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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. 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...
  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. Homology modeling and site-directed mutagenesis to identify selective inhibitors of endothelin-converting enzyme-2.

    Journal of Medicinal Chemistry 51(12):3378 (2008) PMID 18507370 PMCID PMC2706147

    Endothelin-converting enzyme-2 (ECE-2), a member of M13 family of zinc metallopeptidases, has previously been shown to process a number of neuropeptides including those derived from prodynorphin, proenkephalin, proSAAS, and amyloid precursor protein. ECE-2, unlike ECE-1, exhibits restricted neur...
  5. Synthesis and biological evaluation of D-amino acid oxidase inhibitors.

    Journal of Medicinal Chemistry 51(12):3357 (2008) PMID 18507366

    D-amino acid oxidase (DAAO) catalyzes the oxidation of D-amino acids including d-serine, a full agonist at the glycine site of the NMDA receptor. A series of benzo[ d]isoxazol-3-ol derivatives were synthesized and evaluated as DAAO inhibitors. Among them, 5-chloro-benzo[ d]isoxazol-3-ol (CBIO) p...
  6. 16-Cyclopentadienyl tricarbonyl 99mTc 16-oxo-hexadecanoic acid: synthesis and evaluation of fatty acid metabolism in mouse myocardium.

    Journal of Medicinal Chemistry 51(12):3630 (2008) PMID 18503263

    We synthesized 16-cyclopentadienyl tricarbonyl 99mTc 16-oxo-hexadecanoic acid (99mTc-CpTT-16-oxo-HDA, 1) and investigated its potential as a radiotracer for evaluating fatty acid metabolism in myocardium. Radiotracer 1 was synthesized in 22.6 +/- 6.3% decay-corrected yield by a double ligand tra...
  7. Clavatadine A, a natural product with selective recognition and irreversible inhibition of factor XIa.

    Journal of Medicinal Chemistry 51(12):3583 (2008) PMID 18510371

    Bioassay-guided fractionation of a CH2Cl2/MeOH extract of the sponge Suberea clavata using the serine protease factor XIa to detect antithrombotic activity led to the isolation of the new marine natural products, clavatadines A and B. Clavatadines A and B inhibited factor XIa with IC50's of 1.3 ...
  8. 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, ...
  9. Synthesis, cytotoxicity, DNA interaction, and topoisomerase II inhibition properties of novel indeno[2,1-c]quinolin-7-one and indeno[1,2-c]isoquinolin-5,11-dione derivatives.

    Journal of Medicinal Chemistry 51(12):3617 (2008) PMID 18507368

    Indeno[2,1- c]quinolin-7-ones and 6 H-indeno[1,2- c]isoquinolin-5,11-diones, bearing two cationic aminoalkyl side chains, were synthesized and evaluated for DNA interaction, topoisomerases inhibition, and cytotoxicity against human cancer cell lines. They displayed strong interaction with DNA an...
  10. Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives.

    Journal of Medicinal Chemistry 51(12):3654 (2008) PMID 18476684

    3,7-Bis(dialkylamino)phenoxazinium salts were synthesized and evaluated for in vitro activities against Plasmodium falciparum, Trypanosoma cruzi, T. brucei rhodesiense, and Leishmania donovani. Notably, the compounds showed potent antiprotozoal activities, especially against P. falciparum and T....