- Discovery of Orally Bioavailable 1,3,4-Trisubstituted 2-Oxopiperazine-Based Melanocortin-4 Receptor Agonists as Potential Antiobesity Agents.
[作者:Tian, Xinrong;Switzer, Adrian G.;Derose, Steve A.;Mishra, Rajesh K.;Solinsky, Mark G.;Mumin, Rashid N.;Ebetino, Frank H.;Jayasinghe, Lalith R.;Webster, Mark E.;Colson, Anny-Odile;Crossdoersen, Doreen;Pinney, Beth B.;Farmer, Julie A.;Dowty, Martin E.;Obrin,期刊:Journal of Medicinal Chemistry, 页码:6055-6066 , 文章类型: 研究论文,,卷期:2008年51-19]
- basic guanidine moiety contained in potent MC4R agonists, as exemplified by 1, led to the discovery of initial nonguanidine lead 5. Pr analog 23 was subsequently found to be equipotent to 5, whereas analogs bearing smal...
- 2-Aminothienopyridazines as Novel Adenosine A1 Receptor Allosteric Modulators and Antagonists.
[作者:Ferguson, Gemma N.;Valant, Celine;Horne, James;Figler, Heidi;Flynn, Bernard L.;Linden, Joel;Chalmers, David K.;Sexton, Patrick M.;Christopoulos, Arthur;Scammells, Peter J.;,期刊:Journal of Medicinal Chemistry, 页码:6165-6172 , 文章类型: 研究论文,,卷期:2008年51-19]
- A pharmacophore-based screen identified 32 compds. including Et 5-amino-3-(4-tert-butylphenyl)-4-oxo-3,4-dihydrothieno[3,4-d]pyridazine -1-carboxylate [I, (R = 4-tert-Bu)] as a new allosteric modulator of the adenosine A...
- Whole structure-activity relationships of the fat-accumulation inhibitor (-)-ternatin: Recognition of the importance of each amino acid residue.
[作者:Shimokawa, Kenichiro;Iwase, Yoshiaki;Miwa, Ryoka;Yamada, Kaoru;Uemura, Daisuke;,期刊:Journal of Medicinal Chemistry, 页码:5912-5914 , 文章类型: 研究论文,,卷期:2008年51-19]
- A series of Ala and Aoc (Ala = alanine; Aoc = 2-aminooctane carboxylic acid) analogs of (-)-ternatin were prepd., and their bioactivities were assessed by a fat-accumulation inhibition assay using 3T3-L1 adipocytes, whic...
- Potent, Orally Bioavailable Delta Opioid Receptor Agonists for the Treatment of Pain: Discovery of N,N-Diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamid e (ADL5859).
[作者:Le Bourdonnec, Bertrand;Windh, Rolf T.;Ajello, Christopher W.;Leister, Lara K.;Gu, Minghua;Chu, Guo-Hua;Tuthill, Paul A.;Barker, William M.;Koblish, Michael;Wiant, Daniel D.;Graczyk, Thomas M.;Belanger, Serge;Cassel, Joel A.;Feschenko, Marina S.;Brogdon,,期刊:Journal of Medicinal Chemistry, 页码:5893-5896 , 文章类型: 研究论文,,卷期:2008年51-19]
- Selective d opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic deriv. was identified as a promising hit through screening. Subsequent ...
- Structure-Activity Relationship Studies for the Peptide Portion of the Bladder Epithelial Cell Antiproliferative Factor from Interstitial Cystitis Patients.
[作者:Kaczmarek, Piotr;Keay, Susan K.;Tocci, Gillian M.;Koch, Kristopher R.;Zhang, Chen-Ou;Barchi, Joseph J., Jr.;Grkovic, David;Guo, Li;Michejda, Christopher J.;,期刊:Journal of Medicinal Chemistry, 页码:5974-5983 , 文章类型: 研究论文,,卷期:2008年51-19]
- We performed comprehensive structure-activity relationship (SAR) studies on the peptide portion of antiproliferative factor (APF), a sialylated frizzled-8 related glycopeptide that inhibits normal bladder epithelial and ...
- Discovery of Biphenyl Piperazines as Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists.
[作者:Jin, Jian;Budzik, Brian;Wang, Yonghui;Shi, Dongchuan;Wang, Feng;Xie, Haibo;Wan, Zehong;Zhu, Chongye;Foley, James J.;Webb, Edward F.;Berlanga, Manuela;Burman, Miriam;Sarau, Henry M.;Morrow, Dwight M.;Moore, Michael L.;Rivero, Ralph A.;Palovich, Michael;Sal,期刊:Journal of Medicinal Chemistry, 页码:5915-5918 , 文章类型: 研究论文,,卷期:2008年51-19]
- A series of novel biphenyl piperazines was discovered as highly potent muscarinic acetylcholine receptor antagonists via high throughput screening and subsequent optimization. Compd. (I) with resp. 500- and 20-fold subt...
- Structure-Activity Relationship Anatomy by Network-like Similarity Graphs and Local Structure-Activity Relationship Indices.
[作者:Wawer, Mathias;Peltason, Lisa;Weskamp, Nils;Teckentrup, Andreas;Bajorath, Juergen;,期刊:Journal of Medicinal Chemistry, 页码:6075-6084 , 文章类型: 研究论文,,卷期:2008年51-19]
- The study of structure-activity relationships (SARs) of small mols. is of fundamental importance in medicinal chem. and drug design. Here, we introduce an approach that combines the anal. of similarity-based mol. networ...
- Heteroarylnitrones as Drugs for Neurodegenerative Diseases: Synthesis, Neuroprotective Properties, and Free Radical Scavenger Properties.
[作者:Porcal, Williams;Hernandez, Paola;Gonzalez, Mercedes;Ferreira, Ana;Olea-Azar, Claudio;Cerecetto, Hugo;Castro, Ana;,期刊:Journal of Medicinal Chemistry, 页码:6150-6159 , 文章类型: 研究论文,,卷期:2008年51-19]
- Compounds (More Than One Hetero Atom)) Section New 1,2,4-thiadiazolylnitrones and furoxanylnitrones were developed and evaluated as neuroprotective agents on a human neuroblastoma (SH-SY5Y) cells model. They inhibited a...
- Antitumor Compounds Based on a Natural Product Consensus Pharmacophore.
[作者:Lagisetti, Chandraiah;Pourpak, Alan;Jiang, Qin;Cui, Xiaoli;Goronga, Tinopiwa;Morris, Stephan W.;Webb, Thomas R.;,期刊:Journal of Medicinal Chemistry, 页码:6220-6224 , 文章类型: 研究论文,,卷期:2008年51-19]
- (Biomolecules and Their Synthetic Analogs) Section We report the design and highly enantioselective synthesis of a potent analog of the spliceosome inhibitor FR901464, based on a non-natural product scaffold. The design...
- Synthesis, Cytotoxicity, and Anti-Trypanosoma cruzi Activity of New Chalcones.
[作者:Aponte, Jose C.;Verastegui, Manuela;Malaga, Edith;Zimic, Mirko;Quiliano, Miguel;Vaisberg, Abraham J.;Gilman, Robert H.;Hammond, Gerald B.;,期刊:Journal of Medicinal Chemistry, 页码:6230-6234 , 文章类型: 研究论文,,卷期:2008年51-19]
- (Biomolecules and Their Synthetic Analogs) Section Synthesis of a cytotoxic dihydrochalcone, first isolated from a traditional Amazonian medicinal plant Iryanthera juruensis Warb (Myristicaceae), followed by a comprehens...
- Design, Synthesis, and Structure-Activity Relationships of Novel Insulin Receptor Tyrosine Kinase Activators.
[作者:Lum, Robert T.;Cheng, Mingshan;Cristobal, Cristina P.;Goldfine, Ira D.;Evans, Joseph L.;Keck, James G.;Macsata, Robert W.;Manchem, Vara Prasad;Matsumoto, Yukiharu;Park, Sophia J.;Rao, Sandhya S.;Robinson, Louise;Shi, Songyuan;Spevak, Wayne R.;Schow, Steve,期刊:Journal of Medicinal Chemistry, 页码:6173-6187 , 文章类型: 研究论文,,卷期:2008年51-19]
- A novel series of sym. ureas of [(7-amino(2-naphthyl))sulfonyl]phenylamines, e.g., I, were designed, synthesized, and tested for their ability to increase glucose transport in mouse 3T3-L1 adipocytes, a surrogate readout...
- Discovery of Inhibitors of Escherichia coli Methionine Aminopeptidase with the Fe(II)-Form Selectivity and Antibacterial Activity.
[作者:Wang, Wen-Long;Chai, Sergio C.;Huang, Min;He, Hong-Zhen;Hurley, Thomas D.;Ye, Qi-Zhuang;,期刊:Journal of Medicinal Chemistry, 页码:6110-6120 , 文章类型: 研究论文,,卷期:2008年51-19]
- Derivatives, and Condensed Benzenoid Compounds) Section Methionine aminopeptidase (MetAP) is a promising target to develop novel antibiotics, because all bacteria express MetAP from a single gene that carries out the ess...
- Biotin Sulfone as a New Tool for Synthetic Oligosaccharide Immobilization: Application to Multiple Analysis Profiling and Surface Plasmonic Analysis of Anti-Candida albicans Antibody Reactivity against a and b (1?) Oligomannosides.
[作者:Collot, Mayeul;Sendid, Boualem;Fievez, Aurelie;Savaux, Camille;Standaert-Vitse, Annie;Tabouret, Marc;Drucbert, Anne Sophie;Danze, Pierre Marie;Poulain, Daniel;Mallet, Jean-Maurice;,期刊:Journal of Medicinal Chemistry, 页码:6201-6210 , 文章类型: 研究论文,,卷期:2008年51-19]
- and basic anal. of yeast-related pathogenic mechanisms, a library of 1? oligomannosides suitable for immunoanal. was prepd. The use of biotin sulfone, an oxidized form of biotin, offers a convenient soln. for both oligo...
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