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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37条记录   Synthesis of indolizidinone analogues of cytotoxic alkaloids: Monocyclic precursors are also active [作者：Boto, A; Miguelez, J; Marin, R; Diaz, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3402-3407 , 文章类型： Article，,卷期：2012年22-10] Readily available proline derivatives can be transformed in just two steps into analogues of cytotoxic phenanthroindolizidine alkaloids. The key step uses a sequential radical scission-oxidation-alkylation process, which... Tetrahydro-naphthols as orally available TRPV1 inhibitors [作者：Urbahns, K; Yura, T; Gupta, JB; Tajimi, M; Fujishima, H; Masuda, T; Yamamoto, N; Ikegami, Y; Marumo, M; Yasoshima, K; Yoshida, N; Moriwaki, T; Madge, D; Chan, FN; Mogi, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3408-3411 , 文章类型： Article，,卷期：2012年22-10] Starting from a naphthol-based lead series with low oral bioavailability, we have identified potent TRPV1 antagonists with oral bioavailability in rats. These compounds emerged from SAR studies aimed at replacing the lea... Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity [作者：Ryabtsova, O; Jansen, K; Van Goethem, S; Joossens, J; Cheng, JD; Lambeir, AM; De Meester, I; Augustyns, K; Van der Veken, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3412-3417 , 文章类型： Article，,卷期：2012年22-10] A series of N-acylated glycyl-(2-cyano) pyrrolidines were synthesized with the aim of generating structure-activity relationship (SAR) data for this class of compounds as inhibitors of fibroblast activation protein (FAP)... Synthesis and characterization of folic acid modified water-soluble chitosan derivatives for folate-receptor-mediated targeting [作者：Jing, HH; Guo, ZD; Guo, WY; Yang, WJ; Xu, P; Zhang, XZ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3418-3424 , 文章类型： Article，,卷期：2012年22-10] Three chemical modification methods of carboxymethylation, quaternization and hydroxypropylation were used to synthesize water-soluble chitosan derivatives. In order to study the feasibility of these chitosan derivatives... Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK) [作者：Lavogina, D; Kalind, K; Bredihhina, J; Hurt, M; Vaasa, A; Kasari, M; Enkvist, E; Raidaru, G; Uri, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3425-3430 , 文章类型： Article，,卷期：2012年22-10] In the present work, conjugates of 5-isoquinolinesulfonylamides and D-arginine-rich peptides were developed into highly potent inhibitors for basophilic protein kinases. Based on Hidaka's inhibitor H9, a generic fluoresc... Novel triazolopyridylbenzamides as potent and selective p38 alpha inhibitors [作者：Aiguade, J; Balague, C; Carranco, I; Caturla, F; Dominguez, M; Eastwood, P; Esteve, C; Gonzalez, J; Lumeras, W; Orellana, A; Preciado, S; Roca, R; Vidal, L; Vidal, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3431-3436 , 文章类型： Article，,卷期：2012年22-10] A new class of p38 alpha inhibitors based on a biaryl-triazolopyridine scaffold was investigated. X-ray crystallographic data of the initial lead compound cocrystallised with p38 alpha was crucial in order to uncover a u... Discovery of cariprazine (RGH-188): A novel antipsychotic acting on dopamine D-3/D-2 receptors [作者：Agai-Csongor, E; Domany, G; Nogradi, K; Galambos, J; Vago, I; Keseru, GM; Greiner, I; Laszlovszky, I; Gere, A; Schmidt, E; Kiss, B; Vastag, M; Tihanyi, K; Saghy, K; Laszy, J; Gyertyan, I; Zajer-Balazs, M; Gemesi, L; Kapas, M; Szombathelyi, Z,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3437-3440 , 文章类型： Article，,卷期：2012年22-10] Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D-3/D-2 compound (1) led to a series of new piperazine derivatives having affinity to both dopa... Practical access to four stereoisomers of naftidrofuryl and their binding affinity towards 5-hydroxytryptamine 2A receptor [作者：Hao, J; Chen, B; Yao, YW; Hossain, M; Nagatomo, T; Yao, HQ; Kong, LY; Sun, HB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3441-3444 , 文章类型： Article，,卷期：2012年22-10] Naftidrofuryl oxalate (Praxilene (R), 1) has been used for the treatment of intermittent claudication for more than 30 years. It selectively blocks vascular and platelet 5-hydroxytryptamine 2 (2-HT2) receptors. This drug... A novel pyrimidine derivatives with aryl urea, thiourea and sulfonamide moieties: Synthesis, anti-inflammatory and antimicrobial evaluation [作者：Keche, AP; Hatnapure, GD; Tale, RH; Rodge, AH; Birajdar, SS; Kamble, VM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3445-3448 , 文章类型： Article，,卷期：2012年22-10] A series of novel 4-(3-(trifluoromethyl) phenylamino-6-(4-(3-arylureiodo/arylthioureido/arylsulfonamido)-pyrimidine derivatives of biological interest were prepared by the sequential Suzuki cross coupling, acid amination... Synthesis and biological evaluation of some novel thiazole substituted benzotriazole derivatives [作者：Gaikwad, ND; Patil, SV; Bobade, VD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3449-3454 , 文章类型： Article，,卷期：2012年22-10] A series of novel hybrid molecules 4a-y containing thiazole and benzotriazole templates were designed and synthesized. The structures of the synthesized compounds were elucidated by IR, H-1 NMR, C-13 NMR and mass spectra... Solvent effect on copper-catalyzed azide-alkyne cycloaddition (CuAAC): Synthesis of novel triazolyl substituted quinolines as potential anticancer agents [作者：Ellanki, AR; Islam, A; Rama, VS; Pulipati, RP; Rambabu, D; Krishna, GR; Reddy, CM; Mukkanti, K; Vanaja, GR; Kalle, AM; Kumar, KS; Pal, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3455-3459 , 文章类型： Article，,卷期：2012年22-10] A regioselective route to novel mono triazolyl substituted quinolines has been developed via copper-catalyzed azide-alkyne cycloaddition (CuAAC) of 2,4-diazidoquinoline with terminal alkynes in DMF. The reaction provided... Identification of ETP-46321, a potent and orally bioavailable PI3K alpha, delta inhibitor [作者：Gonzalez, SM; Hernandez, AI; Varela, C; Rodriguez-Aristegui, S; Lorenzo, M; Rodriguez, A; Rivero, V; Martin, JI; Saluste, CG; Ramos-Lima, F; Cendon, E; Cebrian, D; Aguirre, E; Gomez-Casero, E; Albarran, M; Alfonso, P; Garcia-Serelde, B; Oyarzabal, J; Rabal, O; Mulero, F; Gonzalez-Granda, T; Link, W; Fominaya, J; Barbacid, M; Bischoff, JR; Pizcueta, P; Pastor, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3460-3466 , 文章类型： Article，,卷期：2012年22-10] Phosphoinositide-3-kinase (PI3K) is an important target for cancer therapeutics due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein, we describe the optimization of imidazo [1,2-a... Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM(1) muscarinic acetylcholine receptor [作者：Melancon, BJ; Gogliotti, RD; Tarr, JC; Saleh, SA; Chauder, BA; Lebois, EP; Cho, HP; Utley, TJ; Sheffler, DJ; Bridges, TM; Morrison, RD; Daniels, JS; Niswender, CM; Conn, PJ; Lindsley, CW; Wood, MR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3467-3472 , 文章类型： Article，,卷期：2012年22-10] This Letter describes the continued optimization of the MLPCN probe molecule ML071. After introducing numerous cyclic constraints and novel substitutions throughout the parent structure, we produced a number of more high... Synthesis, biological evaluation and structure-activity relationships of glycyrrhetinic acid derivatives as novel anti-hepatitis B virus agents [作者：Wang, LJ; Geng, CA; Ma, YB; Huang, XY; Luo, J; Chen, H; Zhang, XM; Chen, JJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3473-3479 , 文章类型： Article，,卷期：2012年22-10] Fifty-seven derivatives of glycyrrhetinic acid (GA) were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Among them, sixteen compounds showed greater anti-HBV activity tha... Synthesis and anti-norovirus activity of pyranobenzopyrone compounds [作者：Pokhrel, L; Kim, Y; Nguyen, TDT; Prior, AM; Lu, JY; Chang, KO; Hua, DH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3480-3484 , 文章类型： Article，,卷期：2012年22-10] During the last decade, noroviruses have gained media attention as the cause of large scale outbreaks of gastroenteritis on cruise ships, dormitories, nursing homes, etc. Although noroviruses do not multiply in food or w... The effect of vindoline C-16 substituents on the biomimetic coupling reaction: Synthesis and cytotoxicity evaluation of the corresponding vinorelbine analogues [作者：Song, WB; Hu, LJ; Meng, YH; Ma, L; Guo, D; Liu, X; Hu, LH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3485-3487 , 文章类型： Article，,卷期：2012年22-10] A new series of vinorelbine analogues are designed and synthesized to explore the vindoline C-16 substituent effects on the biomimetic coupling with catharanthine, and the structure-activity relationships of these vinore...