个性化文献订阅>文章检索

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81条记录   Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents [作者：Khera, MK; Cliffe, IA; Mathur, T; Prakash, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2887-2889 , 文章类型： Article，,卷期：2011年21-10] The synthesis and antibacterial activity of 3-(4-([1,2,4] triazolo[4,3-a] pyrimidin-3-yl) phenyl) oxazolidin-2-ones is reported. Thiocarbonyl derivatives were found to be potent inhibitors of Gram-positive pathogens and ... SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors [作者：Zhou, G; Ting, PC; Aslanian, R; Cao, JH; Kim, DW; Kuang, RZ; Lee, JF; Schwerdt, J; Wu, HP; Herr, RJ; Zych, AJ; Yang, JH; Lam, S; Wainhaus, S; Black, TA; McNicholas, PM; Xu, YM; Walker, SS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2890-2893 , 文章类型： Article，,卷期：2011年21-10] A novel series of pyridazinone analogs has been developed as potent beta-1,3-glucan synthase inhibitors through structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl... Penicisteroids A and B, antifungal and cytotoxic polyoxygenated steroids from the marine alga-derived endophytic fungus Penicillium chrysogenum QEN-24S [作者：Gao, SS; Li, XM; Li, CS; Proksch, P; Wang, BG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2894-2897 , 文章类型： Article，,卷期：2011年21-10] Two new polyoxygenated steroids, namely, penicisteroids A and B (1 and 2), were obtained from the culture extract of Penicillium chrysogenum QEN-24S, an endophytic fungus isolated from an unidentified marine red algal sp... 2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors [作者：Dai, CY; Li, DS; Popovici-Muller, J; Zhao, LY; Girijavallabhan, VM; Rosner, KE; Lavey, BJ; Rizvi, R; Shankar, BB; Wong, MKC; Guo, ZY; Orth, P; Strickland, CO; Sun, J; Niu, XD; Chen, SY; Kozlowski, JA; Lundell, DJ; Piwinski, JJ; Shih, NY; Siddiqui, MA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3172-3176 , 文章类型： Article，,卷期：2011年21-10] TNF-alpha converting enzyme (TACE) inhibitors are promising agents to treat inflammatory disorders and cancer. We have investigated novel tartrate diamide TACE inhibitors where the tartrate core binds to zinc in a unique... Dual function inhibitors of relevance to chronic obstructive pulmonary disease [作者：Dou, DF; He, GJ; Alliston, KR; Groutas, WC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3177-3180 , 文章类型： Article，,卷期：2011年21-10] The general strategy and rationale underlying the design of COPD therapeutics that possess protease inhibitory activity and are also capable of releasing a species that attenuates inflammation by inhibiting caspase-1, ar... Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo-pyrimidines as potent human A(3) adenosine receptor antagonists [作者：Cheong, SL; Federico, S; Venkatesan, G; Paira, P; Shao, YM; Spalluto, G; Yap, CW; Pastorin, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2898-2905 , 文章类型： Article，,卷期：2011年21-10] A ligand-based pharmacophore was obtained for a new series of 2-unsubstituted and 2-(para-substituted) phenyl-pyrazolo-triazolo-pyrimidines as potent human A(3) adenosine receptor antagonists. Through comparative molecul... Antifibrotic constituents of Alnus firma on hepatic stellate cells [作者：Lee, M; Lee, MK; Kim, YC; Sung, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2906-2910 , 文章类型： Article，,卷期：2011年21-10] Suppression of hepatic stellate cell (HSC) growth and activation have been proposed as therapeutic strategies for the treatment and prevention of liver fibrosis. In the course of screening antifibrotic activity of natura... Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists [作者：Wang, LP; Hubert, JA; Lee, SJ; Pan, J; Qian, S; Reitman, ML; Strack, AM; Weingarth, DT; MacNeil, DJ; Weber, AE; Edmondson, SD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2911-2915 , 文章类型： Article，,卷期：2011年21-10] A series of six-membered heterocycle carboxamides were synthesized and evaluated as cholecystokinin 1 receptor (CCK1R) agonists. A pyrimidine core proved to be the best heterocycle, and SAR studies resulted in the discov... Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents [作者：Liu, XH; Ruan, BF; Liu, JX; Song, BA; Jing, LH; Li, J; Yang, Y; Zhu, HL; Qi, XB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2916-2920 , 文章类型： Article，,卷期：2011年21-10] A series of novel N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential telomerase inhibitors were synthesized. The bioassay tests show that compound 4a exhibited high activity against human gastric canc... Synthesis of 5(6)-dihydro-OSW-1 analogs bearing three kinds of disaccharides linking at 15-hydroxy and their antitumor activities [作者：Guan, YY; Zheng, D; Zhou, L; Wang, HX; Yan, Z; Wang, N; Chang, H; She, PP; Lei, PS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2921-2924 , 文章类型： Article，,卷期：2011年21-10] In order to study the SAR of 5(6)-dihydro-OSW-1, eight 15(alpha)beta-O-glycosyl analogs (26-33) carrying three kinds of disaccharides including [beta-D-Xylp-(1-3)-alpha-L-Arap], [beta-D-Xylp-(1-4)-alpha-L-Arap] and [alph... Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus [作者：Zheng, XF; Hudyma, TW; Martin, SW; Bergstrom, C; Ding, M; He, F; Romine, J; Poss, MA; Kadow, JF; Chang, CH; Wan, J; Witmer, MR; Morin, P; Camac, DM; Sheriff, S; Beno, BR; Rigat, KL; Wang, YK; Fridell, R; Lemm, J; Qiu, D; Liu, MP; Voss, S; Pelosi, L; Roberts, SB; Gao, M; Knipe, J; Gentles, RG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2925-2929 , 文章类型： Article，,卷期：2011年21-10] Herein, we present initial SAR studies on a series of bridged 2-arylindole-based NS5B inhibitors. The introduction of bridging elements between the indole N1 and the ortho-position of the 2-aryl moiety resulted in confor... Total synthesis of solamargine [作者：Wei, GH; Wang, J; Du, YG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2930-2933 , 文章类型： Article，,卷期：2011年21-10] Solamargine, (25R)-3 beta-{O-alpha-L-rhamnopyranosyl-(1 -> 2)-[O-alpha-L-rhamnopyranosyl-(1 -> 4)]-beta-D-glucopyranosyloxy}-22 alpha-N-spirosol-5-ene, has been synthesized in 13 steps in a 10.5% overall yield starting f... A chemically modified lipase preparation for catalyzing the transesterification reaction in even highly polar organic solvents [作者：Solanki, K; Gupta, MN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2934-2936 , 文章类型： Article，,卷期：2011年21-10] Acylation of Pseudomonas cepacia lipase with Pyromellitic dianhydride to modify 72% of total amino groups was carried out. Different organic solvents were screened for precipitation of modified lipase. It was found that ... Synthesis and transfection activity of novel galactosylated polycationic lipid [作者：Maslov, MA; Medvedeva, DA; Rapoport, DA; Serikov, RN; Morozova, NG; Serebrennikova, GA; Vlassov, VV; Zenkova, MA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2937-2940 , 文章类型： Article，,卷期：2011年21-10] In this study, we synthesized a new galactosylated cationic lipid and investigated its biological activity. The structure of lipid combines both spermine residue for DNA compaction and galactose moiety for the improvemen... Tumor-specific hybrid polyhydroxybutyrate nanoparticle: Surface modification of nanoparticle by enzymatically synthesized functional block copolymer [作者：Lee, J; Jung, SG; Park, CS; Kim, HY; Batt, CA; Kim, YR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2941-2944 , 文章类型： Article，,卷期：2011年21-10] A new approach to functionalize the surface of hydrophobic nanocarrier through enzymatic polymerization was demonstrated. The effective coupling between the hydrophobic surface of PHB nanoparticle and PHB chain grown fro... Inhibition and structural reliability of prenylated flavones from the stem bark of Morus lhou on beta-secretase (BACE-1) [作者：Cho, JK; Ryu, YB; Curtis-Long, MJ; Kim, JY; Kim, D; Lee, S; Lee, WS; Park, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2945-2948 , 文章类型： Article，,卷期：2011年21-10] The action of beta-secretase is strongly tied to the onset of Alzheimer's disease. The development of inhibitors of beta-secretase is thus critical to combating this disease, which threatens an ever increasing number of ...