2-N-Methyl modifications and SAR studies of manzamine A.

abstract：:Streptococcus pneumoniae is among the major human pathogens. Several interactions of this bacterium with its host appear to have been mediated by bacterial cell wall components. Specifically, phosphorylcholine residues covalently attached to teichoic and lipoteichoic acids serve as anchors for many surface-located pro...

journal_title：Bioorganic & medicinal chemistry

authors： Campillo NE,Páez JA,Lagartera L,Gonzalez A

更新日期：2005-12-01 00:00:00

abstract：:A group of (E)-3-(4-methanesulfonylphenyl)acrylic acids possessing a substituted-phenyl ring (4-H, 4-Br, 3-Br, 4-F, 4-OH, 4-OMe, 4-OAc, and 4-NHAc) attached to the acrylic acid C-2 position were prepared using a stereospecific Perkin condensation reaction. A related group of compounds having 4- and 3-(4-isopropyloxyph...

journal_title：Bioorganic & medicinal chemistry

authors： Moreau A,Chen QH,Praveen Rao PN,Knaus EE

更新日期：2006-12-01 00:00:00

abstract：:A series of novel pyrazolo[1,5-a]pyrazin-4(5H)-one derivatives were synthesized by the reaction of ethyl 3-aryl-1-(2-bromoethyl)-1H-pyrazole-5-carboxylate and amine in the general heating condition and microwave-assisted condition. The structures of the compounds were determined by IR, (1)H NMR and mass spectroscopy, ...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang JH,Fan CD,Zhao BX,Shin DS,Dong WL,Xie YS,Miao JY

更新日期：2008-12-15 00:00:00

abstract：:The ability as P-glycoprotein (P-gp, ABCB1) modulators of thirty (1-30) triterpenoids of the cucurbitane-type was evaluated on human L5178 mouse T-lymphoma cell line transfected with the human MDR1 gene, through the rhodamine-123 exclusion assay. Compounds (1-26, and 29, 30) were previously obtained from the African m...

journal_title：Bioorganic & medicinal chemistry

authors： Ramalhete C,Mulhovo S,Molnar J,Ferreira MU

更新日期：2016-11-01 00:00:00

abstract：:The nitronate and nitrovinyl methods to synthesize indole glucosinolates (GLs) have been investigated. The results were applied to generally the most prevalent natural indole glucosinolates to synthesize 4-methoxyglucobrassicin (MGB) and neo-glucobrassicin (NGB) in moderate overall yield for the first time. The anti-i...

journal_title：Bioorganic & medicinal chemistry

authors： Vo QV,Trenerry C,Rochfort S,Wadeson J,Leyton C,Hughes AB

更新日期：2014-01-15 00:00:00

abstract：:1,2,3-Triazole-, arylamino- and thio-substituted naphthoquinones (24, 8, and 2 representatives, respectively) were synthesized in moderate yields and evaluated against several human cancer cell lines (blood, ovarian, breast, central nervous system, colon, and prostate cancers and melanoma), showing, for some of them, ...

journal_title：Bioorganic & medicinal chemistry

authors： da Cruz EH,Hussene CM,Dias GG,Diogo EB,de Melo IM,Rodrigues BL,da Silva MG,Valença WO,Camara CA,de Oliveira RN,de Paiva YG,Goulart MO,Cavalcanti BC,Pessoa C,da Silva Júnior EN

更新日期：2014-03-01 00:00:00

abstract：:Alzheimer's disease (AD) is characterized by the buildup of insoluble aggregated amyloid-β protein (Aβ) into plaques that accumulate between the neural cells in the brain. AD is the sixth leading cause of death in the United States and is the only cause of death among the top ten that cannot currently be treated or cu...

journal_title：Bioorganic & medicinal chemistry

authors： Turner JP,Chastain SE,Park D,Moss MA,Servoss SL

更新日期：2017-01-01 00:00:00

abstract：:A novel series of aryloxyalkyl derivatives of imidazole and 1,2,4-triazole, 17-31, was designed and synthesized as inhibitors of heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2). Some of these compounds were found to be good inhibitors of HO-1, in particular those carrying an imidazole moiety as azolyl group and a ...

journal_title：Bioorganic & medicinal chemistry

authors： Salerno L,Pittalà V,Romeo G,Modica MN,Siracusa MA,Di Giacomo C,Acquaviva R,Barbagallo I,Tibullo D,Sorrenti V

更新日期：2013-09-01 00:00:00

abstract：:An efficient technique is presented which integrates cofactor dependent enzymic phosphorylation and dehydrogenation into a single, closed-loop system by employing phosphoenolpyruvate as the sacrificial reagent for sequential ATP and NAD+ recycling steps. Exemplary applications are developed for the synthesis of 6-phos...

journal_title：Bioorganic & medicinal chemistry

authors： Fessner WD,Sinerius G

更新日期：1994-07-01 00:00:00

abstract：:Glycosylated beta-amino acids (3-18, 38, 39), obtained by hydrolysis of glycosylated beta-amino esters on reaction with hydroxylamine hydrochloride in presence of DIC/DCC afforded glycosyl beta-amino hydroxamates (19-34, 40, 41) in fair to good yields. Compounds (19-34, 40, 41) were screened against human malarial par...

journal_title：Bioorganic & medicinal chemistry

authors： Mishra RC,Tripathi R,Katiyar D,Tewari N,Singh D,Tripathi RP

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：:Serine/threonine protein kinases Aurora A, B, and C play essential roles in cell mitosis and cytokinesis, and a number of Aurora kinase inhibitors have been evaluated in the clinic. Herein we report the synthesis and their antiproliferation of 3,5-disubstituted-2-aminopyrazines as kinases inhibitors. Amongst, 4-((3-am...

journal_title：Bioorganic & medicinal chemistry

authors： Bo YX,Xiang R,Xu Y,Hao SY,Wang XR,Chen SW

更新日期：2020-03-01 00:00:00

abstract：:A series of 3-amino-benzo[d]isoxazole-/3-aminoindazole-based compounds were designed, synthesized and pharmacologically evaluated as tyrosine kinase c-Met inhibitors. The SAR study was conducted leading to identification of nine compounds (8d, 8e, 12, 28a-d, 28h and 28i) with IC50s less than 10nM against c-Met. Compou...

journal_title：Bioorganic & medicinal chemistry

authors： Jiang X,Liu H,Song Z,Peng X,Ji Y,Yao Q,Geng M,Ai J,Zhang A

更新日期：2015-02-01 00:00:00

abstract：:Equol is a metabolite produced in vivo from the soy phytoestrogen daidzein by the action of gut microflora. It is known to be estrogenic, so human exposure to equol could have significant biological effects. Equol is a chiral molecule that can exist as the enantiomers R-equol and S-equol. To study the biological activ...

journal_title：Bioorganic & medicinal chemistry

authors： Muthyala RS,Ju YH,Sheng S,Williams LD,Doerge DR,Katzenellenbogen BS,Helferich WG,Katzenellenbogen JA

更新日期：2004-03-15 00:00:00

abstract：:Sphingolipids are ubiquitous and abundant components of all eukaryotic and some prokaryotic organisms. Sphingolipids show a large structural variety not only between the different species, but also within an individual cell. This variety is not limited to alterations in the polar headgroups of e.g. glycosphingolipids,...

journal_title：Bioorganic & medicinal chemistry

authors： Saied EM,Le TL,Hornemann T,Arenz C

更新日期：2018-08-07 00:00:00

abstract：:The PU-H58-dimers 13a-15b were efficiently synthesized and their biological properties were evaluated. The copper-catalyzed alkyne azide coupling was effective in simultaneously linking three components via a triazole formation to afford the target dimers. These synthesized dimers exhibited binding affinity to the N-t...

journal_title：Bioorganic & medicinal chemistry

authors： Sekiguchi H,Muranaka K,Osada A,Ichikawa S,Matsuda A

更新日期：2010-08-01 00:00:00

abstract：:3,5-Dihydroxyphenyl decanoate (DPD) is found to inhibit the diphenolase activity of tyrosinase from mushroom (Agaricus bisporus). The effects of DPD on the diphenolase activity of mushroom tyrosinase have been studied. The results show that the enzyme activity decreases very slowly with an increase in DPD concentratio...

journal_title：Bioorganic & medicinal chemistry

authors： Qiu L,Chen QX,Wang Q,Huang H,Song KK

更新日期：2005-11-15 00:00:00

abstract：:Novel benzimidazole derivatives were synthesized and their pharmacological activities were examined. These compounds showed a good suppressive action on histamine release from rat peritoneal mast cells produced by antigen-antibody reaction, an antagonistic action on guinea pig ileum contraction caused by histamine, an...

journal_title：Bioorganic & medicinal chemistry

authors： Nakano H,Inoue T,Kawasaki N,Miyataka H,Matsumoto H,Taguchi T,Inagaki N,Nagai H,Satoh T

更新日期：2000-02-01 00:00:00

abstract：:G protein coupled receptors (GPCRs) are important drug targets in pharmaceutical research. Traditionally, most research efforts have been devoted towards the design of small molecule agonists and antagonists. An interesting, yet poorly investigated class of GPCR modulators comprise the bivalent ligands, in which two r...

journal_title：Bioorganic & medicinal chemistry

authors： Bonger KM,van den Berg RJ,Heitman LH,IJzerman AP,Oosterom J,Timmers CM,Overkleeft HS,van der Marel GA

更新日期：2007-07-15 00:00:00

abstract：:Pyrazolopyrimidines are the fused heterocyclic ring systems which structurally resemble purines which prompted biological investigations to assess their potential therapeutic significance. They are known to play a crucial role in numerous disease conditions. The advent of their first bioactivity as adenosine antagonis...

journal_title：Bioorganic & medicinal chemistry

authors： Chauhan M,Kumar R

更新日期：2013-09-15 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：:Forty-five novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds contain novel cinnamic acid moieties at C-7 that were synthesized using a key Heck reaction followed by nucleophilic aromatic substitution reactions. The most active compound...

journal_title：Bioorganic & medicinal chemistry

authors： Springer DM,Luh BY,Goodrich J,Bronson JJ

更新日期：2003-01-17 00:00:00

abstract：:The calpains are a conserved family of cysteine proteases that includes several isoforms of which µ-calpain and m-calpain are the most widely distributed in mammalian cells. Calpains have been implicated in normal physiological processes as well as cellular abnormalities such as neurodegenerative disorders, cataract, ...

journal_title：Bioorganic & medicinal chemistry

authors： Donkor IO,Xu J,Liu J,Cameron K

更新日期：2020-05-01 00:00:00

abstract：:Previous studies have shown that several imidazole derivatives possess affinity to histamine H(3) and H(4) receptors. Continuing our study on structural requirements responsible for affinity and selectivity for H(3)/H(4) receptor subtypes, two series of 3-(1H-imidazol-4-yl)propyl carbamates were prepared: a series of ...

journal_title：Bioorganic & medicinal chemistry

authors： Więcek M,Kottke T,Ligneau X,Schunack W,Seifert R,Stark H,Handzlik J,Kieć-Kononowicz K

更新日期：2011-05-01 00:00:00

abstract：:Sigma-1 receptor imaging probes for determining the expression levels are desirable for diagnoses of various diseases and companion diagnoses of therapeutic agents targeting the sigma-1 receptor. In this study, we aimed to develop probes with higher affinity for the sigma-1 receptor. For this purpose, we synthesized a...

journal_title：Bioorganic & medicinal chemistry

authors： Ogawa K,Masuda R,Mishiro K,Wang M,Kozaka T,Shiba K,Kinuya S,Odani A

更新日期：2019-05-15 00:00:00

abstract：:The previously reported morphinan derivative SN-28 showed high selectivity and agonist activity for the δ opioid receptor. In the course of examining the structure-activity relationship of SN-28 derivatives, the derivatives with the 4-hydroxy group (SN-24, 26, 27) showed higher selectivities for the δ receptor over th...

journal_title：Bioorganic & medicinal chemistry

authors： Ida Y,Nemoto T,Hirayama S,Fujii H,Osa Y,Imai M,Nakamura T,Kanemasa T,Kato A,Nagase H

更新日期：2012-01-15 00:00:00

abstract：:A series of trans-2-aryl-cyclopropylamine derived compounds were synthesized and evaluated their biological activities against DPP-IV. The structure-activity relationships (SAR) led to the discovery of novel series of DPP-IV inhibitors, having IC(50) values of <100 nM with excellent selectivity over the closely relate...

journal_title：Bioorganic & medicinal chemistry

authors： Tsai TY,Hsu T,Chen CT,Cheng JH,Yeh TK,Chen X,Huang CY,Chang CN,Yeh KC,Hsieh SH,Chien CH,Chang YW,Huang CH,Huang YW,Huang CL,Wu SH,Wang MH,Lu CT,Chao YS,Jiaang WT

更新日期：2009-03-15 00:00:00

abstract：:The piperazine ring of the potent nootropic drug DM235 has been decorated with H-bond donor and acceptor groups (CH2OH, CH2OMe, CH2OCOMe, COOEt); the aim was to insert new functional groups, suitable for further chemical manipulation. The influence of these modifications on nootropic activity was assessed by means of ...

journal_title：Bioorganic & medicinal chemistry

authors： Martino MV,Guandalini L,Di Cesare Mannelli L,Menicatti M,Bartolucci G,Dei S,Manetti D,Teodori E,Ghelardini C,Romanelli MN

更新日期：2017-03-15 00:00:00

abstract：:The 3C-like main proteinase of the severe acute respiratory syndrome (SARS) coronavirus, SARS-CoV M(pro), is widely considered to be a major drug target for the development of anti-SARS treatment. Based on the chemical structure of a lead compound from a previous screening, we have designed and synthesized a number of...

journal_title：Bioorganic & medicinal chemistry

authors： Niu C,Yin J,Zhang J,Vederas JC,James MN

更新日期：2008-01-01 00:00:00

abstract：:The free fatty acid receptor 1 (FFA1) is a novel antidiabetic target for the treatment of type 2 diabetes based on particular mechanism in amplifying glucose-stimulated insulin secretion. We have previously identified a series of phenoxyacetic acid derivatives. Herein, we describe the further chemical modification of ...

journal_title：Bioorganic & medicinal chemistry

authors： Li Z,Wang X,Xu X,Yang J,Xia W,Zhou X,Huang W,Qian H

更新日期：2015-11-15 00:00:00