- Hydrolytic Reactivity Trends among Potential Prodrugs of the O2-Glycosylated Diazeniumdiolate Family. Targeting Nitric Oxide to Macrophages for Antileishmanial Activity.
[作者:Valdez, Carlos A.;Saavedra, Joseph E.;Showalter, Brett M.;Davies, Keith M.;Wilde, Thomas C.;Citro, Michael L.;Barchi, Joseph J., Jr.;Deschamps, Jeffrey R.;Parrish, Damon;El-Gayar, Stefan;Schleicher, Ulrike;Bogdan, Christian;Keefer, Larry K.;,期刊:Journal of Medicinal Chemistry, 页码:3961-3970 , 文章类型: 研究论文,,卷期:2008年51-13]
- Glycosylated diazeniumdiolates of structure R2NN(O)=NO-R' (R' = a saccharide residue) are potential prodrugs of the nitric oxide (NO)-releasing but acid-sensitive R2NN(O)=NO- ion. Moreover, cleaving the acid-stable glyc...
- Structure-Activity Relationships of the Cycloalkanol Ethylamine Scaffold: Discovery of Selective Norepinephrine Reuptake Inhibitors.
[作者:Mahaney, Paige E.;Gavrin, Lori K.;Trybulski, Eugene J.;Stack, Gary P.;Vu, An T.;Cohn, Stephen T.;Ye, Fei;Belardi, Justin K.;Santilli, Arthur A.;Sabatucci, Joseph P.;Leiter, Jennifer;Johnston, Grace H.;Bray, Jenifer A.;Burroughs, Kevin D.;Cosmi, Scott A.;L,期刊:Journal of Medicinal Chemistry, 页码:4038-4049 , 文章类型: 研究论文,,卷期:2008年51-13]
- Further exploration of the cycloalkanol ethylamine scaffold, of which venlafaxine (1) is a member, was undertaken to develop novel and selective norepinephrine reuptake inhibitors (NRIs) for evaluation in a variety of pr...
- 2-Aminobenzophenones as a Novel Class of Bradykinin B1 Receptor Antagonists.
[作者:Su, Dai-Shi;Lim, John L.;Tinney, Elizabeth;Wan, Bang-Lin;Murphy, Kathy L.;Reiss, Duane R.;Harrell, C. Meacham;O'Malley, Stacy S.;Ransom, Rick W.;Chang, Raymond S. L.;Pettibone, Douglas J.;Yu, Jian;Tang, Cuyue;Prueksaritanont, Thomayant;Freidinger, Roger M,期刊:Journal of Medicinal Chemistry, 页码:3946-3952 , 文章类型: 研究论文,,卷期:2008年51-13]
- Selective bradykinin (BK) B1 receptor antagonists could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure activity relationships of the structurally novel HTS lead compd...
- Discovery of a Novel Series of Biphenyl Benzoic Acid Derivatives as Highly Potent and Selective Human b3 Adrenergic Receptor Agonists with Good Oral Bioavailability. Part II.
[作者:Imanishi, Masashi;Itou, Shinji;Washizuka, Kenichi;Hamashima, Hitoshi;Nakajima, Yutaka;Araki, Takanobu;Tomishima, Yasuyo;Sakurai, Minoru;Matsui, Shigeo;Imamura, Emiko;Ueshima, Koji;Yamamoto, Takao;Yamamoto, Nobuhiro;Ishikawa, Hirofumi;Nakano, Keiko;Unami,,期刊:Journal of Medicinal Chemistry, 页码:4002-4020 , 文章类型: 研究论文,,卷期:2008年51-13]
- (FGB) series was modified to improve in vitro and in vivo b3-AR potency without loss of oral bioavailability. First, in this study, we focused our efforts on replacement of the 3-chlorophenyl moiety in the LHS of FGB an...
- Potent Non-Nucleoside Inhibitors of the Measles Virus RNA-Dependent RNA Polymerase Complex.
[作者:Sun, Aiming;Yoon, Jeong-Joong;Yin, Yan;Prussia, Andrew;Yang, Yutao;Min, Jaeki;Plemper, Richard K.;Snyder, James P.;,期刊:Journal of Medicinal Chemistry, 页码:3731-3741 , 文章类型: 研究论文,,卷期:2008年51-13]
- Measles virus (MV) is one of the most infectious pathogens known. In spite of the existence of a vaccine, approx. 350000 deaths/yr result from MV or assocd. complications. Antimeasles compds. could conceivably diminish...
- Theoretical Studies on the Structure and Symmetry of the Transmembrane Region of Glutamatergic GluR5 Receptor.
[作者:Kaczor, Agnieszka A.;Kijkowska-Murak, Urszula A.;Matosiuk, Dariusz;,期刊:Journal of Medicinal Chemistry, 页码:3765-3776 , 文章类型: 研究论文,,卷期:2008年51-13]
- There is numerous exptl. and conceptual proof that the extracellular portion of ionotropic glutamate receptors (iGluRs), i.e., N-terminal domain (NTD) and ligand-binding core (LBD), exhibits 2-fold rotational symmetry an...
- Enhanced Concentration-Dependent Cytotoxic Effect of the Dinuclear Copper(II) Complex of L-Carnitine [Cu2(L-carnitine)2Cl2(H2O)2]Cl2, Compared to L-Carnitine or Copper Chloride Dihydrate, in Human Leukemic Cell Lines.
[作者:Thomadaki, Hellinida;Karaliota, Alexandra;Litos, Charalambos;Scorilas, Andreas;,期刊:Journal of Medicinal Chemistry, 页码:3713-3719 , 文章类型: 研究论文,,卷期:2008年51-13]
- We studied the antitumor properties of the dinuclear copper(II) complex of L-carnitine [Cu2(L-carnitine)2Cl2(H2O)2]Cl2, as well as those of L-carnitine and copper chloride dihydrate, in human leukemic cells. The complex...
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