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Journal of Medicinal Chemistry

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  1. Conformationally constrained analogues of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716): design, synthesis, computational analysis, and biological evaluations.

    Journal of Medicinal Chemistry 51(12):3526 (2008) PMID 18512901

    Structure-activity relationships (SARs) of 1 (SR141716) have been extensively documented, however, the conformational properties of this class have received less attention. In an attempt to better understand ligand conformations optimal for receptor recognition, we have designed and synthesized ...
  2. Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.

    Journal of Medicinal Chemistry 51(12):3422 (2008) PMID 18507371

    The coagulation enzyme factor Xa (FXa) has been recognized as a promising target for the development of new antithrombotic agents. We previously found compound 1 to be an orally bioavailable FXa inhibitor in fasted monkeys; however, 1 showed poor bioavailability in rats and fed monkeys. To work ...
  3. DNA interactions of monofunctional organometallic osmium(II) antitumor complexes in cell-free media.

    Journal of Medicinal Chemistry 51(12):3635 (2008) PMID 18494458

    This work is the first in-depth study of osmium binding to DNA and confirms the pharmacological activity of a new class of anticancer metallodrugs. We investigated the interactions between the potential biological target DNA and four osmium(II) arene complexes, of the type [(eta 6-arene)Os(LL)Cl...
  4. Flavonoids for controlling starch digestion: structural requirements for inhibiting human alpha-amylase.

    Journal of Medicinal Chemistry 51(12):3555 (2008) PMID 18507367

    In this study we investigated the structural requirements for inhibition of human salivary alpha-amylase by flavonoids. Four flavonols and three flavones, out of the 19 flavonoids tested, exhibited IC50 values less than 100 microM against human salivary alpha-amylase activity. Structure-activity...
  5. Chemically induced dimerization of human nonpancreatic secretory phospholipase A2 by bis-indole derivatives.

    Journal of Medicinal Chemistry 51(12):3360 (2008) PMID 18522384

    A series of novel bis-indole compounds, 1,omega-bis(((3-acetamino-5-methoxy-2-methylindole)-2-methylene)phenoxy)alkane, have been designed and synthesized on the basis of the enzyme structure of human nonpancreatic secretory phospholipase A2 (hnps PLA2). Their inhibition activities against hnps ...
  6. Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.

    Journal of Medicinal Chemistry 51(12):3588 (2008) PMID 18517184

    A novel series of donepezil-tacrine hybrids designed to simultaneously interact with the active, peripheral and midgorge binding sites of acetylcholinesterase (AChE) have been synthesized and tested for their ability to inhibit AChE, butyrylcholinesterase (BChE), and AChE-induced A beta aggregat...
  7. Identification of MMP-12 inhibitors by using biosensor-based screening of a fragment library.

    Journal of Medicinal Chemistry 51(12):3449 (2008) PMID 18494455

    Small inhibitors of matrix metalloproteinase 12 (MMP-12) have been identified with a biosensor-based screening strategy and a specifically designed fragment library. The interaction between fragments and three variants of the target and a reference protein with an active-site zinc ion was measur...
  8. New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities.

    Journal of Medicinal Chemistry 51(12):3414 (2008) PMID 18503262

    A series of 5-alkylindolobenzazepin-7-ones was synthesized by Suzuki coupling between 3-iodoindole-2-carboxylates and the appropriate alpha-alkylbenzylamino o-boronic acids followed by cyclization to the lactam. Derivatives having a linear alkyl chain at C5 were found to be highly cytotoxic to K...
  9. Crystal structure of the oxazolidinone antibiotic linezolid bound to the 50S ribosomal subunit.

    Journal of Medicinal Chemistry 51(12):3353 (2008) PMID 18494460

    The oxazolidinone antibacterials target the 50S subunit of prokaryotic ribosomes. To gain insight into their mechanism of action, the crystal structure of the canonical oxazolidinone, linezolid, has been determined bound to the Haloarcula marismortui 50S subunit. Linezolid binds the 50S A-site, ...
  10. Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.

    Journal of Medicinal Chemistry 51(12):3487 (2008) PMID 18507372 PMCID PMC3744893

    Alkylcarbamic acid biphenyl-3-yl esters are a class of fatty acid amide hydrolase (FAAH) inhibitors that comprises cyclohexylcarbamic acid 3'-carbamoylbiphenyl-3-yl ester (URB597), a compound with analgesic, anxiolytic-like and antidepressant-like properties in rat and mouse models. Here, we ext...