,Liu H,Zhan P,Pannecouque C,Balzarini J,De Clercq E,Liu X

更新日期：2014-10-01 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：:The first committed step in lipid A biosynthesis is catalyzed by uridine diphosphate-(3-O-(R-3-hydroxymyristoyl))-N-acetylglucosamine deacetylase (LpxC), a zinc-dependent deacetylase, and inhibitors of LpxC may be useful in the development of antibacterial agents targeting a broad spectrum of Gram-negative bacteria. H...

journal_title：Bioorganic & medicinal chemistry

authors： Shin H,Gennadios HA,Whittington DA,Christianson DW

更新日期：2007-04-01 00:00:00

abstract：:A tetracyclic, conformationally constrained analogue of delta8-THC (2) has been synthesized in which a two carbon bridge exists between C2 and C2'. Two conceptually related syntheses of 2 are described, both of which employ 5,7-dimethoxy-4-oxo-1,2,3,4-tetrahydronaphthoic acid (11) as starting material. This substrate ...

journal_title：Bioorganic & medicinal chemistry

authors： Huffman JW,Yu S

更新日期：1998-12-01 00:00:00

abstract：:An efficient synthesis of a library of 5-amino-thiazolo[4,5-d]pyrimidines is reported. Regioselective displacements of chlorines, as well as regioselective diazotation reactions are described, which allow the introduction of structural diversity on the scaffold by consecutive reactions. Screening of this focused libra...

journal_title：Bioorganic & medicinal chemistry

authors： Jang MY,De Jonghe S,Segers K,Anné J,Herdewijn P

更新日期：2011-01-01 00:00:00

abstract：:Thymidylate synthase (TS) (EC 2.1.1.45), an enzyme involved in the DNA synthesis of both prokaryotic and eukaryotic cells, is a potential target for the development of anticancer and antinfective agents. Recently, we described a series of phthalein and naphthalein derivatives as TS inhibitors. These compounds have str...

journal_title：Bioorganic & medicinal chemistry

authors： Ghelli S,Rinaldi M,Barlocco D,Gelain A,Pecorari P,Tondi D,Rastelli G,Costi MP

更新日期：2003-03-20 00:00:00

abstract：:Family C G-protein coupled receptors (GPCRs) consist of the metabotropic glutamate receptors (mGluRs), the calcium-sensing receptor (CaSR), the T1R taste receptors, the GABA(B) receptor, the V2R pheromone receptors, and several chemosensory receptors. A common feature of Family C receptors is the presence of an amino ...

journal_title：Bioorganic & medicinal chemistry

authors： Wang M,Hampson DR

更新日期：2006-03-15 00:00:00

abstract：:Cytochrome P450 2C9 (2C9) is one of the three major drug metabolizing cytochrome P450 enzymes in human liver. Although the crystal structure of 2C9 has been solved, the important physicochemical properties of substrate-enzyme interactions remain difficult to be determined. This is due in part to the conformational fle...

journal_title：Bioorganic & medicinal chemistry

authors： Peng CC,Rushmore T,Crouch GJ,Jones JP

更新日期：2008-04-01 00:00:00

abstract：:We isolated the 4 kinds of flavonoids from strawberry 'Nohime' and examined the effect of these flavonoids on the degranulation in RBL-2H3 cells. The flavonoids were found to suppress the degranulation from Ag-stimulated RBL-2H3 cells to different extents. To disclose the inhibitory mechanism of degranulation by flavo...

journal_title：Bioorganic & medicinal chemistry

authors： Itoh T,Ninomiya M,Yasuda M,Koshikawa K,Deyashiki Y,Nozawa Y,Akao Y,Koketsu M

更新日期：2009-08-01 00:00:00

abstract：:The activity of p90 ribosomal S6 kinase 2 (RSK2) has emerged as an attractive target for cancer therapy due to its role in the regulation of diverse cellular processes, such as cell transformation and proliferation. Several pan-RSK inhibitors have been identified with BI-D1870 and the pseudo-analogs LJH685 and LJI308 ...

journal_title：Bioorganic & medicinal chemistry

authors： Casalvieri KA,Matheson CJ,Backos DS,Reigan P

更新日期：2020-03-01 00:00:00

abstract：:The irreversible inhibition of histidine ammonia lyase by L-cysteine and dioxygen has been reexamined. After denaturation and consecutive digestion of the inhibited enzyme by trypsin and endoproteinase Glu-C, the generated chromophoric system (lambda max = 340 nm) remained intact and was isolated in an octapeptide con...

journal_title：Bioorganic & medicinal chemistry

authors： Weber K,Rétey J

更新日期：1996-07-01 00:00:00

abstract：:In this work, we further investigated a previously introduced class of cholinesterase inhibitors. The removal of the carbamic function from the lead compound xanthostigmine led to a reversible cholinesterase inhibitors 3. Some new 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-one analogs were designed, synthesized, and...

journal_title：Bioorganic & medicinal chemistry

authors： Piazzi L,Belluti F,Bisi A,Gobbi S,Rizzo S,Bartolini M,Andrisano V,Recanatini M,Rampa A

更新日期：2007-01-01 00:00:00

abstract：:The synthesis of docetaxel esters of malic acid is described. These compounds were found to have greatly improved water solubility and are stable in solution at neutral pH. The C2' modified compounds 2a-c and 3a-c behave as prodrugs, that is, docetaxel is generated upon exposure to human plasma, whereas the C7 and C2'...

journal_title：Bioorganic & medicinal chemistry

authors： Du W,Hong L,Yao T,Yang X,He Q,Yang B,Hu Y

更新日期：2007-09-15 00:00:00

abstract：:A series of new 4-amino-3-[3-[4-(2-methoxy or nitro phenyl)-1-piperazinyl] propyl]thio]-5-(substitutedphenyl)[1,2,4]triazoles 11a-t was synthesized in order to obtain compounds with high affinity and selectivity for 5-HT(1A) receptor over the alpha(1)-adrenoceptor. A series of isomeric 4-amino-2-[3-[4-(2-methoxy or ni...

journal_title：Bioorganic & medicinal chemistry

authors： Sarvà MC,Romeo G,Guerrera F,Siracusa M,Salerno L,Russo F,Cagnotto A,Goegan M,Mennini T

更新日期：2002-02-01 00:00:00

abstract：:A series of 16 1-phenyl-1H-1,2,3-triazoles with substituents at both the 4- and 5-positions of the triazole ring were synthesized, and a total of 49 compounds, including previously reported 4- or 5-monosubstituted analogues, were examined for their ability to inhibit the specific binding of [(3)H]4'-ethynyl-4-n-propyl...

journal_title：Bioorganic & medicinal chemistry

authors： Alam MS,Huang J,Ozoe F,Matsumura F,Ozoe Y

更新日期：2007-08-01 00:00:00

abstract：:N-Methylpyrrole (Py)-N-methylimidazole (Im) polyamides are small organic molecules that can recognize predetermined DNA sequences with high sequence specificity. As many eukaryotic promoter regions contain highly GC-rich sequences, it is valuable to synthesize and characterize Py-Im polyamides that recognize GC-rich m...

journal_title：Bioorganic & medicinal chemistry

authors： Han YW,Kashiwazaki G,Morinaga H,Matsumoto T,Hashiya K,Bando T,Harada Y,Sugiyama H

更新日期：2013-09-01 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