(R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT1B/1D ligands.

abstract：:2('),3(')-Didehydro-2('),3(')-dideoxynucleosides are clinically relevant antiviral agents. These nucleosides could be degraded under acidic conditions. Acidic stability studies showed the D4N had the following increasing stability order: D4G

journal_title：Bioorganic & medicinal chemistry letters

authors： Shi J,Ray AS,Mathew JS,Anderson KS,Chu CK,Schinazi RF

更新日期：2004-05-03 00:00:00

abstract：:A series of 4,4-disubstituted cyclohexylamine based CCR5 antagonists has been designed and synthesized. Their antiviral structure-activity relationship has been extensively explored. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Duan M,Aquino C,Dorsey GF Jr,Ferris R,Kazmierski WM

更新日期：2009-09-01 00:00:00

abstract：:A general protocol for the synthesis of paclitaxel C-10 carbamates is described. The method entails MeI-mediated activation of 2'-O-TBS-7-O-TES-10-O-deacetyl-paclitaxel-10-O-carbonylimidazole prior to reaction with amines. This method is effective for the synthesis of paclitaxel C-10 derivatives, including bifunctiona...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ballatore C,Aspland SE,Castillo R,Desharnais J,Eustaquio T,Sun C,Castellino AJ,Smith AB 3rd

更新日期：2005-05-16 00:00:00

abstract：:Selective metabotropic glutamate receptor 2 (mGluR2) inhibitors have been demonstrated to show therapeutic effects by improving alleviating symptoms of schizophrenic patients in clinical studies. Herein we report the synthesis and preliminary evaluation of a 11C-labeled positron emission tomography (PET) tracer origin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumata K,Zhang Y,Ogawa M,Kurihara Y,Mori W,Hu K,Fujinaga M,Nengaki N,Zhang MR

更新日期：2020-12-01 00:00:00

abstract：:Cu(II) complexes of Alzheimer's disease-related β-amyloid (Aβ) peptides exhibit metal-centered oxidation chemistry. The metallo-Aβ complexes are the hallmark of the disease and have been attributed to the generation of reactive oxygen species (ROS), causing oxidative stress. In this communication, the inhibitions of t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hashim A,Wang L,Juneja K,Ye Y,Zhao Y,Ming LJ

更新日期：2011-11-01 00:00:00

abstract：:The resistance of pathogenic fungi and failure of drug therapy increased dramatically. Numerous studies have reported the individual or synergistic antifungal potency of natural and synthesized flavonoids, especially against drug-resistant fungi. This brief review summarizes the structure and individual or synergistic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin YS

更新日期：2019-10-01 00:00:00

abstract：:Synthetic array technology was utilized to rapidly synthesize and analyze a diverse set of reductive alkylation analogues of daptomycin. Analysis of the array suggested the use of polar functionality such as sulfonamides or amide or polar spaces such as piperazine would beneficially affect activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Siedlecki J,Hill J,Parr I,Yu X,Morytko M,Zhang Y,Silverman J,Controneo N,Laganas V,Li T,Li J,Keith D,Shimer G,Finn J

更新日期：2003-12-01 00:00:00

abstract：:Extensive SAR studies and optimization of ADME properties of benzimidazol-2-one derivatives led to the identification of BMS-433771 (3) as an orally active RSV fusion inhibitor. In order to extend the structure-activity relationships for this compound series, substitution of the benzimidazole ring was examined with a ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang XA,Cianci CW,Yu KL,Combrink KD,Thuring JW,Zhang Y,Civiello RL,Kadow KF,Roach J,Li Z,Langley DR,Krystal M,Meanwell NA

更新日期：2007-08-15 00:00:00

abstract：:Various bis(2-hydroxy-3-chloropropyl)alkylamines were synthesized by coupling primary amine with epichlorohydrin and utilized as a monomer to react with ethylenediamine (EDA), N,N'-dimethylethylenediamine (DMEDA), or tetramethylethylenediamine (TMEDA) to generate a series of lipopolyhydroxylalkyleneamines. The number-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Q,Zhang G,Marhefka J,Kameneva MV,Liu D

更新日期：2006-05-01 00:00:00

abstract：:The alpha7 subtype of the neuronal nicotinic acetylcholine receptors (nAChRs) was targeted for the design of selective agonists deriving from the quinuclidine scaffold. Arylidene groups at the 3-position and N-methyl quinuclidine were found to be selective agonists with EC(50)s of 1.5 and 40 microM, respectively. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Leonik FM,Papke RL,Horenstein NA

更新日期：2007-03-15 00:00:00

abstract：:Bruton's Tyrosine Kinase (BTK) is one of the crucial kinases for the B cell maturation and mast cell activation, and specific inhibitors of BTK are considered to be attractive targets in drug discovery research. In this Letter, we have designed and synthesized a new fluorescent probe for TR-FRET-based high-throughput ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Asami T,Kawahata W,Sawa M

更新日期：2015-01-01 00:00:00

abstract：:Compound 2 was previously identified as a potent inhibitor of factor XIa lacking oral bioavailability. A structure-based approach was used to design analogs of 2 with novel P1 moieties with good selectivity profiles and oral bioavailability. Further optimization of the P1 group led to the identification of a 4-chlorop...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pinto DJ,Smallheer JM,Corte JR,Austin EJ,Wang C,Fang T,Smith LM 2nd,Rossi KA,Rendina AR,Bozarth JM,Zhang G,Wei A,Ramamurthy V,Sheriff S,Myers JE Jr,Morin PE,Luettgen JM,Seiffert DA,Quan ML,Wexler RR

更新日期：2015-04-01 00:00:00

abstract：:Novel, low brain penetrant, orally bioavailable CB1 receptor agonists were designed starting from a mature lead series of potent brain penetrant CB1 receptor agonists. Increasing the calculated polar surface area was found to be a good strategy for reducing brain penetration whilst retaining drug-like properties. This...

journal_title：Bioorganic & medicinal chemistry letters

authors： Adam JM,Clark JK,Davies K,Everett K,Fields R,Francis S,Jeremiah F,Kiyoi T,Maidment M,Morrison A,Ratcliffe P,Prosser A,Schulz J,Wishart G,Baker J,Boyce S,Campbell R,Cottney JE,Deehan M,Martin I

更新日期：2012-04-15 00:00:00

abstract：:The reaction mechanisms of hypochlorous acid (HOCl) with several tryptophan and tryptamine derivatives, previously reported to scavenge this powerful oxidant, was investigated to determine whether ionic or radical pathways were involved. For this purpose, the reaction of tryptamine and tryptophan derivatives with HOCl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Carvalho LC,Estevão MS,Ferreira LM,Fernandes E,Marques MM

更新日期：2010-11-15 00:00:00

abstract：:We designed and synthesized novel δ opioid receptor (DOR) agonists 3a-i with an azatricyclodecane skeleton, which was a novel structural class of DOR agonists. Among them, 3b exhibited high values of binding affinity and potent agonistic activity for the DOR that were approximately equivalent to those of 2 which bore ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Watanabe Y,Hayashida K,Saito D,Takahashi T,Sakai J,Nakata E,Kanda T,Iwai T,Hirayama S,Fujii H,Yamakawa T,Nagase H

更新日期：2017-08-01 00:00:00

abstract：:Twenty-six new hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes having a seven-membered ring structure between a bidentate carrier ligand and a platinum atom have been synthesized and most of them were evaluated for their in vitro cytotoxicity toward A549 human non-small cell lung carcinoma and HC...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu H,Cui K,Wang L,Gou S

更新日期：2005-11-15 00:00:00

abstract：:Amiodarone (Cordarone, Wyeth-Ayerst Pharmaceuticals) is a clinically available drug used to treat a wide variety of cardiac arrhythmias. We report here the synthesis and characterization of a panel of potential amiodarone metabolites that have significant structural similarity to thyroid hormone and its metabolites th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Snead AN,Miyakawa M,Tan ES,Scanlan TS

更新日期：2008-11-15 00:00:00

abstract：:Novel dihydroalkoxybenzyloxopyrimidine (S-DABO) derivatives targeting the non-nucleoside inhibitor (NNI) binding site of human immunodeficiency virus (HIV) reverse transcriptase (RT) have been synthesized using a novel computer model for the NNI binding pocket and tested for their RT inhibitory activity in cell-free a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vig R,Mao C,Venkatachalam TK,Tuel-Ahlgren L,Sudbeck EA,Uckun FM

更新日期：1998-06-16 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：:Practical, asymmetric total syntheses of the title phospholipids from a readily available myo-inositol derivative as well as short chain and cross-linkable aminoether analogues are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Falck JR,Krishna UM,Capdevila JH

更新日期：2000-08-07 00:00:00

abstract：:Small molecule JAK inhibitors have been demonstrated efficacy in rheumatoid arthritis, inflammatory bowel disease, and psoriasis with the approval of several drugs. Aiming to develop potent JAK1/2 inhibitors, two series of triazolo [1,5-a] pyridine derivatives were designed and synthesized by various strategies. The p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lu K,Wu W,Zhang C,Liu Z,Xiao B,Yuan Z,Li A,Chen D,Zhai X,Jiang Y

更新日期：2020-07-15 00:00:00

abstract：:Pyrido[1,2-a]indole-1,4-diones and benzo[f]pyrido[1,2-a]indole-6,11-diones were synthesized and tested for in vitro antifungal activity against two pathogenic strains of fungi. Among them tested, many compounds showed good antifungal activity. The results suggest that pyrido[1,2-a]indole-1,4-diones and benzo[f]pyrido[...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ryu CK,Yoon JH,Song AL,Im HA,Kim JY,Kim A

更新日期：2012-01-01 00:00:00

abstract：:In the present study, an efficient synthesis of some Mannich base of 5-methyl-2-[(2-oxo-2H-chromen-3-yl)carbonyl]-2,4-dihydro-3H-pyrazol-3-one (4a-j) have been described by using conventional and non-conventional (microwave) techniques. Microwave assisted reactions showed that require shorter reaction time and good yi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sivakumar KK,Rajasekaran A,Senthilkumar P,Wattamwar PP

更新日期：2014-07-01 00:00:00

abstract：:The synthesis of six α,β,-unsaturated amides and six 2,4-disubstituted oxazolines derivatives and their evaluation against two Mycobacterium tuberculosis strains (sensitive H37Rv and a resistant clinical isolate) is reported. 2,4-Disubstituted oxazolines (S)-3b,d,e were the most active in the sensitive strain with a M...

journal_title：Bioorganic & medicinal chemistry letters

authors： Avalos-Alanís FG,Hernández-Fernández E,Carranza-Rosales P,López-Cortina S,Hernández-Fernández J,Ordóñez M,Guzmán-Delgado NE,Morales-Vargas A,Velázquez-Moreno VM,Santiago-Mauricio MG

更新日期：2017-02-15 00:00:00

abstract：:Novel indole-3-heterocycles were designed and synthesized and found to be potent CB1 receptor agonists. Starting from a microsomally unstable lead 1, a bioisostere approach replacing a piperazine amide was undertaken. This was found to be a good strategy for improving stability both in vitro and in vivo. This led to t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morrison AJ,Adam JM,Baker JA,Campbell RA,Clark JK,Cottney JE,Deehan M,Easson AM,Fields R,Francis S,Jeremiah F,Keddie N,Kiyoi T,McArthur DR,Meyer K,Ratcliffe PD,Schulz J,Wishart G,Yoshiizumi K

更新日期：2011-01-01 00:00:00

abstract：:Scavenger receptor A (SRA) has been implicated in the processes of tumor invasion and acts as an immunosuppressor during therapeutic cancer vaccination. Pharmacological inhibition of SRA function thus holds a great potential to improve treatment outcome of cancer therapy. Macromolecular natural product sennoside B was...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yuan Y,Li X,Zaidi SA,Arnatt CK,Yu X,Guo C,Wang XY,Zhang Y

更新日期：2015-08-15 00:00:00

abstract：:Two series of aminosubstituted coumarins were synthesised and evaluated in vitro as inhibitors of DNA gyrase and as potential antibacterials. Novel novobiocin-like coumarins, 4-(dialkylamino)methylcoumarins and 4-((2-alkylamino)ethoxy)coumarins, were discovered as gyrase B inhibitors with promising antibacterial activ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Laurin P,Ferroud D,Schio L,Klich M,Dupuis-Hamelin C,Mauvais P,Lassaigne P,Bonnefoy A,Musicki B

更新日期：1999-10-04 00:00:00

abstract：:The synthesis and receptor binding of novel adenosine receptor antagonists is described. We found that non-xanthine 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives may have high affinity and substantial selectivity for the adenosine A(1) receptor. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： van Tilburg EW,van der Klein PA,de Groote M,Beukers MW,IJzerman AP

更新日期：2001-08-06 00:00:00

abstract：:Structure- and ligand-based virtual-screening methods (docking, 2D- and 3D-similarity searching) were analyzed for their effectiveness in virtual screening against FFAR2. To evaluate the performance of these methods, retrospective virtual screening was performed. Statistical quality of the methods was evaluated by BED...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fells JI,Ai X,Weinglass A,Feng W,Lei Y,Finley M,Hoveyda HR,Fraser GL,Machacek M

更新日期：2020-11-01 00:00:00

abstract：:A series of 1H-1,2,3-triazole/acylhydrazide-tethered tetrahydro-β-carboline-4-aminoquinoline conjugates was synthesized with an aim to study their anti-plasmodial structure-activity relationship. The presence of 1H-1,2,3-triazole-core along with a flexible alkyl chain length on aminoquinoline core has favourable influ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharma B,Kaur S,Legac J,Rosenthal PJ,Kumar V

更新日期：2020-01-15 00:00:00