Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for the opioid receptors.

abstract：:Two series of 2-substituted and three new diacetyl benzofurans were synthesized through palladium-catalyzed reactions and their in vitro antimicrobial spectra were assessed. The compounds demonstrated mild to significant growth inhibition against antibiotic-susceptible standard and clinically isolated strains of Gram-...

journal_title：Bioorganic & medicinal chemistry

authors： Wahab Khan M,Jahangir Alam M,Rashid MA,Chowdhury R

更新日期：2005-08-15 00:00:00

abstract：:A quencher-free molecular beacon capable of generating pyrene excimer fluorescence has been constructed using strategically positioned pyrene-UNA monomers. Hybridization of a fully complementary RNA target was accompanied by a pyrene excimer emission increase of more than 900%, and detection of RNA in living cells was...

journal_title：Bioorganic & medicinal chemistry

authors： Karlsen KK,Okholm A,Kjems J,Wengel J

更新日期：2013-10-15 00:00:00

abstract：:An unusual class of diterpenoid natural products, 'cycloterpenals' (with a central cyclohexadienal core), that arise in nature by condensation of retinoids and other isoprenes, have been isolated from a variety of organisms including marine sponges as well as from the human eye. A milk whey protein has also demonstrat...

journal_title：Bioorganic & medicinal chemistry

authors： Bench BJ,Tichy SE,Perez LM,Benson J,Watanabe CM

更新日期：2008-08-15 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：:Racemic ethyl 2-benzyl-3-(tert-butylsulfonyl)propionate (1) and racemic ethyl 2-benzyl-3-[[1-methyl-1-((morpholin-4-yl)carbonyl)ethyl]sulfonyl] propionate (3) were enantioselectively hydrolyzed by subtilisin Carlsberg generating the respective (S)-acids used as building blocks for renin inhibitors. The esters were rea...

journal_title：Bioorganic & medicinal chemistry

authors： Doswald S,Estermann H,Kupfer E,Stadler H,Walther W,Weisbrod T,Wirz B,Wostl W

更新日期：1994-06-01 00:00:00

abstract：:The acyclic chiral nucleic acid analogue, Glycol Nucleic Acid (GNA), displayed exceptional structural simplicity and atom economy while forming self-paired duplexes, using canonical Watson-Crick base pairing. We disclose here that the replacement of phosphodiester linker in GNA with somewhat rigid and shorter carbamat...

journal_title：Bioorganic & medicinal chemistry

authors： Bose T,Kumar VA

更新日期：2014-11-01 00:00:00

abstract：:The quinolinone skeleton has been utilized to develop various mechanism-based immune modulators. However, the effects of quinolinone derivatives on the release of T cell-associated interleukin-2 (IL-2) have not been established. In this study, a series of novel quinolinone derivatives was synthesized, and their immuno...

journal_title：Bioorganic & medicinal chemistry

authors： Kwak SH,Kang JA,Kim M,Lee SD,Park JH,Park SG,Ko H,Kim YC

更新日期：2016-11-01 00:00:00

abstract：:1-2 Annulated adamantane piperidines 4, 6, 16, 17, 19, 23 and 25 were synthesized and evaluated for anti-influenza A virus activity. The stereoelectronic requirements for optimal antiviral potency were investigated. Piperidine 23 proved to be the most active of the compounds tested against influenza A virus, being 3.5...

journal_title：Bioorganic & medicinal chemistry

authors： Zoidis G,Kolocouris N,Naesens L,De Clercq E

更新日期：2009-02-15 00:00:00

abstract：:Glucuronide derivatives of CBI-bearing CC-1065 analogues have been synthesized, and their cytotoxicities tested against U937 leukemia cells. The new compounds show potent antitumor activity in vitro. Compounds 1 and 2, and their corresponding glucuronides 3 and 4 have IC(50) values of 0.6, 0.1, 1.4 and 0.6 nM, respect...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Y,Yuan H,Wright SC,Wang H,Larrick JW

更新日期：2003-04-03 00:00:00

abstract：:Synthesis and molecular validation of 6-substituted-2-(3-phenoxyphenyl)-4-phenylquinoline derivatives (4a-h) as antibacterial/DNA gyrase inhibitors reported. Primarily, 6-substituted-2-(3-phenoxyphenyl)-4-phenylquinoline derivatives were docked into the active sites of DNA gyrase A&B, to ensure the binding mode of the...

journal_title：Bioorganic & medicinal chemistry

authors： Alagumuthu M,Arumugam S

更新日期：2017-02-15 00:00:00

abstract：:Esa1 (essential Sas2-related acetyltransferase 1) and Tip60 (HIV-1 TAT-interactive protein, 60 kDa) are key members of the MYST family of histone acetyltransferases (HATs) and play important functions in many cellular processes. In this work, we designed, synthesized and evaluated a series of substrate-based analogs f...

journal_title：Bioorganic & medicinal chemistry

authors： Wu J,Xie N,Wu Z,Zhang Y,Zheng YG

更新日期：2009-02-01 00:00:00

abstract：:6-N-(Benzothiazol-2-yl)deoxyadenosine (A(BT)) was synthesized and incorporated into DNAs. Although, the multipoint benzothiazole (BT) modification of oligodeoxynucleotides reduced the stability of duplexes with their complementary strands, it induced the strong exciton coupling between BT moieties. The circular dichro...

journal_title：Bioorganic & medicinal chemistry

authors： Masaki Y,Ohkubo A,Seio K,Sekine M

更新日期：2010-01-15 00:00:00

abstract：:Peptidomimetic compounds possessing a caprolactam ring constraint were prepared and evaluated as interleukin-1beta converting enzyme (ICE) inhibitors. The caprolactam ring was used to constrain the P3 region of our inhibitors. This strategy proved to be effective for the synthesis of ICE inhibitors, maintaining key hy...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Y,O'Neil SV,Wos JA,Oppong KA,Laufersweiler MC,Soper DL,Ellis CD,Baize MW,Fancher AN,Lu W,Suchanek MK,Wang RL,Schwecke WP,Cruze CA,Buchalova M,Belkin M,De B,Demuth TP Jr

更新日期：2007-02-01 00:00:00

abstract：:Valinol is part of numerous pharmaceuticals and has various other important applications. Optically pure valinol (ee >99%) was prepared employing different ω-transaminases from the corresponding prochiral hydroxy ketone. By the choice of the enzyme the (R)- as well as the (S)-enantiomer were accessible. Reductive amin...

journal_title：Bioorganic & medicinal chemistry

authors： Fuchs CS,Simon RC,Riethorst W,Zepeck F,Kroutil W

更新日期：2014-10-15 00:00:00

abstract：:The conjugate addition reaction between glutathione, N-Boc-cysteine methyl ester, N-acetyl cysteine methyl ester and N-acetyl cysteine and several substituted cyclopentenones is described. The reversibility of this process was demonstrated by thio-adduct metathesis on treatment of the adduct with a different cysteinyl...

journal_title：Bioorganic & medicinal chemistry

authors： Bickley JF,Ciucci A,Evans P,Roberts SM,Ross N,Santoro MG

更新日期：2004-06-15 00:00:00

abstract：:In the search for potent and selective human beta3-adrenergic receptor (AR) agonists as potential drugs for the treatment of obesity and noninsulin-dependent (type II) diabetes, we prepared a novel series of phenoxypropanolamine derivatives containing the thiourea moiety and evaluated their biological activities at hu...

journal_title：Bioorganic & medicinal chemistry

authors： Maruyama T,Seki N,Onda K,Suzuki T,Kawazoe S,Hayakawa M,Matsui T,Takasu T,Ohta M

更新日期：2009-08-01 00:00:00

abstract：:Diacylhydrazine derivatives have been identified as one of the most important insect growth regulators. A variety of diacylhydrazine derivatives were designed and synthesized in recent years due to their unique action mechanism, simple structure, and environmental benign character. This paper describes the molecular d...

journal_title：Bioorganic & medicinal chemistry

authors： Zhao PL,Li J,Yang GF

更新日期：2007-03-01 00:00:00

abstract：:P-glycoprotein (P-gp) is known to mediate multidrug resistance (MDR) by acting as an efflux pump to actively transport chemotherapeutic agents out of carcinoma cells. Inhibition of P-gp function may represent one of the strategies to reverse MDR. We have previously reported that marchantin C (MC), a macrocyclic bisbib...

journal_title：Bioorganic & medicinal chemistry

authors： Xi GM,Sun B,Jiang HH,Kong F,Yuan HQ,Lou HX

更新日期：2010-09-15 00:00:00

abstract：:The methanolic extract of the roots of Saussurea lappa CLARKE, a Chinese medicinal herb Saussureae Radix, was found to inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-activated mouse peritoneal macrophages. Among the constituents from the methanolic extract, two sesquiterpene lactones (costunolide and...

journal_title：Bioorganic & medicinal chemistry

authors： Matsuda H,Toguchida I,Ninomiya K,Kageura T,Morikawa T,Yoshikawa M

更新日期：2003-03-06 00:00:00

abstract：:We synthesized modified 2'-deoxyuridine triphosphates bearing amino acids at the C5 position and investigated their substrate properties for KOD Dash DNA polymerase during polymerase chain reaction (PCR). PCR using C5-modified dUTP having an amino acyl group (arginyl, histidyl, lysyl, phenylalanyl, tryptophanyl, leucy...

journal_title：Bioorganic & medicinal chemistry

authors： Kuwahara M,Hanawa K,Ohsawa K,Kitagata R,Ozaki H,Sawai H

更新日期：2006-04-15 00:00:00

abstract：:Biphenylic compounds related to the natural products magnolol and 4'-O-methylhonokiol were synthesized, evaluated and optimized as positive allosteric modulators (PAMs) of GABA(A) receptors. The most efficacious compounds were the magnolol analog 5-ethyl-5'-hexylbiphenyl-2,2'-diol (45) and the honokiol analogs 4'-meth...

journal_title：Bioorganic & medicinal chemistry

authors： Fuchs A,Baur R,Schoeder C,Sigel E,Müller CE

更新日期：2014-12-15 00:00:00

abstract：:The increasing resistance of the malarial parasite to antimalarial drugs is a major contributor to the reemergence of the disease and increases the need for new drug targets. The two aspartic proteases, plasmepsins I and II, from Plasmodium falciparum have recently emerged as potential targets. In an effort to inhibit...

journal_title：Bioorganic & medicinal chemistry

authors： Muthas D,Nöteberg D,Sabnis YA,Hamelink E,Vrang L,Samuelsson B,Karlén A,Hallberg A

更新日期：2005-09-15 00:00:00

abstract：:The enzyme 17alpha-hydroxylase/17,20-lyase (P-450(17alpha) has recently become the focus of research into the fight against hormone dependent prostate cancer. However, the specific nature of this enzyme, in particular, the dual role of its active site, remains unknown. In our drive to elucidate further information reg...

journal_title：Bioorganic & medicinal chemistry

authors： Ahmed S

更新日期：1999-08-01 00:00:00

abstract：:The preparation of a novel series of N-aryl CBI derivatives in which an aryl substituent could be used to predictably modulate the reactivity of the resulting CC-1065/duocarmycin alkylation subunit analogue is detailed and its extension to a unique series of N-alkenyl derivatives is reported. The N-aryl derivatives we...

journal_title：Bioorganic & medicinal chemistry

authors： Parrish JP,Trzupek JD,Hughes TV,Hwang I,Boger DL

更新日期：2004-11-15 00:00:00

abstract：:This study describes the synthesis and radiosynthesis of eight new [18F]fluoro-inositol-based radiotracers in myo- and scyllo-inositol configuration. These radiotracers are equipped with a propyl linker bearing fluorine-18. This fluorinated arm is either on a hydroxyl group, i.e. O-alkylated inositols, or on the cyclo...

journal_title：Bioorganic & medicinal chemistry

authors： Collet C,Schmitt S,Maskali F,Clément A,Chrétien F,Karcher G,Marie PY,Poussier S,Lamandé-Langle S

更新日期：2017-10-15 00:00:00

abstract：:Substituted diphenyl sulfones (10a-n) were synthesised, and the structures were confirmed by NMR, LC-MS and X-ray crystallography. Their antagonistic activities towards 5-HT₆ receptor were assessed in a cell-based functional assay. Diphenyl sulfone 10a, in spite of being the smallest and simplest known sulfonyl-contai...

journal_title：Bioorganic & medicinal chemistry

authors： Ivachtchenko A,Golovina E,Kadieva M,Mitkin O,Tkachenko S,Okun I

更新日期：2013-08-01 00:00:00

abstract：:Herein, we describe the design, synthesis, and structure-activity relationships of novel benzylpyrazole acylsulfonamides as non-thiazolidinedione (TZD), non-carboxylic-acid-based peroxisome proliferator-activated receptor (PPAR) γ agonists. Docking model analysis of in-house weak agonist 2 bound to the reported PPARγ ...

journal_title：Bioorganic & medicinal chemistry

authors： Rikimaru K,Wakabayashi T,Abe H,Imoto H,Maekawa T,Ujikawa O,Murase K,Matsuo T,Matsumoto M,Nomura C,Tsuge H,Arimura N,Kawakami K,Sakamoto J,Funami M,Mol CD,Snell GP,Bragstad KA,Sang BC,Dougan DR,Tanaka T,Katayama

更新日期：2012-01-15 00:00:00

abstract：:A new class of compounds able to block the replication of subgenomic HCV RNA in liver cells is described. 3-Amino-2(5H)furanones 4 may be regarded as diketoacid analogues and were obtained by basic rearrangement of the isoxazolidine nucleus. ...

journal_title：Bioorganic & medicinal chemistry

authors： Iannazzo D,Piperno A,Romeo G,Romeo R,Chiacchio U,Rescifina A,Balestrieri E,Macchi B,Mastino A,Cortese R

更新日期：2008-11-01 00:00:00

abstract：:The first inhibition study of the transmembrane carbonic anhydrase (CA, EC 4.2.1.1) isozymes hCA XIV with a library of aromatic and heteroaromatic sulfonamides synthesized earlier is reported. Most of the inhibitors were sulfanilamide, homosulfanilamide and 4-aminoethyl-benzenesulfonamide derivatives, to which tails t...

journal_title：Bioorganic & medicinal chemistry

authors： Ozensoy O,Nishimori I,Vullo D,Puccetti L,Scozzafava A,Supuran CT

更新日期：2005-11-15 00:00:00

abstract：:Oleoyl Formononetin (OF) has good weight loss activity and hypolipidemic activity, could improve insulin sensitivity and suppress adipogenesis. To acquire better biological activities, three series of flavonoid fatty acid esters were designed and synthesized by optimizing the structure of OF. Their bioactivities were ...

journal_title：Bioorganic & medicinal chemistry

authors： Zhao W,Sun J,Xiang H,Zeng YY,Li XB,Xiao H,Chen DY,Ma RL

更新日期：2011-05-15 00:00:00