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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81条记录   Novel N-chloroheterocyclic antimicrobials [作者：Francavilla, C; Turtle, ED; Kim, B; O'Mahony, DJR; Shiau, TP; Low, E; Alvarez, NJ; Celeri, CE; D'Lima, L; Friedman, LC; Ruado, FS; Xu, P; Zuck, ME; Anderson, MB; Najafi, R; Jain, RK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3029-3033 , 文章类型： Article，,卷期：2011年21-10] Antimicrobial compounds with broad-spectrum activity and minimal potential for antibiotic resistance are urgently needed. Toward this end, we prepared and investigated a novel series of N-chloroheterocycles. Of the compo... Dibenzylideneacetone analogues as novel Plasmodium falciparum inhibitors [作者：Aher, RB; Wanare, G; Kawathekar, N; Kumar, RR; Kaushik, NK; Sahal, D; Chauhan, VS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3034-3036 , 文章类型： Article，,卷期：2011年21-10] A series of dibenzylideneacetones (A1-A12) and some of their pyrazolines (B1-B4) were synthesized and evaluated in vitro for blood stage antiplasmodial properties in Plasmodium falciparum culture using SYBR-green-I fluor... Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor [作者：Young, RJ; Alderton, W; Angell, ADR; Beswick, PJ; Brown, D; Chambers, CL; Crowe, MC; Dawson, J; Hamlett, CCF; Hodgson, ST; Kleanthous, S; Knowles, RG; Russell, LJ; Stocker, R; Woolven, JM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3037-3040 , 文章类型： Article，,卷期：2011年21-10] Heteroalicyclic carboxamidines were synthesised and evaluated as inhibitors of nitric oxide synthases. (2R)-2-Pyrrolidinecarboxamidine, in particular, was shown to be a highly potent in vitro (IC50 = 0.12 mu M) and selec... Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related alpha-glucosidase inhibitors and liver X receptor antagonists [作者：Motoshima, K; Sugita, K; Hashimoto, Y; Ishikawa, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3041-3045 , 文章类型： Article，,卷期：2011年21-10] Novel dipeptidyl peptidase IV (DPP-IV) inhibitors with a phenethylphenylphthalimide skeleton were prepared based on alpha-glucosidase inhibitors and liver X receptor (LXR) antagonists derived from thalidomide. Representa... Semisynthesis of triptolide analogues: Effect of gamma-lactone and C-14 substituents on cytotoxic activities [作者：Aoyagi, Y; Hitotsuyanagi, Y; Hasuda, T; Fukaya, H; Takeya, K; Aiyama, R; Matsuzaki, T; Hashimoto, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3046-3049 , 文章类型： Article，,卷期：2011年21-10] Triptolide gamma-lactone and C-14 analogues were prepared and evaluated cytotoxity against human lung adenocarcinoma epithelial A549 cells and human colon adenocarcinoma HT-29 cells. gamma-Lactone substructure and C-14 s... The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors [作者：Xiang, YB; Hirth, B; Asmussen, G; Biemann, HP; Bishop, KA; Good, A; Fitzgerald, M; Gladysheva, T; Jain, A; Jancsics, K; Liu, JY; Metz, M; Papoulis, A; Skerlj, R; Stepp, JD; Wei, RR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3050-3056 , 文章类型： Article，,卷期：2011年21-10] Novel benzofuran-2-carboxylic acids, exemplified by 29, 38 and 39, have been discovered as potent Pim-1 inhibitors using fragment based screening followed by X-ray structure guided medicinal chemistry optimization. The c... Design and synthesis of benzoxazole containing indole analogs as peroxisome proliferator-activated receptor-gamma/delta dual agonists [作者：Gim, HJ; Cheon, YJ; Ryu, JH; Jeon, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3057-3061 , 文章类型： Article，,卷期：2011年21-10] A series of benzoxazole or benzothiazole containing indole analogs, 6-alkoxyindole-2-carboxylic acids and 5-alkoxy-3-indolylacetic acids, were synthesized as novel candidates of PPAR gamma/delta dual agonists and their l... Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5-halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamides [作者：Lv, K; Wang, LL; Liu, ML; Zhou, XB; Fan, SY; Liu, HY; Zheng, ZB; Li, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3062-3065 , 文章类型： Article，,卷期：2011年21-10] We report herein the design and synthesis of novel 1-[3-(dimethylamino) propyl]indolin-2-one derivatives based on the structural features of Sunitinib, a known multitargeted receptor tyrosine kinase inhibitor, and TMP-20... Synthesis and biological evaluation of benzyl styrylsulfonyl derivatives as potent anticancer mitotic inhibitors [作者：Chahrour, O; Abdalla, A; Lam, F; Midgley, C; Wang, SD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3066-3069 , 文章类型： Article，,卷期：2011年21-10] We herein report the synthesis, biological activity and structure activity relationship of derivatives of benzylstyrylsulfone, benzylstyrylsulfine and benzylsulfonyl-N-phenylacetamide. A lead compound 7 represents a new ... Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonists [作者：Morales-Ramos, AI; Li, YH; Hilfiker, M; Mecom, JS; Eidam, P; Shi, DC; Tseng, PS; Brooks, C; Zhang, D; Wang, N; Jaworski, JP; Morrow, D; Fries, H; Edwards, R; Jin, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2806-2811 , 文章类型： Article，,卷期：2011年21-10] Multiple regions of the 3-oxazolidinedione-6-naphthyl-pyridinone series identified via high throughput screening were explored. SAR studies of these regions including the left-hand side oxazolidinedione moiety, alpha-sub... Synthesis and antibacterial activity of alaremycin derivatives for the porphobilinogen synthase [作者：Iwai, N; Nakayama, K; Oku, J; Kitazume, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2812-2815 , 文章类型： Article，,卷期：2011年21-10] The preparation and the antibacterial activity of alaremycin derivatives such as their CF3-derivatives and (R)- and (S)-4-oxo-5-acetylaminohexanoic acid for the porphobilinogen synthase (PBGS), were described. The IC50 v... SAR of 2-amino and 2,4-diamino pyrimidines with in vivo efficacy against Trypanosoma brucei [作者：Perales, JB; Freeman, J; Bacchi, CJ; Bowling, T; Don, R; Gaukel, E; Mercer, L; Moore, JA; Nare, B; Nguyen, TM; Noe, RA; Randolph, R; Rewerts, C; Wring, SA; Yarlett, N; Jacobs, RT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2816-2819 , 文章类型： Article，,卷期：2011年21-10] A series of 2,4-diaminopyrimidines was investigated and compounds were found to have in vivo efficacy against Trypanosoma brucei in an acute mouse model. However, in vitro permeability data suggested the 2,4-diaminopyrim... Chitosan gallate as potential antioxidant biomaterial [作者：Cho, YS; Kim, SK; Je, JY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3070-3073 , 文章类型： Article，,卷期：2011年21-10] Chitosan gallate were synthesized using a free radical-induced grafting reaction. Chitosan gallate showed enhanced water-solubility compared to plain chitosan, and exhibited good thermal stability. The IC50 value of chit... Synthesis and in vitro antitumor activity of new butenolide-containing dithiocarbamates [作者：Wang, XJ; Xu, HW; Guo, LL; Zheng, JX; Xu, B; Guo, X; Zheng, CX; Liu, HM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3074-3077 , 文章类型： Article，,卷期：2011年21-10] Three series of butenolide-containing dithiocarbamates were designed and synthesized. Their anti-tumor activity in vitro was evaluated. Among them compound I-14 exhibited broad spectrum anti-cancer activity against five ... Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery [作者：Erlanson, DA; Arndt, JW; Cancilla, MT; Cao, K; Elling, RA; English, N; Friedman, J; Hansen, SK; Hession, C; Joseph, I; Kumaravel, G; Lee, WC; Lind, KE; McDowell, RS; Miatkowski, K; Nguyen, C; Nguyen, TB; Park, S; Pathan, N; Penny, DM; Romanowski, MJ; Scott, D; Silvian, L; Simmons, RL; Tangonan, BT; Yang, WJ; Sun, LH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3078-3083 , 文章类型： Article，,卷期：2011年21-10] We report the use of a fragment-based lead discovery method, Tethering with extenders, to discover a pyridinone fragment that binds in an adaptive site of the protein PDK1. With subsequent medicinal chemistry, this led t... Regioselective one pot synthesis of 3,3 '-diindolylethylene derivatives and study of their cytotoxic activity [作者：Mandal, M; Kumar, D; Roy, R; Sen, R; Das, P; Chatterjee, M; Jaisankar, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3084-3087 , 文章类型： Article，,卷期：2011年21-10] 2,2'-Diphenyl-3,3'-diindolylethylene (DPDIE) derivatives 3a-g were regioselectively prepared in one pot from indoles 1a-g in the presence of Lewis acids and were subsequently evaluated for cytotoxic activity against huma...