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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75条记录   Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides [作者：Xu, LB; Farthing, AK; Dropinski, JF; Meinke, PT; McCallum, C; Leavitt, PS; Hickey, EJ; Colwell, L; Barrett, J; Liu, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3531-3535 , 文章类型： Article，,卷期：2009年19-13] Novel water-soluble amide analogs were synthesized from nocathiacin I (1) through the formation of the carboxylic acid intermediate followed by coupling to primary or secondary amines. Several compounds with potent antib... Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers [作者：Kemnitzer, W; Sirisoma, N; May, C; Tseng, B; Drewe, J; Cai, SX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3536-3540 , 文章类型： Article，,卷期：2009年19-13] We report the discovery of N-((benzo[d][1,3]dioxol-5-yl)methyl)-6-phenylthieno[3,2-d] pyrimidin-4-amine (2a) as an apoptosis inducer using our proprietary cell-and caspase-based ASAP HTS assay, and SAR study of HTS hit 2... Design and optimization of renin inhibitors: Orally bioavailable alkyl amines [作者：Tice, CM; Xu, ZR; Yuan, J; Simpson, RD; Cacatian, ST; Flaherty, PT; Zhao, W; Guo, J; Ishchenko, A; Singh, SB; Wu, ZR; Scott, BB; Bukhtiyarov, Y; Berbaum, J; Mason, J; Panemangalore, R; Cappiello, MG; Muller, D; Harrison, RK; McGeehan, GM; Dillard, LW; Baldwin, JJ; Claremon, DA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3541-3545 , 文章类型： Article，,卷期：2009年19-13] Structure-based drug design led to the identification of a novel class of potent, low MW alkylamine renin inhibitors. Oral administration of lead compound 21l, with MW of 508 and IC50 of 0.47 nM, caused a sustained reduc... Antimalarial activity of thiosemicarbazones and purine derived nitriles [作者：Mallari, JP; Guiguemde, WA; Guy, RK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3546-3549 , 文章类型： Article，,卷期：2009年19-13] Malaria is a devastating illness caused by multiple species of the Plasmodium genus. The parasite's falcipain proteases have been extensively studied as potential drug targets. Here we report the testing of two establish... Identification of a PPAR delta agonist with partial agonistic activity on PPAR gamma [作者：Connors, RV; Wang, ZL; Harrison, M; Zhang, A; Wanska, M; Hiscock, S; Fox, B; Dore, M; Labelle, M; Sudom, A; Johnstone, S; Liu, JS; Walker, NPC; Chai, A; Siegler, K; Li, Y; Coward, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3550-3554 , 文章类型： Article，,卷期：2009年19-13] The discovery and optimization of a series of potent PPAR delta full agonists with partial agonistic activity against PPAR gamma is described. (C) 2009 Elsevier Ltd. All rights reserved. Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability [作者：Degnan, AP; Conway, CM; Dalterio, RA; Macci, R; Mercer, SE; Schartman, R; Xu, C; Dubowchik, GM; Macor, JE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3555-3558 , 文章类型： Article，,卷期：2009年19-13] The calcitonin gene-related peptide (CGRP) receptor has been implicated in the pathogenesis of migraine. A class of urethanamide derivatives has been identified as potent inhibitors of the CGRP receptor. Compound 20 was ... Synthesis, cleavage, and antifungal activity of a number of novel, water-soluble ester prodrugs of antifungal triazole CS-758 [作者：Kagoshima, Y; Mori, M; Suzuki, E; Shibayama, T; Iida, T; Kamai, Y; Konosu, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3559-3563 , 文章类型： Article，,卷期：2009年19-13] In this study, the synthesis and evaluation of a number of esters of CS-758 as injectable prodrugs are described. Phosphoryl ester 1a was soluble in water (> 30 mg/mL) and was converted to CS-758 in human liver microsome... Synthesis of novel 3-(1-(1-substituted piperidin-4-yl)-1H-1,2,3-triazol-4-yl)-1,2,4-oxadiazol-5(4H)-one as antifungal agents [作者：Sangshetti, JN; Nagawade, RR; Shinde, DB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3564-3567 , 文章类型： Article，,卷期：2009年19-13] A novel series of 1,2,3 triazole compounds possessing 1,2,4 oxadiazole ring were efficiently synthesized. Synthesized compounds were evaluated for their in vitro antifungal activities using standard cup plate method. SAR... Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists [作者：Moriya, M; Kishino, H; Sakuraba, S; Sakamoto, T; Suga, T; Takahashi, H; Suzuki, T; Ito, M; Ito, J; Moriya, R; Takenaga, N; Iwaasa, H; Ishihara, A; Kanatani, A; Fukami, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3568-3572 , 文章类型： Article，,卷期：2009年19-13] A series of 2-aminobenzimidazole-based MCH1R antagonists was identified by core replacement of the aminoquinoline lead 1. Subsequent modi. cation of the 2- and 5-positions led to improvement in potency and intrinsic clea... Synthesis and antibacterial evaluation of isoxazolinyl oxazolidinones: Search for potent antibacterial [作者：Varshney, V; Mishra, NN; Shukla, PK; Sahu, DP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3573-3576 , 文章类型： Article，,卷期：2009年19-13] A series of (5S) N-(3-{3-fluoro-4-[4-(3-aryl-4,5-dihydro-isoxazole-5-carbonyl)-piperazin-1-yl]-phenyl}2-oxo-oxazolidin-5-ylmethyl)-acetamide(6a-o) were synthesized and their in vitro antibacterial activity against variou... Serratezomines D and E, new Lycopodium alkaloids from Lycopodium serratum var. serratum [作者：Kubota, T; Yahata, H; Yamamoto, S; Hayashi, S; Shibata, T; Kobayashi, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3577-3580 , 文章类型： Article，,卷期：2009年19-13] Two new Lycopodium alkaloids, serratezomines D (1) and E (2), were isolated from the club moss Lycopodium serratum var. serratum. Serratezomine D (1) is a new lucidine-type alkaloid, while serratezomine E (2) is a new ph...