- Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships and molecular modeling studies.
[作者：Sato, Hiroyuki;Macchiarulo, Antonio;Thomas, Charles;Gioiello, Antimo;Une, Mizuho;Hofmann, Alan F.;Saladin, Regis;Schoonjans, Kristina;Pellicciari, Roberto;Auwerx, Johan;,期刊：Journal of Medicinal Chemistry, 页码：4849-4849 , 文章类型： 研究论文，,卷期：2008年51-15]
- The R1 and R2 groups for UDCA derivs. in Table 3 were incorrect. The correct version of Table 3 is given.
- Novel 4-Aminoquinolines Active against Chloroquine-Resistant and Sensitive P. falciparum Strains that also Inhibit Botulinum Serotype A.
[作者：Solaja, Bogdan A.;Opsenica, Dejan;Smith, Kirsten S.;Milhous, Wilbur K.;Terzic, Natasa;Opsenica, Igor;Burnett, James C.;Nuss, Jon;Gussio, Rick;Bavari, Sina;,期刊：Journal of Medicinal Chemistry, 页码：4388-4391 , 文章类型： 研究论文，,卷期：2008年51-15]
- We report on the initial result of the coupling of 4-amino-7-chloroquinoline with steroidal and adamantane constituents to provide small mols. with excellent in vitro antimalarial activities (IC90 (W2) down to 6.74 nM). ...
- Inorganic Polyhedral Metallacarborane Inhibitors of HIV Protease: A New Approach to Overcoming Antiviral Resistance.
[作者：Kozisek, Milan;Cigler, Petr;Lepsik, Martin;Fanfrlik, Jindrich;Rezacova, Pavlina;Brynda, Jiri;Pokorna, Jana;Plesek, Jaromir;Gruner, Bohumir;Grantz Saskova, Klara;Vaclavikova, Jana;Kral, Vladimir;Konvalinka, Jan;,期刊：Journal of Medicinal Chemistry, 页码：4839-4843 , 文章类型： 研究论文，,卷期：2008年51-15]
- HIV protease (PR) is a prime target for rational anti-HIV drug design. We have previously identified icosahedral metallacarboranes as a novel class of nonpeptidic protease inhibitors. Now we show that substituted metall...
- Structure-Antitussive Activity Relationships of Naltrindole Derivatives.
[作者：Identification of Novel and Potent Antitussive Agents. Sakami, Satoshi;Maeda, Masayuki;Kawai, Koji;Aoki, Takumi;Kawamura, Kuniaki;Fujii, Hideaki;Hasebe, Ko;Nakajima, Mayumi;Endo, Takashi;Ueno, Shinya;Ito, Tsuyoshi;Kamei, Junzo;Nagase, Hiroshi;,期刊：Journal of Medicinal Chemistry, 页码：4404-4411 , 文章类型： 研究论文，,卷期：2008年51-15]
- We have previously reported antitussive effects of naltrindole (NTI), a typical d opioid receptor antagonist, in a rat model. The ED50 values of NTI by i.p. and peroral injections were 104 mg/kg and 1840 mg/kg, resp., c...
- Novel Analogues of Istaroxime, a Potent Inhibitor of Na+,K+-ATPase: Synthesis and Structure-Activity Relationship.
[作者：Gobbini, Mauro;Armaroli, Silvia;Banfi, Leonardo;Benicchio, Alessandra;Carzana, Giulio;Fedrizzi, Giorgio;Ferrari, Patrizia;Giacalone, Giuseppe;Giubileo, Michele;Marazzi, Giuseppe;Micheletti, Rosella;Moro, Barbara;Pozzi, Marco;Scotti, Piero Enrico;Torri, Ma,期刊：Journal of Medicinal Chemistry, 页码：4601-4608 , 文章类型： 研究论文，,卷期：2008年51-15]
- of the Na+,K+-ATPase as pos. inotropic compds. Following the previously described model from which istaroxime was generated, the 5a,14a-androstane skeleton was used as a scaffold to study the space around the basic chai...
- Synthesis of GABAA Receptor Agonists and Evaluation of their a-Subunit Selectivity and Orientation in the GABA Binding Site.
[作者：Jansen, Michaela;Rabe, Holger;Strehless, Axelle;Dieler, Sandra;Debus, Fabian;Dannhardt, Gerd;Akabas, Myles H.;Lueddens, Hartmut;,期刊：Journal of Medicinal Chemistry, 页码：4430-4448 , 文章类型： 研究论文，,卷期：2008年51-15]
- Drugs used to treat various disorders target GABAA receptors. To develop a subunit selective compds., we synthesized 5-(4-piperidyl)-3-isoxazolol (4-PIOL) derivs. The 3-isoxazolol moiety was substituted by 1,3,4-oxadia...
- Inhibition of Acetylcholinesterase, b-Amyloid Aggregation, and NMDA Receptors in Alzheimer's Disease: A Promising Direction for the Multi-target-Directed Ligands Gold Rush.
[作者：Rosini, Michela;Simoni, Elena;Bartolini, Manuela;Cavalli, Andrea;Ceccarini, Luisa;Pascu, Nicoleta;McClymont, David W.;Tarozzi, Andrea;Bolognesi, Maria L.;Minarini, Anna;Tumiatti, Vincenzo;Andrisano, Vincenza;Mellor, Ian R.;Melchiorre, Carlo;,期刊：Journal of Medicinal Chemistry, 页码：4381-4384 , 文章类型： 研究论文，,卷期：2008年51-15]
- Alzheimer's disease (AD) is a multifactorial syndrome with several target proteins contributing to its etiol. To confront AD, an innovative strategy is to design single chem. entities able to simultaneously modulate mor...
- Gold(I)-Mediated Inhibition of Protein Tyrosine Phosphatases: A Detailed in Vitro and Cellular Study.
[作者：Krishnamurthy, Divya;Karver, Mark R.;Fiorillo, Edoardo;Orru, Valeria;Stanford, Stephanie M.;Bottini, Nunzio;Barrios, Amy M.;,期刊：Journal of Medicinal Chemistry, 页码：4790-4795 , 文章类型： 研究论文，,卷期：2008年51-15]
- Gold(I) complexes contg. N-heterocyclic carbene ligands were synthesized, characterized, and along with the antiarthritic drug, auranofin, tested as inhibitors of the cysteine-dependent protein tyrosine phosphatases, whi...
- Slow Self-Activation Enhances The Potency of Viridin Prodrugs.
[作者：Blois, Joseph;Yuan, Hushan;Smith, Adam;Pacold, Michael E.;Weissleder, Ralph;Cantley, Lewis C.;Josephson, Lee;,期刊：Journal of Medicinal Chemistry, 页码：4699-4707 , 文章类型： 研究论文，,卷期：2008年51-15]
- When the viridin wortmannin (Wm) is modified by reaction with certain nucleophiles at the C20 position, the compds. obtained exhibit an improved antiproliferative activity even though a covalent reaction between C20 and ...
- Synthesis and Evaluation of Technetium-99m- and Rhenium-Labeled Inhibitors of the Prostate-Specific Membrane Antigen (PSMA).
[作者：Banerjee, Sangeeta R.;Foss, Catherine A.;Castanares, Mark;Mease, Ronnie C.;Byun, Youngjoo;Fox, James J.;Hilton, John;Lupold, Shawn E.;Kozikowski, Alan P.;Pomper, Martin G.;,期刊：Journal of Medicinal Chemistry, 页码：4504-4517 , 文章类型： 研究论文，,卷期：2008年51-15]
- The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. We prepd. seven 99mTc/Re-labeled compds. by attaching known Tc/Re chelating agents to an ami...
- Central Metal Determines Pharmacokinetics of Chlorophyll-Derived Xenobiotics.
[作者：Szczygiel, Malgorzata;Urbanska, Krystyna;Jurecka, Patrycja;Stawoska, Iwona;Stochel, Grazyna;Fiedor, Leszek;,期刊：Journal of Medicinal Chemistry, 页码：4412-4418 , 文章类型： 研究论文，,卷期：2008年51-15]
- Chlorophyll derivs. are potentially dangerous xenobiotics of dietary origin. The interactions of water-sol. derivs. of chlorophyll a with the animal organism were investigated using chlorophyllide a and its Zn-substitut...
- Highly Specific and Broadly Potent Inhibitors of Mammalian Secreted Phospholipases A2.
[作者：Oslund, Rob C.;Cermak, Nathan;Gelb, Michael H.;,期刊：Journal of Medicinal Chemistry, 页码：4708-4714 , 文章类型： 研究论文，,卷期：2008年51-15]
- We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor. Using the human g...
- Design of a Sialylglycopolymer with a Chitosan Backbone Having Efficient Inhibitory Activity against Influenza Virus Infection.
[作者：Umemura, Myco;Itoh, Masae;Makimura, Yutaka;Yamazaki, Kohji;Umekawa, Midori;Masui, Ayano;Matahira, Yoshiharu;Shibata, Mari;Ashida, Hisashi;Yamamoto, Kenji;,期刊：Journal of Medicinal Chemistry, 页码：4496-4503 , 文章类型： 研究论文，,卷期：2008年51-15]
- We verified here the inhibitory activity of a sialylglycopolymer prepd. from natural products, chitosan and hen egg yolk, against influenza virus infection and estd. the requirements of the mol. for efficient inhibition....
- Discovery of (-)-7-Methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo [2.2.1]heptane, a Radiolabeled Antagonist for Cerebral Nicotinic Acetylcholine Receptor (a4b2-nAChR) with Optimal Positron Emission Tomography Imaging Properties.
[作者：Gao, Yongjun;Kuwabara, Hiroto;Spivak, Charles E.;Xiao, Yingxian;Kellar, Kenneth;Ravert, Hayden T.;Kumar, Anil;Alexander, Mohab;Hilton, John;Wong, Dean F.;Dannals, Robert F.;Horti, Andrew G.;,期刊：Journal of Medicinal Chemistry, 页码：4751-4764 , 文章类型： 研究论文，,卷期：2008年51-15]
- Several isomers of 7-methyl-2-exo-([18F]fluoropyridinyl-5'-pyridinyl)-7-azabicyclo[2.2.1]hept ane have been developed as radioligands with optimized brain kinetics for PET imaging of nAChR. The binding assay demonstrate...
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