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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57条记录   PET imaging using (64)Cu-labeled sulfophthalocyanines: Synthesis and biodistribution [作者：Ranyuk, ER; Cauchon, N; Ali, H; Lecomte, R; Guerin, B; van Lier, JE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7470-7473 , 文章类型： Article，,卷期：2011年21-24] Sulfonated metallo phthalocyanines (MPcS(n)) are second generation photosensitizers advanced for photodynamic therapy of various medical applications. A series of ZnPcS(n) was demetallated and subsequently converted to t... ortho-Quinone tanshinones directly inhibit telomerase through an oxidative mechanism mediated by hydrogen peroxide [作者：Soares, J; Keppler, BR; Wang, XH; Lee, KH; Jarstfer, MB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7474-7478 , 文章类型： Article，,卷期：2011年21-24] The tanshinone natural products possess a variety of pharmacological properties including anti-bacterial, anti-inflammatory, anti-oxidant, and anti-neoplastic activity. The molecular basis of these effects, however, rema... Evaluation of new chalcone derivatives as polyphenol oxidase inhibitors [作者：Sonmez, F; Sevmezler, S; Atahan, A; Ceylan, M; Demir, D; Gencer, N; Arslan, O; Kucukislamoglu, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7479-7482 , 文章类型： Article，,卷期：2011年21-24] A newly series of 4-(phenylurenyl) chalcone (4a-j) and 4'-(phenylurenyl/thiourenyl)chalcone (9a-l) derivatives were synthesized and their inhibitory effects on the diphenolase activity of banana tyrosinase were evaluated... Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases [作者：Miles, TJ; Barfoot, C; Brooks, G; Brown, P; Chen, DZ; Dabbs, S; Davies, DT; Downie, DL; Eyrisch, S; Giordano, I; Gwynnd, MN; Hennessy, A; Hoover, J; Huang, JZ; Jones, G; Markwell, R; Rittenhouse, S; Xiang, H; Pearson, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7483-7488 , 文章类型： Article，,卷期：2011年21-24] As part of our wider efforts to exploit novel mode of action antibacterials, we have discovered a series of cyclohexyl-amide compounds that has good Gram positive and Gram negative potency. The mechanism of action is via... Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases [作者：Miles, TJ; Axten, JM; Barfoot, C; Brooks, G; Brown, P; Chen, DZ; Dabbs, S; Davies, DT; Downie, DL; Eyrisch, S; Gallagher, T; Giordano, I; Gwynn, MN; Hennessy, A; Hoover, J; Huang, JZ; Jones, G; Markwell, R; Miller, WH; Minthorn, EA; Rittenhouse, S; Seefeld, M; Pearson, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7489-7495 , 文章类型： Article，,卷期：2011年21-24] We have identified a series of amino-piperidine antibacterials with a good broad spectrum potency. We report the investigation of various subunits in this series and advanced studies on compound 8. Compound 8 possesses g... The discovery of novel cyclohexylamide CCR2 antagonists [作者：Lanter, JC; Markotan, TP; Zhang, XQ; Subasinghe, N; Kang, FA; Hou, CF; Singer, M; Opas, E; McKenney, S; Crysler, C; Johnson, D; Molloy, CJ; Sui, ZH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7496-7501 , 文章类型： Article，,卷期：2011年21-24] As a result of further SAR studies on a piperidinyl piperidine scaffold, we report the discovery of compound 44, a potent, orally bioavailable CCR2 antagonist. While having some in vitro hERG activity, this molecule was ... Synthetase polyspecificity as a tool to modulate protein function [作者：Young, DD; Jockush, S; Turro, NJ; Schultz, PG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7502-7504 , 文章类型： Article，,卷期：2011年21-24] The site-specific incorporation of unnatural amino acids (UAAs) into proteins in bacteria is made possible by the evolution of aminoacyl-tRNA synthetases that selectively recognize and aminoacylate the amino acid of inte... Molecular properties prediction and synthesis of novel 1,3,4-oxadiazole analogues as potent antimicrobial and antitubercular agents [作者：Ahsan, MJ; Samy, JG; Khalilullah, H; Nomani, MS; Saraswat, P; Gaur, R; Singh, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7246-7250 , 文章类型： Article，,卷期：2011年21-24] In the present investigation, a series of 1,5-dimethyl-2-phenyl-4-{[(5-aryl-1,3,4-oxadiazol-2-yl) methyl] amino}-1,2-dihydro-3H-pyrazol-3-one were subjected to molecular properties prediction, drug-likeness by Molinspira... Synthesis and antihepatotoxic activity of 5-(2,3-dihydro-1,4-benzodioxane-6-yl)-3-substituted-phenyl-4,5-dihydro-1H-pyrazole derivatives [作者：Khalilullah, H; Khan, S; Ahsan, MJ; Ahmed, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7251-7254 , 文章类型： Article，,卷期：2011年21-24] In continuance of our search for newer antihepatotoxic agents some novel pyrazoline derivatives containing 1,4-dioxane ring system were synthesized starting from 3-(2,3-dihydro-1,4-benzodioxane-6-yl)-1-substituted-phenyl... Rational design and synthesis of aminopiperazinones as beta-secretase (BACE) inhibitors [作者：Tresadern, G; Delgado, F; Delgado, O; Gijsen, H; Macdonald, GJ; Moechars, D; Rombouts, F; Alexander, R; Spurlino, J; Van Gool, M; Vega, JA; Trabanco, AA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7255-7260 , 文章类型： Article，,卷期：2011年21-24] Aminopiperazinone inhibitors of BACE were identified by rational design. Structure based design guided idea prioritization and initial racemic hit 18a showed good activity. Modification in decoration and chiral separatio... Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: Control of selectivity by a benzyloxy group [作者：Tripathy, R; McHugh, RJ; Ghose, AK; Ott, GR; Angeles, TS; Albom, MS; Huang, Z; Aimone, LD; Cheng, MG; Dorsey, BD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7261-7264 , 文章类型： Article，,卷期：2011年21-24] Anaplastic lymphoma kinase (ALK) is transmembrane receptor tyrosine kinase, with oncogenic variants that have been implicated in ALCL, NSCLC and other cancers. Screening of a VEGFR2-biased kinase library resulted in iden... A simple synthesis of APM([p-(N-acrylamino)-phenyl]mercuric chloride), a useful tool for the analysis of thiolated biomolecules [作者：de Talance, VL; Bauer, F; Hermand, D; Vincent, SP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7265-7267 , 文章类型： Article，,卷期：2011年21-24] This study describes two novel synthetic procedures to prepare APM, a useful tool for the analysis and the purification of thiolated biomolecules. The methods developed are technically simple and robust and allowed the f... Biaryl analogues of teriflunomide as potent DHODH inhibitors [作者：Erra, M; Moreno, I; Sanahuja, J; Andres, M; Reinoso, RF; Lozoya, E; Pizcueta, P; Godessart, N; Castro-Palomino, JC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7268-7272 , 文章类型： Article，,卷期：2011年21-24] The structure-activity relationships of a novel series of biaryl dihydroorotate dehydrogenase (DHODH) inhibitors related to teriflunomide are disclosed. These biaryl derivatives were the result of structure-based design ... Efficient synthesis and in vitro antitubercular activity of 1,2,3-triazoles as inhibitors of Mycobacterium tuberculosis [作者：Shanmugavelan, P; Nagarajan, S; Sathishkumar, M; Ponnuswamy, A; Yogeeswari, P; Sriram, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7273-7276 , 文章类型： Article，,卷期：2011年21-24] Efficient and rapid synthesis of 1,2,3-triazole derivatives has been achieved via Huisgen's 1,3-dipolar cycloaddition between alkyl/arylazides and diethyl/dimethyl acetylenedicarboxylate in excellent yields under solvent... Discovery of 4-aminomethylphenylacetic acids as gamma-secretase modulators via a scaffold design approach [作者：Xin, ZL; Peng, HR; Zhang, A; Talreja, T; Kumaravel, G; Xu, L; Rohde, E; Jung, MY; Shackett, MN; Kocisko, D; Chollate, S; Dunah, AW; Snodgrass-Belt, PA; Arnold, HM; Taveras, AG; Rhodes, KJ; Scannevin, RH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7277-7280 , 文章类型： Article，,卷期：2011年21-24] Starting from literature examples of nonsteroidal anti-inflammatory drugs (NSAIDs)-type carboxylic acid gamma-secretase modulators (GSMs) and using a scaffold design approach, we identified 4-aminomethylphenylacetic acid... Nicotinic acids: Liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy [作者：Powell, DA; Black, WC; Bleasby, K; Chan, CC; Deschenes, D; Gagnon, M; Gordon, R; Guay, J; Guiral, S; Hafey, MJ; Huang, Z; Isabel, E; Leblanc, Y; Styhler, A; Xu, LJ; Zhang, L; Oballa, RM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7281-7286 , 文章类型： Article，,卷期：2011年21-24] An in vitro screening protocol was used to transform a systemically-distributed SCD inhibitor into a liver-targeted compound. Incorporation of a key nicotinic acid moiety enables molecular recognition by OATP transporter...