- Neuroprotective effects of furopyrazole derivative of benzylindazole analogs on C2 ceramide-induced apoptosis in cultured cortical neurons
[作者:Lin, YC; Chou, LC; Chen, SC; Kuo, SC; Huang, LJ; Gean, PW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3225-3228 , 文章类型: Article,,卷期:2009年19-12]
- Ceramide accumulation in neurons during various disorders is associated with acute and chronic neurodegeneration. Here we investigate the neuroprotective effects of furopyrazole derivative of benzylindazole analogs on C2...
- Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: Design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition
[作者:Capela, R; Oliveira, R; Goncalves, LM; Domingos, A; Gut, J; Rosenthal, PJ; Lopes, F; Moreira, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3229-3232 , 文章类型: Article,,卷期:2009年19-12]
- A series of artemisinin-vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened for antiplasmodial activity ...
- Selective cytochrome P450 3A4 inhibitory activity of Amaryllidaceae alkaloids
[作者:McNulty, J; Nair, JJ; Singh, M; Crankshaw, DJ; Holloway, AC; Bastida, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3233-3237 , 文章类型: Article,,卷期:2009年19-12]
- A library of natural and semi-synthetic Amaryllidaceae alkaloids was screened for cytochrome P450 3A4 (CYP3A4) inhibitory activity. Of the crinane, lycorane and galanthamine representatives examined two semi-synthetic si...
- Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)
[作者:Lin, SN; Lombardo, M; Malkani, S; Hale, JJ; Mills, SG; Chapman, K; Thompson, JE; Zhang, WX; Wang, RX; Cubbon, RM; O'Neill, EA; Luell, S; Carballo-Jane, E; Yang, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3238-3242 , 文章类型: Article,,卷期:2009年19-12]
- Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas are described as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). These compounds demonstrate potent in vitro activity against the enzyme w...
- Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition
[作者:Verheijen, JC; Wiig, KA; Du, SC; Connors, SL; Martin, AN; Ferreira, JP; Slepnev, VI; Kochendorfer, U,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3243-3246 , 文章类型: Article,,卷期:2009年19-12]
- Conjugation of the phenol derived from rivastigmine with amphetamines gave access to novel carbamate cholinesterase inhibitors. All compounds possessed increased affinity and selectivity for AChE compared to rivastigmine...
- Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle
[作者:Pfefferkorn, JA; Lou, JH; Minich, ML; Filipski, KJ; He, MY; Zhou, R; Ahmed, S; Benbow, J; Perez, AG; Tu, MH; Litchfield, J; Sharma, R; Metzler, K; Bourbonais, F; Huang, C; Beebe, DA; Oates, PJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3247-3252 , 文章类型: Article,,卷期:2009年19-12]
- A promising area of novel anti-diabetic therapy involves identification of small molecule activators of the glucokinase enzyme to reduce blood glucose and normalize glucose stimulated insulin secretion. Herein, we report...
- Sulfoximine-substituted trifluoromethylpyrimidine analogs as inhibitors of proline-rich tyrosine kinase 2 (PYK2) show reduced hERG activity
[作者:Walker, DP; Zawistoski, MP; McGlynn, MA; Li, JC; Kung, DW; Bonnette, PC; Baumann, A; Buckbinder, L; Houser, JA; Boer, J; Mistry, A; Han, S; Xing, L; Guzman-Perez, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3253-3258 , 文章类型: Article,,卷期:2009年19-12]
- The synthesis, in vitro properties, and in vivo pharmacokinetics for a series of sulfoximine-substituted trifluoromethylpyrimidines as inhibitors of proline-rich tyrosine kinase, a target for the possible treatment of os...
- A new series of 3-phenylcoumarins as potent and selective MAO-B inhibitors
[作者:Matos, MJ; Vina, D; Quezada, E; Picciau, C; Delogu, G; Orallo, F; Santana, L; Uriarte, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3268-3270 , 文章类型: Article,,卷期:2009年19-12]
- 6-Methyl-3-phenylcoumarins 3-6 were designed, synthesized and evaluated as monoamine oxidase A and B (MAO-A and MAO-B) inhibitors. The synthesis of these new compounds (resveratrol-coumarin hybrids) was carried out with ...
- The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives
[作者:Walters, MJ; Blobaum, AL; Kingsley, PJ; Felts, AS; Sulikowski, GA; Marnett, LJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3271-3274 , 文章类型: Article,,卷期:2009年19-12]
- Sulindac sulfide is a benzylidene-indene that is a potent, time-dependent inhibitor of cyclooxygenases-1 and -2. Removal of the 2'-methyl group from the indene ring dramatically reduces time-dependent inhibition of both ...
- Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator
[作者:Ritzen, A; Sindet, R; Hentzer, M; Svendsen, N; Brodbeck, RM; Bundgaard, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3275-3278 , 文章类型: Article,,卷期:2009年19-12]
- This Letter describes the discovery of a novel series of mGluR5 positive allosteric modulators (PAMs). The lead compound, 11c, exhibits excellent potency (EC50 = 30 nM) in vitro, and reaches high brain levels in both rat...
- Inhibitory effect of a dimerization-arm-mimetic peptide on EGF receptor activation
[作者:Mizuguchi, T; Uchimura, H; Kakizawa, T; Kimura, T; Yokoyama, S; Kiso, Y; Saito, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3279-3282 , 文章类型: Article,,卷期:2009年19-12]
- A cyclic decapeptide was chemically synthesized that mimics the loop structure of a beta-hairpin arm of the EGF receptor, which is highly involved in receptor dimerization upon activation by ligand binding. This peptide ...
- Design, synthesis and biological evaluation of novel substituted benzoylguanidine derivatives as potent Na+/H+ exchanger inhibitors
[作者:Xu, WT; Jin, N; Xu, J; Xu, YG; Wang, QJ; You, QD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3283-3287 , 文章类型: Article,,卷期:2009年19-12]
- A novel series of substituted benzoylguanidine derivatives were designed and synthesized as potent NHE1 inhibitors. Most compounds can significantly inhibit NHE1-mediated platelet swelling in a concentration-dependent ma...
- Functional expression of the Aspergillus flavus PKS-NRPS hybrid CpaA involved in the biosynthesis of cyclopiazonic acid
[作者:Seshime, Y; Juvvadi, PR; Tokuoka, M; Koyama, Y; Kitamoto, K; Ebizuka, Y; Fujii, I,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3288-3292 , 文章类型: Article,,卷期:2009年19-12]
- alpha-Cyclopiazonic acid (CPA) is an indole tetramic acid mycotoxin. Based on our identification of the polyketide synthase-nonribosomal peptide synthase (PKS-NRPS) hybrid gene cpaA involved in cyclopiazonic acid biosynt...
- Total synthesis and evaluation of 22-(3-azidobenzoyloxy)methyl epothilone C for photoaffinity labeling of beta-tubulin
[作者:Hutt, OE; Inagaki, J; Reddy, BS; Nair, SK; Reiff, EA; Henri, JT; Greiner, JF; VanderVelde, DG; Chiu, TL; Amin, EA; Himes, RH; Georg, GI,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3293-3296 , 文章类型: Article,,卷期:2009年19-12]
- The total synthesis of 22-(3-azidobenzoyloxy)methyl epothilone C is described as a potential photoaffinity probe to elucidate the beta-tubulin binding site. A sequential Suzuki-aldol-Yamaguchi macrolactonization strategy...
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