- Docking and SAR studies of salacinol derivatives as alpha-glucosidase inhibitors
[作者：Nakamura, S; Takahira, K; Tanabe, G; Morikawa, T; Sakano, M; Ninomiya, K; Yoshikawa, M; Muraoka, O; Nakanishi, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4420-4423 , 文章类型： Article，,卷期：2010年20-15]
- Salacinol is a potent alpha-glucosidase inhibitor isolated from Salacia reticulata, and a good lead compound for an antidiabetic drug. It is essential to clarify the binding state of salacinol to alpha-glucosidase for ef...
- Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives
[作者：Mokale, SN; Shinde, SS; Elgire, RD; Sangshetti, JN; Shinde, DB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4424-4426 , 文章类型： Article，,卷期：2010年20-15]
- A series of 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives has been synthesized by condensation of thiourea, 5-(4-subtituted phenyl)-5-oxopentanoic acid and substituted aldehyde...
- 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: Selective Aurora A kinase inhibitors
[作者：Ando, R; Ikegami, H; Sakiyama, M; Ooike, S; Hayashi, M; Fujino, Y; Abe, D; Nakamura, H; Mishina, T; Kato, H; Iwase, Y; Tomozane, H; Morioka, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4709-4711 , 文章类型： Article，,卷期：2010年20-15]
- A new class of Aurora A kinase inhibitor was created by transforming 4-(5-methyl-3-pyrazoloamino)pyrimidine moiety of VX-680 to 3-cyano-6-(5-methyl-3pyrazoloamino)pyridine. Compound 6 exhibited a potent Aurora A kinase i...
- In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I
[作者：Revesz, L; Schlapbach, A; Aichholz, R; Feifel, R; Hawtin, S; Heng, R; Hiestand, P; Jahnke, W; Koch, G; Kroemer, M; Mobitz, H; Scheufler, C; Velcicky, J; Huppertz, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4715-4718 , 文章类型： Article，,卷期：2010年20-15]
- Pyrrolo[2,3-f]isoquinoline based amino acids, tetracyclic lactams and cyclic ketone analogues are described as novel MK2 inhibitors with IC50 as low as 5 nM and good selectivity profiles against a number of related kinas...
- In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II
[作者：Revesz, L; Schlapbach, A; Aichholz, R; Dawson, J; Feifel, R; Hawtin, S; Littlewood-Evans, A; Koch, G; Kroemer, M; Mobitz, H; Scheufler, C; Velcicky, J; Huppertz, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4719-4723 , 文章类型： Article，,卷期：2010年20-15]
- Spirocyclopropane- and spiroazetidine-substituted tetracycles 13D-E and 16A are described as orally active MK2 inhibitors. The spiroazetidine derivatives are potent MK2 inhibitors with IC50 <3 nM and inhibit the release ...
- Active site binding modes of dimeric phloroglucinols for HIV-1 reverse transcriptase, protease and integrase
[作者：Gupta, P; Kumar, R; Garg, P; Singh, IP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4427-4431 , 文章类型： Article，,卷期：2010年20-15]
- In a recent report on anti-HIV activity of dimeric phloroglucinol compounds, seven out of twenty one compounds were shown to possess good activity in HIV infected human CD4+ T cell line. The seven active compounds were d...
- Synthesis of highly functionalized 2,4-diaminoquinazolines as anticancer and anti-HIV agents
[作者：Yan, SJ; Zheng, H; Huang, C; Yan, YY; Lin, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4432-4435 , 文章类型： Article，,卷期：2010年20-15]
- Novel polyhalo 2,4-diaminoquinazolines 3a-3d were prepared by reacting polyhaloisophthalonitriles with guanidine carbonate under solvent-free conditions and in the absence of a catalyst with good yields (74-95%). A serie...
- Synthesis and pharmacological evaluation of aryl aminosulfonamide derivatives as potent 5-HT6 receptor antagonists
[作者：Nirogi, RVS; Daulatabad, AV; Parandhama, G; Mohammad, S; Sastri, KR; Shinde, AK; Dubey, PK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4440-4443 , 文章类型： Article，,卷期：2010年20-15]
- A series of novel aryl aminosulfonamides was designed and synthesized as 5-HT6 receptor ligands. Many compounds screened in a functional reporter gene based assay displayed potent antagonistic activity with Kb values in ...
- Derivatives of tetrahydroisoquinoline: Synthesis and initial evaluation of novel non-peptide antagonists of the alpha(IIb)beta(3)-integrin
[作者：Krysko, AA; Krysko, OL; Kabanova, TA; Andronati, SA; Kabanov, VM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4444-4446 , 文章类型： Article，,卷期：2010年20-15]
- The novel RGDF mimetics were synthesized with the use of 4-(1,2,3,4-tetrahydroisoquinoline-7-yl)amino- 4-oxobutyric or 5-(1,2,3,4-tetrahydroisoquinoline-7-yl)amino-5-oxopentanoic acids as a surrogate of Arg-Gly motif. Th...
- 2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors
[作者：Cai, JQ; Bennett, DJ; Rankovic, Z; Dempster, M; Fradera, X; Gillespie, J; Cumming, I; Finlay, W; Baugh, M; Boucharens, S; Bruin, J; Cameron, KS; Hamilton, W; Kerr, J; Kinghorn, E; McGarry, G; Robinson, J; Scullion, P; Uitdehaag, JCM; van Zeeland, M; Potin, D; Saniere, L; Fouquet, A; Chevallier, F; Deronzier, H; Dorleans, C; Nicolai, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4447-4450 , 文章类型： Article，,卷期：2010年20-15]
- Starting from previously disclosed equally potent cathepsin K and S inhibitor 4-propyl-6-(3-trifluoromethylphenyl) pyrimidine-2-carbonitrile 1, a novel 2-phenyl-9H-purine-6-carbonitrile scaffold was identified to provide...
- Petiolins J-M, prenylated acylphloroglucinols from Hypericum pseudopetiolatum var. kiusianum
[作者：Tanaka, N; Otani, M; Kashiwada, Y; Takaishi, Y; Shibazaki, A; Gonoi, T; Shiro, M; Kobayashi, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4451-4455 , 文章类型： Article，,卷期：2010年20-15]
- Four new prenylated acylphloroglucinols, petiolins J-M (1-4), were isolated from aerial parts of Hypericum pseudopetiolatum var. kiusianum, and the structures were elucidated by spectroscopic data and a single-crystal X-...
- Prostaglandin phospholipid conjugates with unusual biophysical and cytotoxic properties
[作者：Pedersen, PJ; Adolph, SK; Andresen, TL; Madsen, MW; Madsen, R; Clausen, MH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4456-4458 , 文章类型： Article，,卷期：2010年20-15]
- The synthesis of two secretory phospholipase A(2) IIA sensitive 15-deoxy-Delta(12,14)-prostaglandin J(2) phospholipid conjugates is described and their biophysical and biological properties are reported. The conjugates s...
- 6-(4 '-Aryloxy-phenyl)vinyl-1,2,4-trioxanes: A new series of orally active peroxides effective against multidrug-resistant Plasmodium yoelii in Swiss mice
[作者：Singh, C; Verma, VP; Naikade, NK; Singh, AS; Hassam, M; Puri, SK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4459-4463 , 文章类型： Article，,卷期：2010年20-15]
- A new series of 6-(4'-aryloxy-phenyl)vinyl-1,2,4-trioxanes 10a-d, 11a-d, and 12a-d have been synthesized and evaluated for their antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice by oral r...
- Synthesis of 2-(4-substituted benzyl-1,4-diazepan-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl)acetamides and their positive inotropic evaluation
[作者：Yang, K; Sun, LP; Liu, JY; Cui, X; Piao, HR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4464-4467 , 文章类型： Article，,卷期：2010年20-15]
- Herein we describe the discovery of compound 3g, a potent positive inotropic agent compared with the standard drug, milrinone. Compound 3g was developed from a series of 2-(4-substitutedbenzyl-1,4-diazepan- 1-yl)-N-(3,4-...
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