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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共45条记录   Discovery of diphenylmethane analogs as anti-bovine diarrhea viral agents [作者：Hosoda, S; Aoyama, H; Goto, Y; Salim, MTA; Okamoto, M; Hashimoto, M; Baba, M; Hashimoto, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3157-3161 , 文章类型： Article，,卷期：2009年19-12] Based on antiviral screening of our diphenylmethane derivatives prepared as steroid substitutes, we identified a 1,1-diphenylcyclobutane analog (9) and two diethyldiphenylsilane analogs (12 and 13) as superior lead compo... Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors [作者：Zebardast, T; Zarghi, A; Daraie, B; Hedayati, M; Dadrass, OG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3162-3165 , 文章类型： Article，,卷期：2009年19-12] A new group of 3-alkyl-2-aryl-1,3-thiazinan-4-ones, possessing a methylsulfonyl pharmacophore, were synthesized and their biological activities were evaluated for cyclooxygenase-2 (COX-2) inhibitory activity. In vitro CO... 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1 alpha inhibitors [作者：Uno, M; Ban, HS; Nakamura, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3166-3169 , 文章类型： Article，,卷期：2009年19-12] A series of 1-[4-(N-benzylamino)phenyl]-3-phenylurea derivatives 2a-r were synthesized as HIF-1 alpha inhibitors. Among the compounds synthesized, compound 2k was found to be a potent inhibitor against HIF-1 alpha accumu... Carbonic anhydrase inhibitors. Phenacetyl-, pyridylacetyl- and thienylacetyl-substituted aromatic sulfonamides act as potent and selective isoform VII inhibitors [作者：Guzel, O; Innocenti, A; Scozzafava, A; Salman, A; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3170-3173 , 文章类型： Article，,卷期：2009年19-12] A series of aromatic/heterocyclic sulfonamides incorporating phenyl(alkyl), halogenosubstituted-phenylor 1,3,4-thiadiazole-sulfonamide moieties and thienylacetamido; phenacetamido- and pyridinylacetamido tails were prepa... Discovery of selective PDE4B inhibitors [作者：Naganuma, K; Omura, A; Maekawara, N; Saitoh, M; Ohkawa, N; Kubota, T; Nagumo, H; Kodama, T; Takemura, M; Ohtsuka, Y; Nakamura, J; Tsujita, R; Kawasaki, K; Yokoi, H; Kawanishi, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3174-3176 , 文章类型： Article，,卷期：2009年19-12] In this study the first PDE4B selective inhibitor is described. Optimization of lead 2-arylpyrimidine derivatives afforded a series of potent PDE4B inhibitors with >100-fold selectivity over the PDE4D isozyme. With a goo... Differences in CYP3A4 catalyzed bioactivation of 5-aminooxindole and 5-aminobenzsultam scaffolds in proline-rich tyrosine kinase 2 (PYK2) inhibitors: Retrospective analysis by CYP3A4 molecular docking, quantum chemical calculations and glutathione adduct detection using linear ion trap/orbitrap mass spectrometry [作者：Sun, H; Sharma, R; Bauman, J; Walker, DP; Aspnes, GE; Zawistoski, MP; Kalgutkar, AS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3177-3182 , 文章类型： Article，,卷期：2009年19-12] Previous studies have demonstrated the CYP3A4 mediated oxidation of the 5-aminooxindole motif, present in the trifluoromethylpyrimidine class of PYK-2 inhibitors, to a reactive bis-imine species, which can be trapped wit... Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists [作者：Ivachtchenko, AV; Frolov, EB; Mitkin, OD; Kysil, VM; Khvat, AV; Okun, IM; Tkachenko, SE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3183-3187 , 文章类型： Article，,卷期：2009年19-12] Synthesis, biological evaluation and structure-activity relationships for a series of novel gamma-carboline analogues of Dimebon (TM) are described. Among the studied compounds, gamma-carbolines 3{8} and 3{14} have been ... Novel non-peptide beta-secretase inhibitors derived from structure-based virtual screening and bioassay [作者：Xu, WJ; Chen, G; Liew, OW; Zuo, ZL; Jiang, HL; Zhu, WL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3188-3192 , 文章类型： Article，,卷期：2009年19-12] This Letter describes an efficient approach by integrating virtual screening with bioassay technology for finding small organic inhibitors targeting beta-secretase (BACE-1). Fifteen hits with inhibitory potencies ranging... An efficient preparation of N-alkyl-2-benzazepine derivatives and investigation of their biological activity [作者：Kamimura, A; So, M; Kuratani, T; Matsuura, K; Inui, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3193-3195 , 文章类型： Article，,卷期：2009年19-12] N-Alkyl-2-benzazepine derivatives are readily prepared through N-alkylation of secondary 2-benzazepines that are constructed via 7-endo selective cyclization of radical cyclization of N-boc-N-(2-bromo5-methoxyphenylmethy... Synthesis, biological evaluation of prenylflavonoids as vasorelaxant and neuroprotective agents [作者：Dong, XW; Qi, LL; Jiang, CY; Chen, J; Wei, EQ; Hu, YZ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3196-3198 , 文章类型： Article，,卷期：2009年19-12] A series of prenylflavonoids with multiple hydroxyl groups were synthesized and evaluated for their vasorelaxant activities against rat aorta rings pre-contracted by phenylephrine (PE), as well as their neuroprotective e... Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain [作者：Sasikumar, TK; Qiang, L; Burnett, DA; Greenlee, WJ; Li, C; Heimark, L; Pramanik, B; Grilli, M; Bertorelli, R; Lozza, G; Reggiani, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3199-3203 , 文章类型： Article，,卷期：2009年19-12] Introduction of small unsaturated alkylamino groups at the 4-position of the A-ring of the tricyclic framework (triazafluorenone) afforded extremely potent and selective mGluR1 antagonists with desirable properties. Comp... A novel class of H-3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin [作者：Kennedy, JP; Conn, PJ; Lindsley, CW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3204-3208 , 文章类型： Article，,卷期：2009年19-12] This Letter describes the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin, and the resulting SAR of H-3 antagonism. Multiple rounds of iterative parallel synthesis impro... Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype [作者：Rodriguez, AL; Williams, R; Zhou, Y; Lindsley, SR; Le, U; Grier, MD; Weaver, CD; Conn, PJ; Lindsley, CW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3209-3213 , 文章类型： Article，,卷期：2009年19-12] This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype. This work demonstrates fu... Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands [作者：Liu, KG; Lo, JR; Comery, TA; Zhang, GM; Zhang, JY; Kowal, DM; Smith, DL; Di, L; Kerns, EH; Schechter, LE; Robichaud, AJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3214-3216 , 文章类型： Article，,卷期：2009年19-12] Cognitive dysfunction is a characteristic of various forms of dementia such as Alzheimer's disease (AD) and a core feature of schizophrenia. As part of our continuing efforts to develop agents for cognitive enhancement, ... Effects of bromide upon reaction of nucleosides with hydrogen peroxide induced by ultraviolet light [作者：Suzuki, T; Moriwaki, N; Kurokawa, K; Inukai, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3217-3219 , 文章类型： Article，,卷期：2009年19-12] When ultraviolet light was irradiated on a neutral solution of deoxynucleosides and hydrogen peroxide, concentrations of all the deoxynucleosides decreased greatly. Addition of bromide in the system suppressed the reacti... Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors [作者：Nakamura, H; Watanabe, M; Ban, HS; Nabeyama, W; Asai, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3220-3224 , 文章类型： Article，,卷期：2009年19-12] A series of boron peptides 11, 13, 15 and 17 were designed and synthesized as proteasome inhibitors based on the structure of Belactosin C. Matteson homologation was a key step in the synthesis of the boron peptides. Com...