Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1.

abstract：:Thermal transformation of the (+)-catechin (1) with heating processing afforded a new oxidation product, gambiriin D (2), along with catechin [6'-8]-catechin (3), and (+)-epicatechin (4). The structure of a new catechin dimer with C-C linkage was determined on the basis of spectroscopic data interpretation. The catech...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim T,Choi HJ,Eom SH,Lee J,Kim TH

更新日期：2014-03-15 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：:Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D(3)/D(2) compound (1) led to a series of new piperazine derivatives having affinity to both dopamine D(3) and D(2) receptors. Several members of this group showed excellent pharmacokinetic and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Agai-Csongor E,Domány G,Nógrádi K,Galambos J,Vágó I,Keserű GM,Greiner I,Laszlovszky I,Gere A,Schmidt E,Kiss B,Vastag M,Tihanyi K,Sághy K,Laszy J,Gyertyán I,Zájer-Balázs M,Gémesi L,Kapás M,Szombathelyi Z

更新日期：2012-05-15 00:00:00

abstract：:High throughput screening of the corporate compound collection led to the discovery of a novel series of substituted aminoalkoxybenzyl pyrrolidines as human urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that led to the identification of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin J,Dhanak D,Knight SD,Widdowson K,Aiyar N,Naselsky D,Sarau HM,Foley JJ,Schmidt DB,Bennett CD,Wang B,Warren GL,Moore ML,Keenan RM,Rivero RA,Douglas SA

更新日期：2005-07-01 00:00:00

abstract：:A group of novel synthetic indoloisoquinolines was prepared and its potential as a novel series of small-molecule anti-malarial leads was assessed. The structure-activity relationship on variation of three distinct regions of chemical space was investigated. A lead compound was generated with an activity close to that...

journal_title：Bioorganic & medicinal chemistry letters

authors： Horrocks P,Fallon S,Denman L,Devine O,Duffy LJ,Harper A,Meredith EL,Hasenkamp S,Sidaway A,Monnery D,Phillips TR,Allin SM

更新日期：2012-02-15 00:00:00

abstract：:Selective inhibition of the aspartyl protease renin has gained attraction as an interesting approach to control hypertension and associated cardiovascular risk factors given its unique position in the renin-angiotensin system. Using a combination of high-throughput screening, parallel synthesis, X-ray crystallography ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scheiper B,Matter H,Steinhagen H,Stilz U,Böcskei Z,Fleury V,McCort G

更新日期：2010-11-01 00:00:00

abstract：:β-Sitosterol is the most abundant plant sterol in the human diet. It is also the major component of several traditional medicines, including saw palmetto and devil's claw. Although β-sitosterol is effective against enlarged prostate in human clinical trials and has anti-cancer and anti-inflammatory activities, the mec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lomenick B,Shi H,Huang J,Chen C

更新日期：2015-11-01 00:00:00

abstract：:The reduced activation of PPARs has a positive impact on cancer cell growth and viability in multiple preclinical tumor models, suggesting a new therapeutic potential for PPAR antagonists. In the present study, the benzothiazole amides 2a-g were synthesized and their activities on PPARs were investigated. Transactivat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ammazzalorso A,De Lellis L,Florio R,Laghezza A,De Filippis B,Fantacuzzi M,Giampietro L,Maccallini C,Tortorella P,Veschi S,Loiodice F,Cama A,Amoroso R

更新日期：2019-08-15 00:00:00

abstract：:A new 'naked-eye' quinoline-based 'reactive' ratiometric fluorescent probe was prepared. The reactive stoichiometry of the probe with Hg²⁺ ion was 2:1. The probe exhibited high selectivity towards Hg²⁺ ion to other metal ions with a 410-fold increase in absorbance intensity ratio (A₄₀₂/A₃₄₀) in aqueous solution over a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Y,Yan Y,Chen S,Gao Z,Xu H

更新日期：2014-12-01 00:00:00

abstract：:Germinal center kinase-like kinase (GLK, also known as MAP4K3) has been hypothesized to have an effect on key cellular activities, including inflammatory responses. GLK is required for activation of protein kinase C-θ (PKCθ) in T cells. Controlling the activity of T helper cell responses could be valuable for the trea...

journal_title：Bioorganic & medicinal chemistry letters

authors： May-Dracka TL,Arduini R,Bertolotti-Ciarlet A,Bhisetti G,Brickelmaier M,Cahir-McFarland E,Enyedy I,Fontenot JD,Hesson T,Little K,Lyssikatos J,Marcotte D,McKee T,Murugan P,Patterson T,Peng H,Rushe M,Silvian L,Spilker K

更新日期：2018-06-01 00:00:00

abstract：:Esculentoside A (EsA) has been reported to possess anti-inflammatory activity and selective inhibitory activity towards cyclooxygenase-2. A series of derivatives of EsA were synthesized by converting the C-28 carboxylic acid group into amides. The haemolytic activity and inhibitory activity towards cyclooxygenase-2 we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wu F,Yi Y,Sun P,Zhang D

更新日期：2007-12-01 00:00:00

abstract：:Surface enhanced resonance Raman scattering (SERRS) is an alternative to fluorescence for use in bioanalysis however due to the different optical mechanism it requires specifically designed reporters. Recently we have reported the use of 8-hydroxyquinolinyl azo dyes and their ester derivatives as reporters of lipase a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ingram A,Moore BD,Graham D

更新日期：2009-03-15 00:00:00

abstract：:We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hong Q,Bakshi RK,Palucki BL,Park MK,Ye Z,He S,Pollard PG,Sebhat IK,Liu J,Guo L,Cashen DE,Martin WJ,Weinberg DH,MacNeil T,Tang R,Tamvakopoulos C,Peng Q,Miller RR,Stearns RA,Chen HY,Chen AS,Strack AM,Fong TM,M

更新日期：2011-04-15 00:00:00

abstract：:A new series of potential inhibitors of DNA topoisomerase II were synthesized from facile materials (aromatic aldehydes, Meldrum's acid and 2-hydroxynaphthalene-1,4-dione) under microwave irradiation. The method provides a valuable tool in designing new and more potent cytotoxic analogues. This procedure is advantageo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wei P,Zhang X,Tu S,Yan S,Ying H,Ouyang P

更新日期：2009-02-01 00:00:00

abstract：:Retinoid X Receptor (RXR) specific ligands are currently being investigated for the treatment of metabolic diseases such as type II diabetes. We report the synthesis of conformationally locked retinoids, which are potent RXR selective ligands, and the attempted synthesis of 9-cyclopropyl locked analogs of RA and 9-cis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vuligonda V,Garst ME,Chandraratna RA

更新日期：1999-02-22 00:00:00

abstract：:The peptide ligase subtiligase, derived from subtilisin, has been employed in the identification of protein N-termini in complex mixtures. Here, the peptide ester substrates for the ligation reaction were optimized with respect to solubility, resulting in greater incorporation of the N-terminal tags. Additionally, the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yoshihara HA,Mahrus S,Wells JA

更新日期：2008-11-15 00:00:00

abstract：:Two (99m)Tc/Re complexes based on flavone and aurone were tested as potential probes for imaging β-amyloid plaques using single photon emission computed tomography. Both (99m)Tc-labeled derivatives showed higher affinity for Aβ(1-42) aggregates than did (99m)Tc-BAT. In sections of brain tissue from an animal model of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ono M,Ikeoka R,Watanabe H,Kimura H,Fuchigami T,Haratake M,Saji H,Nakayama M

更新日期：2010-10-01 00:00:00

abstract：:Previously, potent factor Xa inhibitors were described based on a pyrazole core. Modifications of the pyrazole core have provided additional novel, highly potent factor Xa inhibitors. This manuscript will describe the synthesis and biological activity of factor Xa inhibitors containing the 1H-pyrazolo[4,3-d]pyrimidin-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fevig JM,Cacciola J,Buriak J Jr,Rossi KA,Knabb RM,Luettgen JM,Wong PC,Bai SA,Wexler RR,Lam PY

更新日期：2006-07-15 00:00:00

abstract：:The selective inhibition of coagulation factor Xa has emerged as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe highly potent benzamidine factor Xa inhibitors based on a vicinally-substituted heterocyclic core. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fevig JM,Pinto DJ,Han Q,Quan ML,Pruitt JR,Jacobson IC,Galemmo RA Jr,Wang S,Orwat MJ,Bostrom LL,Knabb RM,Wong PC,Lam PYS,Wexler RR

更新日期：2001-03-12 00:00:00

abstract：:The inhibition of ribonuclease Bi by 3'-N-hydroxyurea-3'-deoxythymidine 5'-phosphate is enhanced by 30-fold in the presence of Zn(2+). Thus, an N-hydroxyurea nucleotide can recruit Zn(2+) to inhibit the enzymatic activity of a ribonuclease. This result engenders a general strategy for the inhibition of non-metalloenzy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Higgin JJ,Yakovlev GI,Mitkevich VA,Makarov AA,Raines RT

更新日期：2003-02-10 00:00:00

abstract：:Bioassay-guided fractionation of the EtOAc extract of the stem bark of Erythrina abyssinica (Leguminosae) resulted in the isolation of three new (1-3), along with 12 known (4-15) pterocarpan derivatives. Their chemical structures were determined by physicochemical and spectroscopic data analysis (IR, UV, [alpha](D), C...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen PH,Le TV,Thuong PT,Dao TT,Ndinteh DT,Mbafor JT,Kang KW,Oh WK

更新日期：2009-12-01 00:00:00

abstract：:New inhibitors of histone deacetylase (HDAC) have been synthesized and evaluated for their activity toward non small lung cancer cell line H661. Their design is based on indanone (or tetralone) systems leading to trichostatin A (TSA) analogs with limited conformational mobility. Molecular modelization at the AM1 level...

journal_title：Bioorganic & medicinal chemistry letters

authors： Charrier C,Bertrand P,Gesson JP,Roche J

更新日期：2006-10-15 00:00:00

abstract：:Nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) are gaining attention as potentially gastric-sparing NSAIDs. Herein, we report a novel class of '1-(nitrooxy)ethyl ester' group-containing NSAIDS as efficient NO releasing 'true' prodrugs of aspirin and naproxen. While an aspirin prodrug exhibite...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gund M,Gaikwad P,Borhade N,Burhan A,Desai DC,Sharma A,Dhiman M,Patil M,Sheikh J,Thakre G,Tipparam SG,Sharma S,Nemmani KVS,Satyam A

更新日期：2014-12-15 00:00:00

abstract：:We have recently reported that the elaboration of the N-substituent in the δ opioid receptor (DOR) antagonist naltrindole (NTI) enabled the regulation of the DOR activities from full inverse agonists to weak partial agonists. The investigations of amide-type NTI derivatives revealed that N-phenylacetyl and N-dihydroci...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujii H,Uchida Y,Shibasaki M,Nishida M,Yoshioka T,Kobayashi R,Honjo A,Itoh K,Yamada D,Hirayama S,Saitoh A

更新日期：2020-06-15 00:00:00

abstract：:The effects of 14 sesquiterpene hydroquinones, including 8 marine sponge-derived avarols (1-8) and 6 semisynthetic derivatives (9-14), on lipid droplet accumulation and neutral lipid synthesis in Chinese hamster ovary (CHO) K1 cells were investigated. In intact CHO-K1 cell assays, avarol (1) markedly decreased the num...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohshiro T,Kobayashi K,Suzuki A,Yamazaki H,Uchida R,Namikoshi M,Tomoda H

更新日期：2019-08-15 00:00:00

abstract：:A novel series of diphenyl lactam containing calcium channel blockers is described. Extensive SAR studies resulted in compounds with low molar activity and good plasma exposure after oral dosing. Compounds 2, 6 and 7 demonstrated significant efficacy in the capsaicin model of secondary hyperalgesia following oral admi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Doherty GA,Bhatia P,Vortherms TA,Marsh KC,Wetter JM,Mack H,Scott VE,Jarvis MF,Stewart AO

更新日期：2012-02-15 00:00:00

abstract：:A novel series of hepatitis C virus (HCV) NS3/4A protease inhibitors bearing a P2-P4 macrocycle and a P1-P1' alpha-ketoamide serine trap is reported. The NS3 protease, which is essential for viral replication, is considered one of the most attractive targets for developing novel anti-HCV therapies. The optimization of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Avolio S,Robertson K,Hernando JI,DiMuzio J,Summa V

更新日期：2009-04-15 00:00:00

abstract：:Thirty-five novel chromone derivatives containing dithioacetal moiety were designed, synthesized, and their anti-TMV activities were evaluated through half-leaf method. The results showed compound c23 illustrates highly curative, protective and inactivating activities against TMV at 500 mg/L, with the values of 68.8%,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li M,Zan N,Huang M,Jiang D,Hu D,Song B

更新日期：2020-03-01 00:00:00

abstract：:The methylendioxyphenyl group, present in a number of potent endothelin receptor antagonists, could have undesirable metabolic interactions with cytochrome P450 in vivo. Using a self-organizing neural network we analysed the features of molecular electrostatic potentials of several endothelin receptor ligands. A libra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Anzali S,Mederski WW,Osswald M,Dorsch D

更新日期：1998-01-06 00:00:00

abstract：:Novel prostaglandin E2 receptor 4 (EP4) agonists featuring a pyridone core and an allylic alcohol ω-chain were discovered. These agonists were shown to be selective over EP1, EP2 and EP3. Analogs harboring a 4-carboxylic acid phenethyl α-chain displayed improved potency over those containing an n-heptanoic acid chain....

journal_title：Bioorganic & medicinal chemistry letters

authors： Dorich S,Cox JH,Burch JD,Chagnon F,Chen B,Léger S,St-Onge M,Fader LD

更新日期：2020-05-15 00:00:00