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Bioorganic & Medicinal Chemistry

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  1. Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines

    Bioorganic & Medicinal Chemistry 22(23):6638 (2014)

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  2. An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB in...

    Bioorganic & Medicinal Chemistry 22(23):6552 (2014)

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  3. The effect of C(5) cytosine methylation at CpG sequences on mitomycin-DNA bonding profiles.

    Bioorganic & Medicinal Chemistry 9(4):863 (2001) PMID 11354669

    We have determined the bonding profiles for mitomycin monoalkylation in two DNA restriction fragments where the CpG sequences were methylated. Three mitomycin substrates were used and two different enzymatic assays employed to monitor the extent of drug modification at the individual base sites. Dru...
  4. TRH mimetics: differentiation of antiamnesic potency from antidepressant effect.

    Bioorganic & Medicinal Chemistry 5(11):2029 (1997) PMID 9416420

    We were pursuing an approach that consists of two steps: (1) 'obligatory' replacement of histidine with glutamine in TRH and (2) the application of conformational constraints for putative bioactive conformation I stabilized by an intramolecular hydrogen bond between C-terminal carboxamide proton and...
  5. Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping

    Bioorganic & Medicinal Chemistry 22(21):6256 (2014)

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  6. Synthesis of IB-01212 by multiple N-methylations of peptide bonds

    Bioorganic & Medicinal Chemistry 22(21):6156 (2014)

  7. Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonis...

    Bioorganic & Medicinal Chemistry 22(21):6026 (2014)

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  8. Human α1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines

    Bioorganic & Medicinal Chemistry 22(21):5910 (2014)

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  9. Regio- and stereoselective hydroxylation of 10-undecenoic acid with a light-driven P450 BM3 biocatalyst yielding a valuable synthon for natu...

    Bioorganic & Medicinal Chemistry 22(20):5687 (2014) PMID 24938497 PMCID PMC4182142

    We report herein the selective hydroxylation of 10-undecenoic acid with a light-activated hybrid P450 BM3 enzyme. Under previously developed photocatalytic reaction conditions, only a monohydroxylated product is detected by gas chromatography. Hydroxylation occurs exclusively at the allylic position...
  10. Synthesis of fluorinated agonist of sphingosine-1-phosphate receptor 1.

    Bioorganic & Medicinal Chemistry 22(17):4955 (2014) PMID 25047939

    The bioactive metabolite sphingosine-1-phosphate (S1P), a product of sphingosine kinases (SphKs), mediates diverse biological processes such as cell differentiation, proliferation, survival and angiogenesis. A fluorinated analogue of S1P receptor agonist has been synthesized by utilizing a ring open...