DNA aptamers that bind to chitin.

abstract：:We have designed and synthesized econazole-derived nitroimidazoles to investigate the antitubercular activity of the nitroimidazole compounds. The introduction of a nitro group at the 4-position of the imidazole on econazole abolished the antitubercular activity. However, alcoholic nitroimidazoles 4 and 6 compounds we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee SH,Kim S,Yun MH,Lee YS,Cho SN,Oh T,Kim P

更新日期：2011-03-01 00:00:00

abstract：:A series of caffeic acid amides were designed, synthesized, and their synergistic activity with fluconazole against fluconazole-resistant Candida albicans was evaluated in vitro. The title caffeic acid amides 3-30 except 26 exhibited potent activity, and the subsequent SAR study was conducted. Compound 3, 5, 21, and 3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dai L,Zang C,Tian S,Liu W,Tan S,Cai Z,Ni T,An M,Li R,Gao Y,Zhang D,Jiang Y

更新日期：2015-01-01 00:00:00

abstract：:We report herein the synthesis of a newly described anti-cancer agent, NRPa-308. This compound antagonizes Neuropilin-1, a multi-partners transmembrane receptor overexpressed in numerous tumors, and thereby validated as promising target in oncology. The preparation of NRPa-308 proved challenging because of the orthogo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Brachet E,Dumond A,Liu WQ,Fabre M,Selkti M,Raynaud F,Hermine O,Benhida R,Belmont P,Garbay C,Lepelletier Y,Ronco C,Pagès G,Demange L

更新日期：2019-12-15 00:00:00

abstract：:The SPOT technology can fulfill most requirements for highly parallel, multiple peptide synthesis of soluble peptides within the upper microgram range. Here, we report on an improved method using hydroxymethylphenoxyacetic acid (HMPA) for 19 amino acids and 4-(4-hydroxymethyl-3-methoxyphenoxy)-butyric acid (HMPB) for ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ay B,Landgraf K,Streitz M,Fuhrmann S,Volkmer R,Boisguerin P

更新日期：2008-07-15 00:00:00

abstract：:The structure-activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagonists (e.g., 2-5) is described. The effect of the lactone carbonyl group on binding to PAR-1 is dependent on the substitution pattern of the pyridine ring. A stereoselective intramolecular Michael additio...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xia Y,Chackalamannil S,Chan TM,Czarniecki M,Doller D,Eagen K,Greenlee WJ,Tsai H,Wang Y,Ahn HS,Boykow GC,McPhail AT

更新日期：2006-09-15 00:00:00

abstract：:Opuntia ficus-indica L. is known for its beneficial effects on human health, but still little is known on cladodes as a potent source of antioxidants. Here, a direct, economic and safe method was set up to obtain water extracts from Opuntia ficus-indica cladodes rich in antioxidant compounds. When human keratinocytes ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Petruk G,Di Lorenzo F,Imbimbo P,Silipo A,Bonina A,Rizza L,Piccoli R,Monti DM,Lanzetta R

更新日期：2017-12-15 00:00:00

abstract：:A series of 5-(piperidinylethyloxy)quinoline 5-HT(1) receptor ligands have been studied by elaboration of the series of dual 5-HT(1)-SSRIs reported previously. These new compounds display a different in vitro pharmacological profile with potent affinity across the 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptors and selectiv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ward SE,Eddershaw P,Flynn ST,Gordon L,Lovell PJ,Moore SH,Scott CM,Smith PW,Thewlis KM,Wyman PA

更新日期：2009-01-15 00:00:00

abstract：:Nobiletin, a major component of polymethoxyflavones in citrus fruits, has a broad spectrum of health beneficial properties including anti-inflammatory and anti-carcinogenic activities. The metabolite identification of nobiletin in mouse urine has concluded that it undergoes mono-demethylation (3'- and 4'-demethylnobil...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li S,Sang S,Pan MH,Lai CS,Lo CY,Yang CS,Ho CT

更新日期：2007-09-15 00:00:00

abstract：:Five new p-terphenyls named prenylterphenyllin D (1), prenylterphenyllin E (2), 2'-O-methylprenylterphenyllin (3), 4-O-methylprenylterphenyllin (4) and 3'-O-methylterphenyllin (5) together with seven known compounds (6-12), were isolated from cultures of Aspergillus sp. YXf3. The structures of the new compounds were e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yan W,Wuringege,Li SJ,Guo ZK,Zhang WJ,Wei W,Tan RX,Jiao RH

更新日期：2017-01-01 00:00:00

abstract：:The synthesis and biological evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1H)-one scaffold is described. Two series of compounds, bearing either an amino or carbon substituent in the 2-position of the pyrimidine ring were investigated. Modification of substituents and chain ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ringom R,Axen E,Uppenberg J,Lundbäck T,Rondahl L,Barf T

更新日期：2004-09-06 00:00:00

abstract：:Multiple-targeted ligands can have certain advantages for the management of hypertension which has multiple controls. Molecules with dual bioactivities are available in literature for treating metabolic disorders like diabetes, hypertension and hypercholesterolemia. After scrutinizing the SAR of prazosin-type α1-block...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yadav MR,Naik PP,Gandhi HP,Chauhan BS,Giridhar R

更新日期：2013-07-01 00:00:00

abstract：:Sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Starting from a screening hit 8 that had modest affinity for the cannabinoid CB(2) receptor, a parallel synthesis approach and initial SAR are described, leading to compound 27 with 120-fold functional selectivity for the CB(2) rec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Worm K,Zhou QJ,Saeui CT,Green RC,Cassel JA,Stabley GJ,DeHaven RN,Conway-James N,LaBuda CJ,Koblish M,Little PJ,Dolle RE

更新日期：2008-05-01 00:00:00

abstract：:A series of potent arenavirus inhibitors sharing a benzimidazole core were previously reported by our group. SAR studies were expanded beyond the previous analysis, which involved the attached phenyl rings and methylamino linker portion, to include modifications focused on the benzimidazole core. These changes include...

journal_title：Bioorganic & medicinal chemistry letters

authors： Burgeson JR,Moore AL,Gharaibeh DN,Larson RA,Cerruti NR,Amberg SM,Hruby DE,Dai D

更新日期：2013-02-01 00:00:00

abstract：:1-((Substituted)methyl)quinoxaline-2,3(1H,4H)-dione (2a-e) and 1-((substituted)acryloyl)quinoxaline-2,3(1H,4H)-dione (4a-c) were synthesized from quinoxaline-2,3(1H,4H)-dione 1 and evaluated for their antimicrobial activities. Results of the antitubercular screening against Mycobacterium tuberculosis H(37)Rv showed th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramalingam P,Ganapaty S,Rao ChB

更新日期：2010-01-01 00:00:00

abstract：:Caffeoylglucosides, which have a glucose ring as a central linker, were synthesized from methyl D-glucosides, and their anti-HIV-1 activities were tested. Among them, four dicaffeoylglucosides (IC50 = 29.1+/-35.1 microM), 6a, 6b, 9b and 10b, showed HIV-1 integrase inhibitory activity as potent as L-chicoric acid. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim SN,Lee JY,Kim HJ,Shin CG,Park H,Lee YS

更新日期：2000-08-21 00:00:00

abstract：:Scaffold hybridization of several natural and synthetic anticancer leads led to the consideration of indenoindolones as potential novel anticancer agents. A series of these compounds were prepared by a diversity-feasible synthetic method. They were found to possess anticancer activities with higher potency compared to...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kashyap M,Das D,Preet R,Mohapatra P,Satapathy SR,Siddharth S,Kundu CN,Guchhait SK

更新日期：2012-04-01 00:00:00

abstract：:Eight stilbenoids, 1-(p-hydroxybenzyl)-4,8-dimethoxyphenanthrene-2,7-diol (1), 2,7-dihydroxy-1,3-bis(p-hydroxybenzyl)-4-methoxy-9,10-dihydrophenanthrene (2), 4,7-dihydroxy-1-(p-hydroxybenzyl)-2-methoxy-9,10-dihydrophenanthrene (3), 3,3'-dihydroxy-2',6'-bis(p-hydroxybenzyl)-5-methoxybibenzyl (4), 3',5-dihydroxy-2-(p-hy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morita H,Koyama K,Sugimoto Y,Kobayashi J

更新日期：2005-02-15 00:00:00

abstract：:To continue our study of 2-morpholino-benzoxazine based compounds, which show useful activity against PI3K family enzymes or antiplatelet activity, we designed and synthesized a series of linear 6.7-fused, 5,6-angular fused and 7,8-angular fused-aryl-morpholino-naphth-oxazines. The compounds were prepared from substit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morrison R,Zheng Z,Jennings IG,Thompson PE,Al-Rawi JMA

更新日期：2016-11-15 00:00:00

abstract：:Novel C(3) propenylamide and propenylsulfonamide cephalosporins have been synthesized and tested for their ability to inhibit the penicillin-binding protein 2' (PBP2') from Staphylococcus epidermidis and the growth of a panel of clinically relevant bacterial species, including methicillin-resistant Staphylococcus aure...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pohlmann J,Vasilevich NI,Glushkov AI,Kellenberger L,Shapiro S,Caspers P,Page MG,Danel F

更新日期：2010-08-01 00:00:00

abstract：:Difluorosialic acids (DFSAs) are potent inhibitors of viral neuraminidase that demonstrate activity against oseltamivir- and zanamivir-resistant strains of influenza. Unfortunately, low oral bioavailability precludes their development as second generation neuraminidase inhibitors for treating influenza as this leaves ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arns S,Tan J,Sun S,Galey A,Zisman N,Ross F,Udechukwu J,Dercho S,Gusti V,Paquette J,Webb M,Bourque E,Withers SG,Liggins R

更新日期：2015-06-15 00:00:00

abstract：:A new class of (E)-2-alkyl-2-(4-methanesulfonylphenyl)-1-phenylethenes were designed for evaluation as selective cyclooxygense-2 (COX-2) inhibitors. The target olefins were synthesized, via a Takeda olefination reaction, followed by oxidation of the respective thiomethyl olefinic intermediate. In vitro COX-1/COX-2 inh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Uddin MJ,Rao PN,Rahim MA,McDonald R,Knaus EE

更新日期：2004-10-04 00:00:00

abstract：:A series of monocyclic thiophenes was designed and synthesized as PTP1B inhibitors. Guided by X-ray co-crystal structural information and computational modeling, rational design led to key interactions with Asp48 and improved inhibitory potency against PTP1B. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wan ZK,Lee J,Xu W,Erbe DV,Joseph-McCarthy D,Follows BC,Zhang YL

更新日期：2006-09-15 00:00:00

abstract：:PC-1 (NPP-1) inhibitors may be useful as therapeutics for the treatment of CDDP (calcium pyrophosphate dehydrate) deposition disease and osteoarthritis. We have identified a series of potent quinazolin-4-piperidin-4-ethyl sulfamide PC-1 inhibitors. The series, however, suffers from high affinity binding to hERG potass...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patel SD,Habeski WM,Cheng AC,de la Cruz E,Loh C,Kablaoui NM

更新日期：2009-06-15 00:00:00

abstract：:The glutamine transporter ASCT2 has been identified as a promising target to inhibit rapid growth of cancer cells. However, ASCT2 pharmacology is not well established. In this report, we performed a systematic structure activity analysis of a series of substituted benzylproline derivatives. Substitutions on the phenyl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh K,Tanui R,Gameiro A,Eisenberg G,Colas C,Schlessinger A,Grewer C

更新日期：2017-02-01 00:00:00

abstract：:A novel class of benzocinnolinones analogs of irdabisant were designed and synthesized as histamine H3R antagonists/inverse agonists. Modifications to the pyridazinone portion of the core and linker led to the identification of molecules with excellent target potency and selectivity with improved rat pharmacokinetic p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Josef KA,Aimone LD,Lyons J,Raddatz R,Hudkins RL

更新日期：2012-06-15 00:00:00

abstract：:Homooligomers constructed with 4- and 6-amino acid fragments of melanocortin (alpha-MSH) bind with higher affinity and with apparent cooperativity to melanocortin receptor, compared to their constituent monomers. Individual ligands were tethered with various spacers of different length and rigidity and the influence o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vagner J,Handl HL,Gillies RJ,Hruby VJ

更新日期：2004-01-05 00:00:00

abstract：:An indole compound with a strong purple-red color was produced by boiling a solution of indican under acidic conditions and purified by chromatographies on DEAE-650S Toyopearl TSK-gel and silica-gel columns. The purple-red compound purified was identified as indoxyl red, on the basis of FAB Mass, (13)C NMR, (1)H NMR, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Song J,Kitamatsu M,Imamura K,Ohmori H,Watanabe K,Nakanishi K

更新日期：2013-02-01 00:00:00

abstract：:Here we report the model studies of the reactions between NADH models (using HEH and BNAH) and sulfane sulfurs (using polysulfides). Such reactions could lead to the oxidation of NADH models and the production of hydrogen sulfide (H2S). Kinetics of the reaction between BNAH and elemental sulfur S8 were determined in e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Peng B,Liu C,Li Z,Day JJ,Lu Y,Lefer DJ,Xian M

更新日期：2017-02-01 00:00:00

abstract：:Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABA(A) receptors that are functionally selective for the alpha2/alpha3 subtypes over the alpha1 subtype. SAR studies to optimise this functional selectivity, pharmacokinetic and behavioural data are describ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jennings AS,Lewis RT,Russell MG,Hallett DJ,Street LJ,Castro JL,Atack JR,Cook SM,Lincoln R,Stanley J,Smith AJ,Reynolds DS,Sohal B,Pike A,Marshall GR,Wafford KA,Sheppard WF,Tye SJ

更新日期：2006-03-15 00:00:00

abstract：:We have demonstrated that the p-trifluoromethylphenylpropionylamino residue at the 2-position of the core structure leads to an active benzophenone-type anti-malarial agent. The attempt to improve water solubility by introduction of an amino group into the alpha-position of the arylpropionyl residue resulted in decrea...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wiesner J,Fucik K,Kettler K,Sakowski J,Ortmann R,Jomaa H,Schlitzer M

更新日期：2003-05-05 00:00:00