- Oxadiazole-carbonylaminothioureas as SIRT1 and SIRT2 Inhibitors.
[作者：Huhtiniemi, Tero;Suuronen, Tiina;Rinne, Valtteri M.;Wittekindt, Carsten;Lahtela-Kakkonen, Maija;Jarho, Elina;Wallen, Erik A. A.;Salminen, Antero;Poso, Antti;Leppanen, Jukka;,期刊：Journal of Medicinal Chemistry, 页码：4377-4380 , 文章类型： 研究论文，,卷期：2008年51-15]
- A new inhibitor for human sirtuin type proteins 1 and 2 (SIRT1 and SIRT2) was discovered through virtual database screening in search of new scaffolds. A series of compds. was synthesized based on the hit compd. (3-[[3-...
- Optimization of the Central Heterocycle of a-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase.
[作者：Garfunkle, Joie;Ezzili, Cyrine;Rayl, Thomas J.;Hochstatter, Dustin G.;Hwang, Inkyu;Boger, Dale L.;,期刊：Journal of Medicinal Chemistry, 页码：4392-4403 , 文章类型： 研究论文，,卷期：2008年51-15]
- The synthesis and evaluation of a refined series of a-ketoheterocycles (OL-135) incorporating systematic changes in the central heterocycle bearing a key set of added substituents are described. The nature of the centra...
- Synthesis, Structure-Activity Relationships, and Biological Profiles of a Quinazolinone Class of Histamine H3 Receptor Inverse Agonists.
[作者：Nagase, Tsuyoshi;Mizutani, Takashi;Ishikawa, Shiho;Sekino, Etsuko;Sasaki, Takahide;Fujimura, Takashi;Ito, Sayaka;Mitobe, Yuko;Miyamoto, Yasuhisa;Yoshimoto, Ryo;Tanaka, Takeshi;Ishihara, Akane;Takenaga, Norihiro;Tokita, Shigeru;Fukami, Takehiro;Sato, Nagaa,期刊：Journal of Medicinal Chemistry, 页码：4780-4789 , 文章类型： 研究论文，,卷期：2008年51-15]
- A new series of quinazolinone derivs. was synthesized and evaluated as nonimidazole H3 receptor inverse agonists. 2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-5-(trifluoromethyl)-4( 3H)-quinazolinone (I) was iden...
- Asymmetric Synthesis of 2,3-Dihydro-2-arylquinazolin-4-ones: Methodology and Application to a Potent Fluorescent Tubulin Inhibitor with Anticancer Activity.
[作者：Chinigo, Gary M.;Paige, Mikell;Grindrod, Scott;Hamel, Ernest;Dakshanamurthy, Sivanesan;Chruszcz, Maksymilian;Minor, Wladek;Brown, Milton L.;,期刊：Journal of Medicinal Chemistry, 页码：4620-4631 , 文章类型： 研究论文，,卷期：2008年51-15]
- For several decades the 2,3-dihydroquinazolinone (DHQZ) heterocycle has been known to possess a variety of important biol. and medicinal properties. Despite the many interesting facets of these mols., synthetic access t...
- Synthesis of New Arylpiperazinylalkylthiobenzimidazole, Benzothiazole, or Benzoxazole Derivatives as Potent and Selective 5-HT1A Serotonin Receptor Ligands.
[作者：Siracusa, Maria A.;Salerno, Loredana;Modica, Maria N.;Pittala, Valeria;Romeo, Giuseppe;Amato, Maria E.;Nowak, Mateusz;Bojarski, Andrzej J.;Mereghetti, Ilario;Cagnotto, Alfredo;Mennini, Tiziana;,期刊：Journal of Medicinal Chemistry, 页码：4529-4538 , 文章类型： 研究论文，,卷期：2008年51-15]
- A series of new compds. contg. a benzimidazole, benzothiazole, or benzoxazole nucleus linked to an arylpiperazine by different thioalkyl chains was prepd. They were tested in radioligand binding expts. to evaluate their...
- False Positives in a Reporter Gene Assay: Identification and Synthesis of Substituted N-Pyridin-2-ylbenzamides as Competitive Inhibitors of Firefly Luciferase.
[作者：Heitman, Laura H.;van Veldhoven, Jacobus P. D.;Zweemer, Annelien M.;Ye, Kai;Brussee, Johannes;IJzerman, Adriaan P.;,期刊：Journal of Medicinal Chemistry, 页码：4724-4729 , 文章类型： 研究论文，,卷期：2008年51-15]
- Luciferase reporter-gene assays are a commonly used technique in high-throughput screening campaigns. In this study, a luciferase inhibitor, 2-(benzoylamino)quinoline, which emerged from an antagonistic G protein-couple...
- Novel Quinolinonyl Diketo Acid Derivatives as HIV-1 Integrase Inhibitors: Design, Synthesis, and Biological Activities.
[作者：Di Santo, Roberto;Costi, Roberta;Roux, Alessandra;Miele, Gaetano;Crucitti, Giuliana Cuzzucoli;Iacovo, Alberto;Rosi, Federica;Lavecchia, Antonio;Marinelli, Luciana;Di Giovanni, Carmen;Novellino, Ettore;Palmisano, Lucia;Andreotti, Mauro;Amici, Roberta;Gallu,期刊：Journal of Medicinal Chemistry, 页码：4744-4750 , 文章类型： 研究论文，,卷期：2008年51-15]
- Novel quinolinonyl diketo acids were designed to obtain integrase (IN) inhibitors selectively active against the strand transfer (ST) step of the HIV integration process. Those new compds. are characterized by a single ...
- 2-Amino-6-furan-2-yl-4-substituted Nicotinonitriles as A2A Adenosine Receptor Antagonists.
[作者：Mantri, Monica;de Graaf, Olivier;van Veldhoven, Jacobus;Goeblyoes, Aniko;von Frijtag Drabbe Kuenzel, Jacobien K.;Mulder-Krieger, Thea;Link, Regina;de Vries, Henk;Beukers, Margot W.;Brussee, Johannes;IJzerman, Adriaan P.;,期刊：Journal of Medicinal Chemistry, 页码：4449-4455 , 文章类型： 研究论文，,卷期：2008年51-15]
- On the basis of a pharmacophore model designed by overlap of nonxanthine type of previously known A2A antagonists, a new class of compds. having a 2-amino nicotinonitrile core moiety, namely, 2-amino-4-R1-6-R2-nicotinoni...
- Antitumor Activity of Bis-indole Derivatives.
[作者：Andreani, Aldo;Burnelli, Silvia;Granaiola, Massimiliano;Leoni, Alberto;Locatelli, Alessandra;Morigi, Rita;Rambaldi, Mirella;Varoli, Lucilla;Landi, Laura;Prata, Cecilia;Berridge, Michael V.;Grasso, Carole;Fiebig, Heinz-Herbert;Kelter, Gerhard;Burger, Angel,期刊：Journal of Medicinal Chemistry, 页码：4563-4570 , 文章类型： 研究论文，,卷期：2008年51-15]
- The synthesis of compds. formed by two indole systems sepd. by a heterocycle (pyridine or piperazine) is reported. As a primary screening, the new compds. were submitted to the National Cancer Institute for evaluation o...
- Substituted 6-Phenyl-2-naphthols. Potent and Selective Nonsteroidal Inhibitors of 17b-Hydroxysteroid Dehydrogenase Type 1 (17b-HSD1): Design, Synthesis, Biological Evaluation, and Pharmacokinetics.
[作者：Marchais-Oberwinkler, Sandrine;Kruchten, Patricia;Frotscher, Martin;Ziegler, Erika;Neugebauer, Alexander;Bhoga, Umadevi;Bey, Emmanuel;Mueller-Vieira, Ursula;Messinger, Josef;Thole, Hubert;Hartmann, Rolf W.;,期刊：Journal of Medicinal Chemistry, 页码：4685-4698 , 文章类型： 研究论文，,卷期：2008年51-15]
- 17b-Estradiol (E2) is implicated in the genesis and the development of estrogen-dependent diseases. Its concn. is mainly regulated by 17b-hydroxysteroid dehydrogenase type 1 (17b-HSD1), which catalyzes the redn. of the ...
- Methyl (11aS)-1,2,3,5,11,11a-Hexahydro-3,3-dimethyl-1-oxo-6H-imidazo-[3',4' :1,2]pyridin[3,4-b]indol-2-Substituted Acetates: Synthesis and Three-Dimensional Quantitative Structure-Activity Relationship Investigation as a Class of Novel Vasodilators.
[作者：Liu, Jiawang;Zhao, Ming;Cui, Guohui;Zhang, Xiaoyi;Wang, Jun;Peng, Shiqi;,期刊：Journal of Medicinal Chemistry, 页码：4715-4723 , 文章类型： 研究论文，,卷期：2008年51-15]
- To find selective inhibitor of phosphodiesterase type 5 (PDE5), the essential structure elements of clin. used drugs sildenafil, vardenafil, and tadalafil were combined and a tetracyclic parent was constructed to which i...
- Novel Indoline-Based Acyl-CoA:Cholesterol Acyltransferase Inhibitor with Antiperoxidative Activity: Improvement of Physicochemical Properties and Biological Activities by Introduction of Carboxylic Acid.
[作者：Takahashi, Kenji;Kasai, Masayasu;Ohta, Masaru;Shoji, Yoshimichi;Kunishiro, Kazuyoshi;Kanda, Mamoru;Kurahashi, Kazuyoshi;Shirahase, Hiroaki;,期刊：Journal of Medicinal Chemistry, 页码：4823-4833 , 文章类型： 研究论文，,卷期：2008年51-15]
- (Heterocyclic Compounds (One Hetero Atom)) Section A series of novel indoline derivs. with an ionizable moiety were synthesized to find a bioavailable acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor with antiperoxi...
- Targeting the Lysosome: Fluorescent Iron(III) Chelators To Selectively Monitor Endosomal/Lysosomal Labile Iron Pools.
[作者：Fakih, Sarah;Podinovskaia, Maria;Kong, Xiaole;Collins, Helen L.;Schaible, Ulrich E.;Hider, Robert C.;,期刊：Journal of Medicinal Chemistry, 页码：4539-4552 , 文章类型： 研究论文，,卷期：2008年51-15]
- Iron-sensitive fluorescent chemosensors in combination with digital fluorescence spectroscopy have led to the identification of a distinct subcellular compartmentation of intracellular redox-active "labile" iron. To inve...
- Selectivity Determinants of Inhibitor Binding to Human 20a-Hydroxysteroid Dehydrogenase: Crystal Structure of the Enzyme in Ternary Complex with Coenzyme and the Potent Inhibitor 3,5-Dichlorosalicylic Acid.
[作者：Dhagat, Urmi;Endo, Satoshi;Sumii, Rie;Hara, Akira;El-Kabbani, Ossama;,期刊：Journal of Medicinal Chemistry, 页码：4844-4848 , 文章类型： 研究论文，,卷期：2008年51-15]
- The crystal structure of human 20a-hydroxysteroid dehydrogenase (AKR1C1) in ternary complex with the coenzyme NADP+ and the potent inhibitor 3,5-dichlorosalicylic acid was detd. at a resoln. of 1.8 ? The inhibitor is he...
- Structure of Daidzin, a Naturally Occurring Anti-Alcohol-Addiction Agent, in Complex with Human Mitochondrial Aldehyde Dehydrogenase.
[作者：Lowe, Edward D.;Gao, Guang-Yao;Johnson, Louise N.;Keung, Wing Ming;,期刊：Journal of Medicinal Chemistry, 页码：4482-4487 , 文章类型： 研究论文，,卷期：2008年51-15]
- The ALDH2*2 gene encoding the inactive variant form of mitochondrial aldehyde dehydrogenase (ALDH2) protects nearly all carriers of this gene from alcoholism. Inhibition of ALDH2 has hence become a possible strategy to ...
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