(+)-4-phosphonophenylglycine (PPG) a new group III selective metabotropic glutamate receptor agonist.


:A new synthesis of (R,S)-PPG (4-phosphonophenylglycine) and the separation of the protected enantiomers leading after deprotection to (+)- and (-)-PPG are described. Pharmacological characterization at the group III metabotropic glutamate receptors hmGluR4a and hmGluR7b revealed (+)-PPG as the active enantiomer.


Bioorg Med Chem Lett


Gasparini F,Inderbitzin W,Francotte E,Lecis G,Richert P,Dragic Z,Kuhn R,Flor PJ




Has Abstract


2000-06-05 00:00:00














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    abstract::3-(N-Alkyl)aminopropylphosphonic acids are potent agonists of four of the five known sphingosine-1-phosphate (S1P) receptor subtypes. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Hale JJ,Doherty G,Toth L,Li Z,Mills SG,Hajdu R,Ann Keohane C,Rosenbach M,Milligan J,Shei GJ,Chrebet G,Bergstrom J,Card D,Rosen H,Mandala S

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  • Identification of an indole series of prostaglandin D2 receptor antagonists.

    abstract::A novel indole series of PGD2 receptor (DP receptor) antagonists is presented. Optimization of this series led to the identification of potent and selective DP receptor antagonists. In particular, antagonists 35 and 36 were identified with Ki values of 2.6 and 1.8 nM, respectively. These two antagonists are also poten...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Sturino CF,Lachance N,Boyd M,Berthelette C,Labelle M,Li L,Roy B,Scheigetz J,Tsou N,Brideau C,Cauchon E,Carriere MC,Denis D,Greig G,Kargman S,Lamontagne S,Mathieu MC,Sawyer N,Slipetz D,O'Neill G,Wang Z,Zamboni R

    更新日期:2006-06-01 00:00:00

  • The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14.

    abstract::A weak, UDP-competitive antagonist of the pyrimidinergic receptor P2RY(14) with a naphthoic acid core was identified through high-throughput screening. Optimization provided compounds with improved potency but poor pharmacokinetics. Acylglucuronidation was determined to be the major route of metabolism. Increasing the...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Gauthier JY,Belley M,Deschênes D,Fournier JF,Gagné S,Gareau Y,Hamel M,Hénault M,Hyjazie H,Kargman S,Lavallée G,Levesque JF,Li L,Mamane Y,Mancini J,Morin N,Mulrooney E,Robichaud J,Thérien M,Tranmer G,Wang Z,Wu J

    更新日期:2011-05-15 00:00:00

  • Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.

    abstract::Millettia pachycarpa Benth, a widely used anthelminthic drug in folk, is rich in flavonoids with various bioactivities. This study aimed to identify active flavonoids with anti-Alzheimer's disease (AD) effect from its seeds by a bioassay-guided isolation. A novel rotenoid with unusual oxidative ring-opening skeleton (...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Tu Y,Wu C,Kang Y,Li Q,Zhu C,Li Y

    更新日期:2019-05-15 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Tsou LK,Dutschman GE,Gullen EA,Telpoukhovskaia M,Cheng YC,Hamilton AD

    更新日期:2010-04-01 00:00:00

  • Novel targeting strategy based on multimeric ligands for drug delivery and molecular imaging: homooligomers of alpha-MSH.

    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

    pub_type: 杂志文章


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

    更新日期:2004-01-05 00:00:00

  • A new class of potent RAR antagonists: dihydroanthracenyl, benzochromenyl and benzothiochromenyl retinoids.

    abstract::The synthesis and biological activity of a novel series of tricyclic retinoic acid receptor antagonists are described. These compounds bind with high affinity to the RARs and are potent antagonists of retinoid function in in vitro and in vivo systems. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Vuligonda V,Standeven AM,Escobar M,Chandraratna RA

    更新日期:1999-03-08 00:00:00

  • Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1.

    abstract::A series of novel 5-trans-hydroxyadamantan-2-yl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-ones that inhibit 11beta-hydroxysteroid dehydrogenase type 1 are described. We discovered these 7-membered cyclic amide derivatives by introducing a distinctive linker through pharmacophore analysis of known ligands included ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Udagawa S,Sakami S,Takemura T,Sato M,Arai T,Nitta A,Aoki T,Kawai K,Iwamura T,Okazaki S,Takahashi T,Kaino M

    更新日期:2013-03-15 00:00:00

  • Macrocarpins A-D, new cytotoxic nor-triterpenes from Maytenus macrocarpa.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Chávez H,Rodríguez G,Estévez-Braun A,Ravelo AG,Estévez-Reyes R,González AG,Fdez-Puente JL,García-Grávalos D

    更新日期:2000-04-17 00:00:00

  • Identification of fragments targeting an alternative pocket on HIV-1 gp41 by NMR screening and similarity searching.

    abstract::The HIV-1 envelope glycoprotein gp41 fusion intermediate is a promising drug target for inhibiting viral entry. However, drug development has been impeded by challenges inherent in mediating the underlying protein-protein interaction. Here we report on the identification of fragments that bind to a C-terminal sub-pock...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Chu S,Gochin M

    更新日期:2013-09-15 00:00:00

  • Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Giannini G,Battistuzzi G,Vesci L,Milazzo FM,De Paolis F,Barbarino M,Guglielmi MB,Carollo V,Gallo G,Artali R,Dallavalle S

    更新日期:2014-01-15 00:00:00

  • A dual fluorinated and iodinated radiotracer for PET and SPECT imaging of β-amyloid plaques in the brain.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    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

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Kannan T,Vinodhkumar S,Varghese B,Loganathan D

    更新日期:2001-09-17 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Anthony Romero F,Hastings NB,Moningka R,Guo Z,Wang M,Di Salvo J,Lei Y,Trusca D,Deng Q,Tong V,Terebetski JL,Ball RG,Ujjainwalla F

    更新日期:2012-01-15 00:00:00

  • Toxocara canis: Larvicidal activity of fatty acid amides.

    abstract::Considering the therapeutic potential of fatty acid amides, the present study aimed to evaluate their in vitro activity against Toxocara canis larvae and their cytotoxicity for the first time. Linoleylpyrrolidilamide was the most potent, with a minimal larvicidal concentration (MLC) of 0.05 mg/mL and 27% cytotoxicity ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Mata-Santos T,D'Oca CDRM,Mata-Santos HA,Fenalti J,Pinto N,Coelho T,Berne ME,da Silva PEA,D'Oca MGM,Scaini CJ

    更新日期:2016-02-01 00:00:00

  • Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes.

    abstract::TGR5 is a member of G protein-coupled receptor (GPCR) superfamily, a promising molecular target for metabolic diseases. Activation of TGR5 promotes secretion of glucagon-like peptide-1 (GLP-1), which activates insulin secretion. A series of 2-thio-imidazole derivatives have been identified as novel, potent and orally ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Agarwal S,Sasane S,Kumar J,Deshmukh P,Bhayani H,Giri P,Giri S,Soman S,Kulkarni N,Jain M

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  • Discovery of a novel azetidine scaffold for colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors by the use of docking models.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Ikegashira K,Ikenogami T,Yamasaki T,Hase Y,Yamaguchi T,Inagaki K,Doi S,Adachi T,Koga Y,Hashimoto H

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  • Flavonoids: structural requirements for antiproliferative activity on breast cancer cells.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Pouget C,Lauthier F,Simon A,Fagnere C,Basly JP,Delage C,Chulia AJ

    更新日期:2001-12-17 00:00:00

  • Inhibitors for expression of IgE receptor on human mast cell from Puerariae Flos.

    abstract::Bioassay-guided separation of the extract of the medicinal plant, Puerariae Flos, disclosed the two isoflavones tectorigenin (1) and genistein (2) as the inhibitors for expression of IgE receptor (FcepsilonRI), the key molecule triggering the allergic reactions, on human mast cells. As a result of analysis of structur...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Tamura S,Yoshihira K,Tokumaru M,Zisheng X,Murakami N

    更新日期:2010-07-01 00:00:00

  • Syntheses and antifilarial profile of 7-chloro-4-(substituted amino) quinolines: a new class of antifilarial agents.

    abstract::The syntheses of 7-chloro-4-(substituted amino) quinolines (2-22) and their antifilarial activities are delineated. Some of the screened compounds have shown promising filarial response and sterilization effect on female Acanthocheilonema viteae in rodents. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Tewari S,Chauhan PM,Bhaduri AP,Fatima N,Chatterjee RK

    更新日期:2000-07-03 00:00:00

  • 4-Substituted (benzo[b]thiophene-2-carbonyl)guanidines as novel Na+/H+ exchanger isoform-1 (NHE-1) inhibitors.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Lee S,Lee H,Yi KY,Lee BH,Yoo SE,Lee K,Cho NS

    更新日期:2005-06-15 00:00:00

  • In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.

    abstract::Structure-activity relationships (SAR) were analyzed within a library of diverse yet simple compounds prepared as histamine H3 antagonists. The libraries were constructed with a variety of low molecular weight pyrrolidines, selected from (R)-2-methylpyrrolidine, (S)-2-methylpyrrolidine, and pyrrolidine. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Nersesian DL,Black LA,Miller TR,Vortherms TA,Esbenshade TA,Hancock AA,Cowart MD

    更新日期:2008-01-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Augustyn E,Finke K,Zur AA,Hansen L,Heeren N,Chien HC,Lin L,Giacomini KM,Colas C,Schlessinger A,Thomas AA

    更新日期:2016-06-01 00:00:00

  • Design, synthesis, and analysis of antagonists of GPR55: Piperidine-substituted 1,3,4-oxadiazol-2-ones.

    abstract::A series of 1,3,4-oxadiazol-2-ones was synthesized and tested for activity as antagonists at GPR55 in cellular beta-arrestin redistribution assays. The synthesis was designed to be modular in nature so that a sufficient number of analogues could be rapidly accessed to explore initial structure-activity relationships. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Meza-Aviña ME,Lingerfelt MA,Console-Bram LM,Gamage TF,Sharir H,Gettys KE,Hurst DP,Kotsikorou E,Shore DM,Caron MG,Rao N,Barak LS,Abood ME,Reggio PH,Croatt MP

    更新日期:2016-04-01 00:00:00

  • 99mTc/Re complexes based on flavone and aurone as SPECT probes for imaging cerebral β-amyloid plaques.

    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

    pub_type: 杂志文章


    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

  • Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists.

    abstract::The synthesis and biological evaluation of new potent opioid receptor-like 1 antagonists are presented. A structure-activity relationship (SAR) study of arylpyrazole lead compound 1 obtained from library screening identified compound 31, (1S,3R)-N-{[1-(3-chloropyridin-2-yl)-5-(5-fluoro-6-methylpyridin-3-yl)-4-methyl-1...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Kobayashi K,Uchiyama M,Ito H,Takahashi H,Yoshizumi T,Sakoh H,Nagatomi Y,Asai M,Miyazoe H,Tsujita T,Hirayama M,Ozaki S,Tani T,Ishii Y,Ohta H,Okamoto O

    更新日期:2009-07-01 00:00:00

  • Poly-guanidinoethylphenylethers organised around a benzene ring: synthesis and evaluation of their antibacterial and cytotoxic properties.

    abstract::A new family of poly-guanidinium species with a benzene core as the organising agent has been developed. Their antibacterial properties have been evaluated against reference Gram positive and Gram negative bacteria, and their cytotoxicity against eukaryotic cells. Most of these compounds exhibited Minimum Inhibitory C...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Massimba Dibama H,Mourer M,Duval RE,Regnouf-de-Vains JB

    更新日期:2014-10-15 00:00:00

  • Fluorine-18 labeled galactosylated chitosan for asialoglycoprotein-receptor-mediated hepatocyte imaging.

    abstract::Galactosylated chitosan (GC) was prepared by reacting lactobionic acid with water-soluble chitosan. GC was labeled with fluorine-18 by conjugation with N-succinimidyl-4-(18)F-fluorobenzoate ([(18)F]SFB) under a slightly basic condition. After rapid purification with HiTrap desalting column, [(18)F]FB-GC was obtained w...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Yang W,Mou T,Guo W,Jing H,Peng C,Zhang X,Ma Y,Liu B

    更新日期:2010-08-15 00:00:00

  • Folic acid conjugates of a bleomycin mimic for selective targeting of folate receptor positive cancer cells.

    abstract::A major challenge in the application of cytotoxic anti-cancer drugs is their general lack of selectivity, which often leads to systematic toxicity due to their inability to discriminate between malignant and healthy cells. A particularly promising target for selective targeting are the folate receptors (FR) that are o...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Geersing A,de Vries RH,Jansen G,Rots MG,Roelfes G

    更新日期:2019-08-01 00:00:00

  • Discovery of novel nonsteroidal glucocorticoid receptor modulators.

    abstract::A new class of selective nonsteroidal glucocorticoid receptor modulators typified by N-[3-[benzyl-(4-chloro-2-fluoro-benzyl)-amino]-2-methyl-phenyl]-methanesulfonamide 19 has been discovered. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Link JT,Sorensen BK,Patel J,Emery M,Grynfarb M,Goos-Nilsson A

    更新日期:2004-05-03 00:00:00