journal of medicinal chemistry سال:2018 - دوره:61

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journal of medicinal chemistry
سال:2018 - دوره:61 - شماره:1

(+)-methyl (1 r, 2s)-2-{[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-mr200] derivatives as potent and selective sigma receptor ligands: stereochemistry and pharmacological properties - صفحه:372-384 7-phenoxy-substituted 3,4-dihydro-2h-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (ampa) receptors with nanomolar potency - صفحه:251-264 a dipolar cycloaddition reaction to access 6-methyl-4,5,6,7-tetrahydro-1h-[1,2,3]triazolo[4,5-c]pyridines enables the discovery synthesis and preclinical profiling of a p2x7 antagonist clinical candidate - صفحه:207-223 a stable heroin analogue that can serve as a vaccine hapten to induce antibodies that block the effects of heroin and its metabolites in rodents and that cross-react immunologically with related drugs of abuse - صفحه:329-343 alkylated piperazines and piperazine-azole hybrids as antifungal agents - صفحه:158-173 aniline-based inhibitors of influenza h1n1 virus acting on hemagglutinin-mediated fusion - صفحه:98-118 discovery of 7-[ 18 f]fluorotryptophan as a novel positron emission tomography (pet) probe for the visualization of tryptophan metabolism in vivo - صفحه:189-206 discovery of an orally bioavailable benzofuran analogue that serves as a β-amyloid aggregation inhibitor for the potential treatment of alzheimer's disease - صفحه:396-402 discovery of novel potent vegfr-2 inhibitors exerting significant antiproliferative activity against cancer cell lines - صفحه:140-157 extra sugar on vancomycin: new analogues for combating multidrug-resistant staphylococcus aureus and vancomycin-resistant enterococci - صفحه:286-304 from experiments to a fast easy-to-use computational methodology to predict human aldehyde oxidase selectivity and metabolic reactions - صفحه:360-371 from the promiscuous asenapine to potent fluorescent ligands acting at a series of aminergic g-protein-coupled receptors - صفحه:174-188 high in vivo stability of 64 cu-labeled cross-bridged chelators is a crucial factor in improved tumor imaging of rgd peptide conjugates - صفحه:385-395 inhibitors of hiv-1 attachment: the discovery and development of temsavir and its prodrug fostemsavir - صفحه:62-80 microbiota-host transgenomic metabolism, bioactive molecules from the inside - صفحه:47-61 mind your ears: a new antidote to aminoglycoside toxicity? - صفحه:81-83 novel terminal bipheny-based diapophytoene desaturases (crtn) inhibitors as anti-mrsa/visr/lrsa agents with reduced herg activity - صفحه:224-250 phenotypic optimization of urea-thiophene carboxamides to yield potent, well tolerated, and orally active protective agents against aminoglycoside-induced hearing loss - صفحه:84-97 recent advances in structure-based drug design targeting class a g protein-coupled receptors utilizing crystal structures and computational simulations - صفحه:1-46 structure-based design of 6-chloro-4-aminoquinazoline-2-carboxamide derivatives as potent and selective p21-activated kinase 4 (pak4) inhibitors - صفحه:265-285 structure-based design, synthesis, and in vivo antinociceptive effects of selective a 1 adenosine receptor agonists - صفحه:305-318 sulfonyl-containing boronate caps for optimization of biological properties of 99m tc(iii) radiotracers [ 99m tccl(cdo)(cdoh) 2 b-r] (cdoh 2 = cyclohexanedione dioxime) - صفحه:319-328 the design and development of a potent and selective novel diprolyl derivative that binds to the n-domain of angiotensin-i converting enzyme - صفحه:344-359 the magic of crystal structure-based inhibitor optimization: development of a butyrylcholinesterase inhibitor with picomolar affinity and in vivo activity - صفحه:119-139