The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines.

abstract：:Herein we report the preparation of a combinatorial library of compounds with potent CCR5 binding affinity. The library design was aided by SAR generated in a traditional medicinal chemistry effort. Compounds with novel combinations of subunits were discovered that have high binding affinity for the CCR5 receptor. A p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Willoughby CA,Berk SC,Rosauer KG,Degrado S,Chapman KT,Gould SL,Springer MS,Malkowitz L,Schleif WA,Hazuda D,Miller M,Kessler J,Danzeisen R,Holmes K,Lineberger J,Carella A,Carver G,Emini EA

更新日期：2001-12-17 00:00:00

abstract：:The synthesis of two separable isomeric testosterone dimers is reported. The dimers are made from testosterone in a 5 step sequence and with 36% overall yield. The key dimerization step was performed using Hoveyda-Grubb's metathesis catalysts on 7alpha-allyltestosterone with 75% yield. The synthesis led to separable i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bastien D,Leblanc V,Asselin E,Bérubé G

更新日期：2010-04-01 00:00:00

abstract：:A novel series of malonamide derivatives was synthesized. These amides were shown to be potent and selective kappa opioid receptor agonists. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chu GH,Gu M,Cassel JA,Belanger S,Graczyk TM,DeHaven RN,Conway-James N,Koblish M,Little PJ,DeHaven-Hudkins DL,Dolle RE

更新日期：2007-04-01 00:00:00

abstract：:A novel series of imidazo[1,5-a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused primarily on dialkylamino side chain optimization. SAR of the aryl and small alkyl substituents was also explored. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hartz RA,Gilligan PJ,Nanda KK,Tebben AJ,Fitzgerald LW,Miller K

更新日期：2002-02-11 00:00:00

abstract：:PNU-159682 is a highly potent secondary metabolite of nemorubicin belonging to the anthracycline class of natural products. Due to its extremely high potency and only partially understood mechanism of action, it was deemed an interesting starting point for the development of a new suite of linker drugs for antibody dr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Holte D,Lyssikatos JP,Valdiosera AM,Swinney Z,Sisodiya V,Sandoval J,Lee C,Aujay MA,Tchelepi RB,Hamdy OM,Gu C,Lin B,Sarvaiya H,Pysz MA,Laysang A,Williams S,Jun Lee D,Holda MK,Purcell JW,Gavrilyuk J

更新日期：2020-12-15 00:00:00

abstract：:A new series of 5-[(3'-chloro-4',4'-disubstituted-2-oxoazetidinyl)(N-nitro)amino]-6-hydroxy-3-alkyl/aryl[1,3]azaphospholo[1,5-a]pyridin-1-yl-phosphorus dichlorides has been synthesized and subjected to acute antibacterial and antifungal screening studies. All the derivatives belonging to this series delineated remarka...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharma P,Kumar A,Sharma S,Rane N

更新日期：2005-02-15 00:00:00

abstract：:By linking the mercapto groups with isopropyl and introducing L-amino acid into the 5-carboxyl of DMSA a class of novel 5-(1-carbonyl-L-amino-acid)-2,2- dimethyl-[1,3]dithiolane-4-carboxylic acids were prepared. Their in vivo activities were evaluated on lead loaded mice at the dose of 0.4 mmol/kg. The results showed ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu Y,Wang Y,Zhao M,Hou B,Peng L,Zheng M,Wu J,Peng S

更新日期：2011-03-15 00:00:00

abstract：:The discovery of potent benzimidazole stearoyl-CoA desaturase (SCD1) inhibitors by ligand-based virtual screening is described. ROCS 3D-searching gave a favorable chemical motif that was subsequently optimized to arrive at a chemical series of potent and promising SCD1 inhibitors. In particular, compound SAR224 was se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matter H,Zoller G,Herling AW,Sanchez-Arias JA,Philippo C,Namane C,Kohlmann M,Pfenninger A,Voss MD

更新日期：2013-03-15 00:00:00

abstract：:A series of glutathione derivatives 1-4, modified at the N,S and/or COOH sites, with in vitro antitrypanosomal activity were tested against bloodstream form Trypanosoma brucei 247 wild type and a T. b. brucei 247 strain over-expressing the multiple drug resistance protein (MRPA) by 50-100x to assess the susceptibility...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alibu VP,Daunes S,D'Silva C

更新日期：2013-08-01 00:00:00

abstract：:The discovery, synthesis, potential binding mode, and in vitro kinase profile of several pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines as potent kinase inhibitors are discussed. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alberti MJ,Auten EP,Lackey KE,McDonald OB,Wood ER,Preugschat F,Cutler GJ,Kane-Carson L,Liu W,Jung DK

更新日期：2005-08-15 00:00:00

abstract：:Valienol-derived allylic C-1 bromides have been used as carbaglycosyl donors for α-xylo configured valienamine pseudodisaccharide synthesis. We synthesised valienamine analogues of the Glc(α1→3)Glc and Glc(α1→3)Man disaccharides representing the linkages cleaved by α-Glucosidase II in N-glycan biosynthesis. These (N1→...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cumpstey I,Ramstadius C,Eszter Borbas K,Alonzi DS,Butters TD

更新日期：2011-09-15 00:00:00

abstract：:In order to exploit cyclophilin as a potential target for neurological drug design, we demonstrate in this presentation that several nonimmunosuppressant analogues of cyclosporin A, modified at the various positions in the 'effector' domain, are equipotent nerve growth agents compared to cyclosporin A. Our results sug...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wei L,Steiner JP,Hamilton GS,Wu YQ

更新日期：2004-09-06 00:00:00

abstract：:A new generation of propylene-spaced fluorous allyltin reagents [(Rf(CH2)3)3SnCH2CH = CH2] is described. These succeed in radical allylations where their lower homologs (ethylene-spaced) fail, and they provide improved performance in transition metal catalyzed allylations. The reagents and byproducts are readily separ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Curran DP,Luo Z,Degenkolb P

更新日期：1998-09-08 00:00:00

abstract：:A protein without natural binding functions was engineered to bind HIV-1 integrase. Phage display selections applied a library of variants based on the C-terminal domain of the eye lens protein human γS-crystallin. Multiple loop regions were altered to encode libraries with ≈3.6 × 10(11) different variants. A crystall...

journal_title：Bioorganic & medicinal chemistry letters

authors： Moody IS,Verde SC,Overstreet CM,Edward Robinson W Jr,Weiss GA

更新日期：2012-09-01 00:00:00

abstract：:The stereospecific synthesis of two all-syn-EPA-derived isoprostanes (iPs), 5-epi-8,12-iso-iPF(3alpha)-VI 17 and 8,12-iso-iPF(3alpha)-VI 18, has been accomplished. These two synthetic probes have been used to discover and identify their presence in human urine. The eventual quantitative measurement of these two iPs ma...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chang CT,Patel P,Kang N,Lawson JA,Song WL,Powell WS,FitzGerald GA,Rokach J

更新日期：2008-10-15 00:00:00

abstract：:The objective of this study was to develop a positron emission tomography (PET) probe with hypoxia targeting specificity and a relatively long half-life. The synthesis, (64)Cu-labeling in vitro and in vivo study of the novel 2-nitroimidazole complex (64)Cu-BMS2P2 is presented in this study. The hypoxia targeting capac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Luo Z,Zhu H,Lin X,Chu T,Luo R,Wang Y,Yang Z

更新日期：2016-03-01 00:00:00

abstract：:A novel series of potent zwitterionic uracil GnRH antagonists were discovered that showed reduced liability for CYP3A4 enzyme inhibition. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Regan CF,Guo Z,Chen Y,Huang CQ,Chen M,Jiang W,Rueter JK,Coon T,Chen C,Saunders J,Brown MS,Betz SF,Struthers RS,Yang C,Wen J,Madan A,Zhu YF

更新日期：2008-08-15 00:00:00

abstract：:Quinolizidinyl derivatives of the tricyclic systems characterizing pirenzepine and nuvenzepine, were prepared and tested as ligands for muscarinic M1, M2 and M3 receptors; 5,11-dihydro-11-[(S-lupinyl)-thioacetyl]-6H-pyrido[2,3-b][1, 4]benzodiazepin-6-one exhibited IC50 = 10 nM for M1 and 760 nM for both M2 and M3 subt...

journal_title：Bioorganic & medicinal chemistry letters

authors： Novelli F,Sparatore A,Tasso B,Sparatore F

更新日期：1999-10-18 00:00:00

abstract：:The paper describes the dominating role of surface tension (ST) on the modeling, monitoring, and estimating pK(a) for a large series of 43 substituted sulfonamides. Because of the direct correlation of ST with parachor (Pc) vis-a-vis molecular volume (MV), ST is considered as a steric parameter. Single as well as mult...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thakur M,Thakur A,Khadikar PV,Supuran CT

更新日期：2005-01-03 00:00:00

abstract：:The synthesis and pharmacological activity of novel nociceptin/orphanin FQ (N/OFQ) analogues modified in the Phe(1)-Gly(2) peptide bond are reported. The aim of the present work was to elucidate the importance of this peptide bond for the N/OFQ receptor (NOP) interaction. Our study indicates that the first peptide bon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guerrini R,Rizzi D,Zucchini M,Tomatis R,Regoli D,Calo' G,Salvadori S

更新日期：2003-02-10 00:00:00

abstract：:Analogues of BIBP 3226, (R)-N(alpha)-diphenylacetyl-N-(4-hydroxybenzyl)argininamide, were synthesized and investigated for Y1 antagonism (Ca2+-assay, HEL cells) and binding on Y1, Y2 and Y5 receptors. Replacing the benzylamino by a tetrahydrobenzazepinyl group preserves most of the Y1 activity. Combination with a N(G)...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aiglstorfer I,Hendrich I,Moser C,Bernhardt G,Dove S,Buschauer A

更新日期：2000-07-17 00:00:00

abstract：:Four platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with different bidentate dicarboxylates (1 oxalate, 2 malonate, 3 1,1-cyclobutanedicarboxylate and 4 3-hydroxy-1,1-cyclobutanedicarboxylate) as leaving groups were synthesized and characterized by elemental analyses, IR and (1)HNMR spectra together w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu G,Zhao J,Gou S,Pang J

更新日期：2015-01-15 00:00:00

abstract：:Constraining the catechol aryl ether moiety of bastadins by incorporation into a macrocyle is not necessary in order to mimic the effects of these marine natural products on neuronal calcium homeostasis. Simple, acyclic analogs that embody the 'western' or 'eastern' parts of bastadins were found to evoke comparable re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zieminska E,Lazarewicz JW,Couladouros EA,Moutsos VI,Pitsinos EN

更新日期：2008-11-01 00:00:00

abstract：:To develop more valuable and effective fungicide candidates, a novel series of 3,4-dichloroisothioxazole-based cycloalkylsulfonamides were synthesized and their structures were identified by 1H NMR, 13C NMR, MS and elemental analysis. Compound 3k was further confirmed by X-ray single crystal diffraction. The in vitro ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Y,Wang M,Ahmed M,He L,Ji M,Qi Z,Li X

更新日期：2019-06-01 00:00:00

abstract：:The discovery of the potency-enhancing effect of 5-substitutions on the novel 2-arylindoles as nonpeptidyl GnRH receptor antagonists led to the identification of several analogues with high affinities on the GnRH receptor. The syntheses and SARs of these 5-substituted-2-arylindole analogues are reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chu L,Lo JL,Yang YT,Cheng K,Smith RG,Fisher MH,Wyvratt MJ,Goulet MT

更新日期：2001-02-26 00:00:00

abstract：:A series of 3-aminoquinazolinediones was synthesized and evaluated for its antibacterial and DNA gyrase activity. The SAR around the quinazolinedione core was explored and the optimal substitutions were combined to give two compounds, 2r and 2s, with exceptional enzyme potency (IC50 = 0.2 microM) and activity against ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tran TP,Ellsworth EL,Sanchez JP,Watson BM,Stier MA,Showalter HD,Domagala JM,Shapiro MA,Joannides ET,Gracheck SJ,Nguyen DQ,Bird P,Yip J,Sharadendu A,Ha C,Ramezani S,Wu X,Singh R

更新日期：2007-03-01 00:00:00

abstract：:A number of novel 1-(3-arylprop-2-ynyl) substituted 1,2-dihydroquinoline derivatives related to nimesulide and their 2-oxo analogues have been designed as potential inhibitors of PDE4. All these compounds were synthesized by using Sonogashira coupling as a key step. In vitro PDE4B inhibitory properties and molecular m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pal S,Durgadas S,Nallapati SB,Mukkanti K,Kapavarapu R,Meda CL,Parsa KV,Pal M

更新日期：2011-11-01 00:00:00

abstract：:Developing targeted validation probes that can interrogate biology is of interest for both chemists and biologists. The synthesis of suitable compounds provides a means for avoiding the costly labeling of cells with specific antibodies and the bias associated with the interpretation of biological validation experiment...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ho LA,Thomas E,McLaughlin RA,Flematti GR,Fuller RO

更新日期：2016-10-15 00:00:00

abstract：:An efficient synthesis of [D-lysine](8)cyclosporin A has been developed. Several analogs of [D-lysine](8)cyclosporin A have been synthesized and show promising anti-HCV activity, particularly compounds 39 and 43, which each exhibit an anti-HCV EC(50)<200 nM, and are each ≥50-fold less immunosuppressive than cyclospori...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scribner A,Houck D,Huang Z,Mosier S,Peel M,Scorneaux B

更新日期：2010-11-15 00:00:00

abstract：:We report herein the synthesis and stereochemical structure-activity relationships of novel morpholine analogues 12 and 13 with regards to NK1, NK2 and NK3 tachykinin receptor binding affinity. An essential requirement for more potent binding affinities was controlled by absolute configuration. (S,R)-12 and (S,R)-13 e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nishi T,Ishibashi K,Takemoto T,Nakajima K,Fukazawa T,Iio Y,Itoh K,Mukaiyama O,Yamaguchi T

更新日期：2000-08-07 00:00:00