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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79条记录   Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists [作者：Zulli, AL; Aimone, LD; Mathiasen, JR; Gruner, JA; Raddatz, R; Bacon, ER; Hudkins, RL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2807-2810 , 文章类型： Article，,卷期：2012年22-8] Optimization of a series of aminomethyl ketone diamine H3R antagonists to reduce the brain exposure by lowering the pKa, led to molecules with improved pharmacokinetic properties. Compounds 9, 19, and 25 had high affinit... A new class of prolylcarboxypeptidase inhibitors, Part 1: Discovery and evaluation [作者：Graham, TH; Liu, WS; Verras, A; Sebhat, IK; Xiong, YS; Bleasby, K; Bhatt, UR; Chen, Q; Garcia-Calvo, M; Geissler, WM; Gorski, JN; He, HB; Lassman, ME; Lisnock, J; Li, XH; Shen, Z; Tong, XC; Tung, EC; Wiltsie, J; Xiao, JY; Xie, D; Xu, SY; Hale, JJ; Pinto, S; Shen, DM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2811-2817 , 文章类型： Article，,卷期：2012年22-8] A new structural class of potent prolylcarboxypeptidase (PrCP) inhibitors was discovered by high-throughput screening. The series possesses a tractable SAR profile with sub-nanomolar in vitro IC50 values. Compared to pri... A new class of prolylcarboxypeptidase inhibitors, Part 2: The aminocyclopentanes [作者：Graham, TH; Liu, WS; Verras, A; Reibarkh, M; Bleasby, K; Bhatt, UR; Chen, Q; Garcia-Calvo, M; Geissler, WM; Gorski, JN; He, HB; Lassman, ME; Lisnock, J; Li, XH; Shen, Z; Tong, XC; Tung, EC; Wiltsie, J; Xie, D; Xu, SY; Xiao, JY; Hale, JJ; Pinto, S; Shen, DM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2818-2822 , 文章类型： Article，,卷期：2012年22-8] A series of potent inhibitors of prolylcarboxypeptidase (PrCP) was developed by modifying a lead structure that was discovered by high-throughput screening. The tert-butyl pyrrolidine was replaced by an aminocyclopentane... Efficient one-pot cyclization/folding of Rhesus theta-defensin-1 (RTD-1) [作者：Aboye, TL; Li, YL; Majumder, S; Hao, JF; Shekhtman, A; Camarero, JA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2823-2826 , 文章类型： Article，,卷期：2012年22-8] We report an efficient approach for the chemical synthesis of Rhesus theta-defensin-1 (RTD-1) using Fmoc-based solid-phase peptide synthesis in combination with an intramolecular version of native chemical ligation. The ... Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties [作者：Shi, DY; Li, J; Jiang, B; Guo, SJ; Su, H; Wang, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2827-2832 , 文章类型： Article，,卷期：2012年22-8] A series of bromophenol derivatives were synthesized and evaluated as protein tyrosine phosphatase 1B (PTP1B) inhibitors in vitro and in vivo based on bromophenol 4e (IC50 = 2.42 mu mol/ L), which was isolated from red a... Deep-red fluorescent imaging probe for bacteria [作者：White, AG; Gray, BD; Pak, KY; Smith, BD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2833-2836 , 文章类型： Article，,卷期：2012年22-8] A versatile deep-red fluorescent imaging probe is described that is comprised of a bis(zinc(II)-dipicolylamine) targeting unit covalently attached to a pentamethine carbocyanine fluorophore with Cy5-like spectroscopic pr... Design and synthesis of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones as VEGFR-2 kinase inhibitors [作者：Han, SY; Choi, JW; Yang, J; Chae, CH; Lee, J; Jung, H; Lee, K; Ha, JD; Kim, HR; Cho, SY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2837-2842 , 文章类型： Article，,卷期：2012年22-8] A series of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones have been identified as a new class of VEGFR-2 kinase inhibitors. A variety of (4,5,6,7-tetrahydro-imidazo[5,4-c]pyridin-2-yl)-acetic ac... Discovery of novel and potent heterocyclic carboxylic acid derivatives as protein tyrosine phosphatase 1B inhibitors [作者：Basu, S; Prasad, UV; Barawkar, DA; De, S; Palle, VP; Menon, S; Patel, M; Thorat, S; Singh, UP; Das Sarma, K; Waman, Y; Niranjan, S; Pathade, V; Gaur, A; Reddy, S; Ansari, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2843-2849 , 文章类型： Article，,卷期：2012年22-8] A series of novel heterocyclic carboxylic acid based protein tyrosine phosphatase 1B (PTP1B) inhibitors with hydrophobic tail have been synthesized and characterized. Structure-activity relationship (SAR) optimization re... Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis-radiosynthesis and first radiopharmacological evaluation of 5-[I-125]Iodo-sunitinib [作者：Kuchar, M; Oliveira, MC; Gano, L; Santos, I; Kniess, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2850-2855 , 文章类型： Article，,卷期：2012年22-8] Sunitinib (R) (SU11248) is a highly potent tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor (VEGFR). Radiolabeled inhibitors of RTKs might be useful tools for monitoring RTKs levels in tumo... Medicinal chemistry approaches to avoid aldehyde oxidase metabolism [作者：Pryde, DC; Tran, TD; Jones, P; Duckworth, J; Howard, M; Gardner, I; Hyland, R; Webster, R; Wenham, T; Bagal, S; Omoto, K; Schneider, RP; Lin, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2856-2860 , 文章类型： Article，,卷期：2012年22-8] Aldehyde oxidase (AO) is a molybdenum-containing enzyme distributed throughout the animal kingdom and capable of metabolising a wide range of aldehydes and N-heterocyclic compounds. Although metabolism by this enzyme in ... Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive alpha-helix mimetic library [作者：Whitby, LR; Boyle, KE; Cai, LF; Yu, XQ; Gochin, M; Boger, DL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2861-2865 , 文章类型： Article，,卷期：2012年22-8] The evaluation of a comprehensive alpha-helix mimetic library for binding the gp41 NHR hydrophobic pocket recognizing an intramolecular CHR alpha-helix provided a detailed depiction of structural features required for bi... Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: Potent allosteric inhibitors of the hepatitis C virus NS5B polymerase [作者：Ding, M; He, F; Hudyma, TW; Zheng, XF; Poss, MA; Kadow, JF; Beno, BR; Rigat, KL; Wang, YK; Fridell, RA; Lemm, JA; Qiu, D; Liu, MP; Voss, S; Pelosi, LA; Roberts, SB; Gao, M; Knipe, J; Gentles, RG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2866-2871 , 文章类型： Article，,卷期：2012年22-8] Presented here are initial structure-activity relationship (SAR) studies on a series of novel heteroaryl fused tetracyclic indole-based inhibitors of the hepatitis C viral polymerase, NS5B. The introduction of alternativ... Design, synthesis, synergistic antimicrobial activity and cytotoxicity of 4-aryl substituted 3,4-dihydropyrimidinones of curcumin [作者：Lal, J; Gupta, SK; Thavaselvam, D; Agarwal, DD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2872-2876 , 文章类型： Article，,卷期：2012年22-8] 3,4-Dihydropyrimidinones of curcumin were synthesized in excellent yield by multi-component one-pot condensation of curcumin, substituted aromatic aldehydes and urea/thiourea under solvent free conditions using SnCl2 cen... Discovery of a novel chemotype of potent human ENaC blockers using a bioisostere approach. Part 2: alpha-Branched quaternary amines [作者：Hunt, T; Atherton-Watson, HC; Collingwood, SP; Coote, KJ; Czarnecki, S; Danahay, H; Howsham, C; Hunt, P; Paisley, D; Young, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2877-2879 , 文章类型： Article，,卷期：2012年22-8] We report the synthesis and biological evaluation of a series of novel alpha-branched pyrazinoyl quaternary amines for their ability to block ion transport via the epithelial sodium channel (ENaC) in human bronchial epit... 2-Anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1 [作者：Blanchard, S; Soh, CK; Lee, CP; Poulsen, A; Bonday, Z; Goh, KL; Goh, KC; Goh, MK; Pasha, MK; Wang, HS; Williams, M; Wood, JM; Ethirajulu, K; Dymock, BW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2880-2884 , 文章类型： Article，,卷期：2012年22-8] A series of 2-anilino substituted 4-aryl-8H-purines were prepared as potent inhibitors of PDK1, a serine-threonine kinase thought to play a role in the PI3K/Akt signaling pathway, a key mediator of cancer cell growth, su...