New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center.

abstract：:Synthesis of a symmetrically branched diglycerol (BGL002, involving one iminodiacetic residue) as a G2 dendron, and the tetradecaglycerol (BGL014, involving one iminodiacetic residue) as a G4 dendron, is described. Several members of the BGL family of G2-G4 dendrons were assembled, with G2 bearing four hydroxyl groups...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nemoto H,Ishihara A,Araki T,Katagiri A,Kamiya M,Matsushita T,Hattori H,Mimura Y,Tomoda Y,Yamasaki M

更新日期：2011-08-15 00:00:00

abstract：:A series of novel hybrid molecules 4a-y containing thiazole and benzotriazole templates were designed and synthesized. The structures of the synthesized compounds were elucidated by IR, (1)H NMR, (13)C NMR and mass spectral data. All the synthesized compounds were tested for their antimicrobial activity (zone of inhib...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gaikwad ND,Patil SV,Bobade VD

更新日期：2012-05-15 00:00:00

abstract：:Paclitaxel (PTX) was complexed with beta-cyclodextrin (1), 2,6-dimethyl-beta-cyclodextrin (2) and 2,3,6-trimethyl-beta-cyclodextrin (3). PTX-CYD complexes were characterized both at the solid and liquid states. Experimental findings are in agreement with molecular modeling analysis, which showed different PTX-CYD inte...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alcaro S,Ventura CA,Paolino D,Battaglia D,Ortuso F,Cattel L,Puglisi G,Fresta M

更新日期：2002-06-17 00:00:00

abstract：:Numerous potent P2X3 antagonists have been discovered and the therapeutic potential of P2X3 antagonism already comprises proof-of-concept data obtained in clinical trials with the most advanced compound. We have lately reported the discovery and optimization of thia-triaza-tricycle compounds with potent P2X3 antagonis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Szántó G,Makó A,Vágó I,Hergert T,Bata I,Farkas B,Kolok S,Vastag M

更新日期：2016-08-15 00:00:00

abstract：:Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2' p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cumming JN,Le TX,Babu S,Carroll C,Chen X,Favreau L,Gaspari P,Guo T,Hobbs DW,Huang Y,Iserloh U,Kennedy ME,Kuvelkar R,Li G,Lowrie J,McHugh NA,Ozgur L,Pan J,Parker EM,Saionz K,Stamford AW,Strickland C,Tadesse D,

更新日期：2008-06-01 00:00:00

abstract：:Bacterial resistance is rapidly growing, necessitating the need to discover new agents. Novel bacterial topoisomerase inhibitors (NBTIs) are new class of broad-spectrum antibacterial agents targeting bacterial DNA gyrase and topoisomerase IV. This class of inhibitors binds to an alternative binding site relative to fl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh SB,Kaelin DE,Wu J,Miesel L,Tan CM,Meinke PT,Olsen DB,Lagrutta A,Wei C,Peng X,Wang X,Fukuda H,Kishii R,Takei M,Shibata T,Ohata K,Takano H,Kurasaki H,Takeuchi T,Nishimura A,Fukuda Y

更新日期：2015-06-01 00:00:00

abstract：:A series of substituted 2-(aminoheteroaryl)-thiazole-5-carboxamide analogs have been synthesized as novel, potent inhibitors of the Src-family kinase p56Lck. Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen P,Norris D,Das J,Spergel SH,Wityak J,Leith L,Zhao R,Chen BC,Pitt S,Pang S,Shen DR,Zhang R,De Fex HF,Doweyko AM,McIntyre KW,Shuster DJ,Behnia K,Schieven GL,Barrish JC

更新日期：2004-12-20 00:00:00

abstract：:The optimization of the 4-position of recently described new 3,4-disubstituted piperidine-based renin inhibitors is reported herein. The synthesis and characterization of compounds leading to the discovery of 11 (ACT-178882, MK-1597), a renin inhibitor with a suitable profile for development is described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Corminboeuf O,Bezençon O,Remeň L,Grisostomi C,Richard-Bildstein S,Bur D,Prade L,Strickner P,Hess P,Fischli W,Steiner B,Treiber A

更新日期：2010-11-01 00:00:00

abstract：:A 26-member library of novel N-hydroxyquinolinone derivatives was synthesized by a one-pot Buchwald-type palladium catalyzed amidation and condensation sequence. The design of these rare scaffolds was inspired from N-hydroxypyridones and 2-quinolinones classes of compounds which have been shown to have rich biological...

journal_title：Bioorganic & medicinal chemistry letters

authors： Teng Y,Suwanarusk R,Ngai MH,Srinivasan R,Ong AS,Ho B,Rénia L,Chai CL

更新日期：2015-02-01 00:00:00

abstract：:The synthesis of [1-[(5-hydroxy-4-(phenylmethyl)-3-oxazolidinyl)carbonyl]-2-ethylpropy lcarbamic acid phenylmethyl ester (2; MDL 104,903), a potent inhibitor of calpain, is described. Synthesis of related compounds, which offer insights into the mechanism of action for 2, are also described, as is an O-acetyl prodrug ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Peet NP,Kim HO,Marquart AL,Angelastro MR,Nieduzak TR,White JN,Friedrich D,Flynn GA,Webster ME,Vaz RJ,Linnik MD,Koehl JR,Mehdi S,Bey P,Emary B,Hwang KK

更新日期：1999-08-16 00:00:00

abstract：:Accumulation of beta-amyloid (Abeta), produced by the proteolytic cleavage of amyloid precursor protein (APP) by beta- and gamma-secretase, is widely believed to be associated with Alzheimer's disease (AD). Research around the high-throughput screening hit (S)-4-chlorophenylsulfonyl isoleucinol led to the identificati...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cole DC,Stock JR,Kreft AF,Antane M,Aschmies SH,Atchison KP,Casebier DS,Comery TA,Diamantidis G,Ellingboe JW,Harrison BL,Hu Y,Jin M,Kubrak DM,Lu P,Mann CW,Martone RL,Moore WJ,Oganesian A,Riddell DR,Sonnenberg-Reine

更新日期：2009-02-01 00:00:00

abstract：:We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca(2+) channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca(2+) channels and N-type Ca(2+) channels. Among them, 5b (KYS05044, IC(50)=0.56+/-0.10 microM) was identified as potent T-type C...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rhim H,Lee YS,Park SJ,Chung BY,Lee JY

更新日期：2005-01-17 00:00:00

abstract：:A novel class of 2,3-diaminopyridine bradykinin B1 receptor antagonists is disclosed. Structure-activity relationship studies (SARs) that led to compounds with significantly improved potency and pharmacokinetic properties relative to the lead compound are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng DM,Wai JM,Kuduk SD,Ng C,Murphy KL,Ransom RW,Reiss D,Chang RS,Harrell CM,MacNeil T,Tang C,Prueksaritanont T,Freidinger RM,Pettibone DJ,Bock MG

更新日期：2005-05-02 00:00:00

abstract：:In the screening search for Hepatitis B virus inhibitory agents from medicinal plants, the ethanol extract of Piper longum Linn. was found to possess superior anti-HBV activity in vitro. Bioassay-guided fractionation coupled with repeated purification resulted in the isolation of four new compounds, involving two new ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jiang ZY,Liu WF,Zhang XM,Luo J,Ma YB,Chen JJ

更新日期：2013-04-01 00:00:00

abstract：:The benzothiazole aniline (BTA) conjugated with monoamine-monoamide (MAMA) was synthesized and then labeled with (99m)Tc. Its corresponding rhenium analogue was synthesized, and the fluorescent staining was performed in brain sections of both Tg mouse and Alzheimer's disease (AD) patient. The fluorescent rhenium compl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen X,Yu P,Zhang L,Liu B

更新日期：2008-02-15 00:00:00

abstract：:Methanolic extract of Miliusa balansae Finet et Gagnep exerts an anti-inflammatory effect via inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated murine RAW 264.7 macrophage cells. Three new megastigmane glycosides, milbasides A-C (1-3), together with fifteen known compounds (4-18), were ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thao NP,Luyen BT,Tai BH,Cuong NM,Kim YC,Minh CV,Kim YH

更新日期：2015-09-15 00:00:00

abstract：:3-alkyl-2,4,5-triarylfurans with basic side-chain substituents were prepared as ligands for the estrogen receptor. Those analogues having the basic side chain on the C(4) phenol were high-affinity, ERalpha-selective antagonists. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mortensen DS,Rodriguez AL,Sun J,Katzenellenbogen BS,Katzenellenbogen JA

更新日期：2001-09-17 00:00:00

abstract：:A series of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides were synthesized in an effort to prepare novel atypical antipsychotic agents. The compounds were synthesized by either microwave irradiation technique or by conventional synthesis and were characterized by spectral data (IR, (1)H N...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sekhar KV,Rao VS,Devambatla RKV,Kumar MM

更新日期：2008-12-01 00:00:00

abstract：:Benzalacetone synthase (BAS) and chalcone synthase (CHS) are plant-specific type III polyketide synthases (PKSs), sharing 70% amino acid sequence identity and highly homologous overall protein structures. BAS catalyzes the decarboxylative coupling of 4-coumaroyl-CoA with malonyl-CoA to produce the diketide benzalaceto...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shimokawa Y,Morita H,Abe I

更新日期：2010-09-01 00:00:00

abstract：:Quantitative fluorescence-based methods have been developed to determine the nuclear concentration of polyamide-fluorescein conjugates in cell culture. Confocal laser scanning microscopy and flow cytometry techniques are utilized to plot calibration curves, from which the nuclear concentration can be interpolated. Upo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hsu CF,Dervan PB

更新日期：2008-11-15 00:00:00

abstract：:Replacement of the C-terminal carboxylic acid functionality of peptide inhibitors of hepatitis C virus (HCV) NS3 protease (complexed with NS4A peptide cofactor) by activated carbonyl groups does not produce any substantial increase in potency. These latter inhibitors also inhibit a variety of other serine and cysteine...

journal_title：Bioorganic & medicinal chemistry letters

authors： Llinàs-Brunet M,Bailey M,Déziel R,Fazal G,Gorys V,Goulet S,Halmos T,Maurice R,Poirier M,Poupart MA,Rancourt J,Thibeault D,Wernic D,Lamarre D

更新日期：1998-10-06 00:00:00

abstract：:In our ongoing search for new anti-invasive chemotypes, we have made an excursion from previously reported potent 1,3-diarylpropenones (chalcones) to congeners bearing longer linkers between the aromatic moieties. Nine 1,ω-diarylalkenones, including curcumin and bisdemethoxycurcumin, were evaluated in the chick heart ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roman BI,De Ryck T,Verhasselt S,Bracke ME,Stevens CV

更新日期：2015-03-01 00:00:00

abstract：:We screened 1434 small heterocyclic molecules and identified thirteen 2,3,6-trisubstituted quinoxaline derivatives that were able to inhibit the Wnt/β-catenin signal pathway and cell proliferation. In the screen, some of the hit compounds such as the ethylene group-coupled quinoxaline derivatives were shown to hold pr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee SB,Park YI,Dong MS,Gong YD

更新日期：2010-10-01 00:00:00

abstract：:A series of N-7-methyl-imidazolopyrimidine inhibitors of the mTOR kinase have been designed and prepared, based on the hypothesis that the N-7-methyl substituent on imidazolopyrimidine would impart selectivity for mTOR over the related PI3Kα and δ kinases. The corresponding N-Me substituted pyrrolo[3,2-d]pyrimidines a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee W,Ortwine DF,Bergeron P,Lau K,Lin L,Malek S,Nonomiya J,Pei Z,Robarge KD,Schmidt S,Sideris S,Lyssikatos JP

更新日期：2013-09-15 00:00:00

abstract：:We report a fluorinated and iodinated radiotracer as a probe for PET/SPECT to detect of β-amyloid (Aβ) plaques in the brain of patients with Alzheimer's disease (AD). We successfully designed and synthesized the fluorinated and iodinated aurone derivative (3) and its radiolabels ([(125)I]3 and [(18)F]3). In binding ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Watanabe H,Ono M,Kimura H,Kagawa S,Nishii R,Fuchigami T,Haratake M,Nakayama M,Saji H

更新日期：2011-11-01 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：:We report the first biological evaluation the 1,2,3-thiaselenazole class of compound and utilising a concise synthetic approach of sulfur extrusion, selenium insertion of the 1,2,3-dithiazoles. We created a small diverse library of compounds to contrast the two ring systems. This approach has highlighted new structure...

journal_title：Bioorganic & medicinal chemistry letters

authors： Asquith CRM,Meili T,Laitinen T,Baranovsky IV,Konstantinova LS,Poso A,Rakitin OA,Hofmann-Lehmann R

更新日期：2019-07-15 00:00:00

abstract：:The biosynthetic gene cluster of brassicicene C was identified in Alternaria brassicicola strain ATCC 96836 from genome database search. In vivo and in vitro study clearly revealed the function of Orf8 and Orf6 as a fusicoccadiene synthase and methyltransferase, respectively. The understanding toward the biosynthetic ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Minami A,Tajima N,Higuchi Y,Toyomasu T,Sassa T,Kato N,Dairi T

更新日期：2009-02-01 00:00:00

abstract：:A novel class of indomethacin analogs were synthesized wherein a N-difluoromethyl-1,2-dihydropyrid-2-one moiety (5-LOX pharmacophore) was attached at its C-4 or C-5 position via either a CO (14a-b) or CH(2) (19a-b) linker to the indole N(1)-position. In this regard, replacement of the 4-chlorobenzoyl group present in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chowdhury MA,Huang Z,Abdellatif KR,Dong Y,Yu G,Velázquez CA,Knaus EE

更新日期：2010-10-01 00:00:00

abstract：:Virtual screening, a fast, computational approach to identify drug leads [Perola, E.; Xu, K.; Kollmeyer, T. M.; Kaufmann, S. H.; Prendergast, F. G. J. Med. Chem.2000, 43, 401; Miller, M. A. Nat. Rev. Drug Disc.2002, 1 220], is limited by a known challenge in crystallographically determining flexible regions of protein...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dooley AJ,Shindo N,Taggart B,Park JG,Pang YP

更新日期：2006-02-15 00:00:00