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Daniel Zimmerli

Explore the profile of Daniel Zimmerli including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 12
Citations 192
Followers 0
Related Specialties
Chemistry
Biochemistry
Pharmacology
Top 10 Co-Authors
Synese Jolidon
Daniela Alberati
Emmanuel Pinard
Holger Fischer
Dominik Hainzl
Bjorn Wagner
Francois Diederich
Anke Kurt
Manfred Kansy
Klaus Muller
Published In
Bioorg Med Chem Lett
ChemMedChem
Chemistry
J Med Chem
Angew Chem Int Ed Engl
Affiliations
Soon will be listed here.
Recent Articles
1.
Sugar Acetonides are a Superior Motif for Addressing the Large, Solvent-Exposed Ribose-33 Pocket of tRNA-Guanine Transglycosylase
Movsisyan L, Schafer E, Nguyen A, Ehrmann F, Schwab A, Rossolini T, et al.
Chemistry . 2018 Jun; 24(39):9957-9967. PMID: 29939431
The intestinal disease shigellosis caused by Shigella bacteria affects over 120 million people annually. There is an urgent demand for new drugs as resistance against common antibiotics emerges. Bacterial tRNA-guanine...
2.
Effect of Partially Fluorinated N-Alkyl-Substituted Piperidine-2-carboxamides on Pharmacologically Relevant Properties
Vorberg R, Trapp N, Zimmerli D, Wagner B, Fischer H, Kratochwil N, et al.
ChemMedChem . 2016 Sep; 11(19):2216-2239. PMID: 27629993
The modulation of pharmacologically relevant properties of N-alkyl-piperidine-2-carboxamides was studied by selective introduction of 1-3 fluorine atoms into the n-propyl and n-butyl side chains of the local anesthetics ropivacaine and...
3.
Fluorination Patterning: A Study of Structural Motifs That Impact Physicochemical Properties of Relevance to Drug Discovery
Huchet Q, Kuhn B, Wagner B, Kratochwil N, Fischer H, Kansy M, et al.
J Med Chem . 2015 Nov; 58(22):9041-60. PMID: 26523333
The synthesis of a collection of 3-substituted indole derivatives incorporating partially fluorinated n-propyl and n-butyl groups is described along with an in-depth study of the effects of various fluorination patterns...
4.
Replacement of water molecules in a phosphate binding site by furanoside-appended lin-benzoguanine ligands of tRNA-guanine transglycosylase (TGT)
Barandun L, Ehrmann F, Zimmerli D, Immekus F, Giroud M, Grunenfelder C, et al.
Chemistry . 2014 Dec; 21(1):126-35. PMID: 25483606
The enzyme tRNA-guanine transglycosylase has been identified as a drug target for the foodborne illness shigellosis. A key challenge in structure-based design for this enzyme is the filling of the...
5.
Strain-accelerated formation of chiral, optically active buta-1,3-dienes
Chiu M, Tchitchanov B, Zimmerli D, Sanhueza I, Schoenebeck F, Trapp N, et al.
Angew Chem Int Ed Engl . 2014 Nov; 54(1):349-54. PMID: 25425560
The formal [2+2] cycloaddition-retroelectrocyclization (CA-RE) reactions between tetracyanoethylene (TCNE) and strained, electron-rich dibenzo-fused cyclooctynes were studied. The effect of ring strain on the reaction kinetics was quantified, revealing that the...
6.
Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors
Pinard E, Alberati D, Bender M, Borroni E, Brom V, Burner S, et al.
Bioorg Med Chem Lett . 2010 Oct; 20(23):6960-5. PMID: 20974532
Benzoylisoindolines were discovered as a novel structural class of GlyT1 inhibitors. SAR studies and subsequent lead optimization efforts focused primarily on addressing hERG liability and on improving in vivo efficacy...
7.
Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia
Pinard E, Alanine A, Alberati D, Bender M, Borroni E, Bourdeaux P, et al.
J Med Chem . 2010 May; 53(12):4603-14. PMID: 20491477
The GlyT1 transporter has emerged as a key novel target for the treatment of schizophrenia. Herein, we report on the optimization of the 2-alkoxy-5-methylsulfonebenzoylpiperazine class of GlyT1 inhibitors to improve...
8.
Predicting and tuning physicochemical properties in lead optimization: amine basicities
Morgenthaler M, Schweizer E, Hoffmann-Roder A, Benini F, Martin R, Jaeschke G, et al.
ChemMedChem . 2007 May; 2(8):1100-15. PMID: 17530727
This review describes simple and useful concepts for predicting and tuning the pK(a) values of basic amine centers, a crucial step in the optimization of physical and ADME properties of...
9.
4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters
Alberati D, Hainzl D, Jolidon S, Kurt A, Pinard E, Thomas A, et al.
Bioorg Med Chem Lett . 2006 Jun; 16(16):4321-5. PMID: 16762550
A novel class of 4-substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-ones have been discovered and developed as potent and selective GlyT1 inhibitors. The molecules are devoid of activity at the GlyT2 isoform and display excellent selectivities...
10.
Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors
Alberati D, Ceccarelli S, Jolidon S, Krafft E, Kurt A, Maier A, et al.
Bioorg Med Chem Lett . 2006 Jun; 16(16):4305-10. PMID: 16762548
A novel class of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-ones have been discovered and developed as potent and selective GlyT1 inhibitors. The molecules are devoid of activity at the GlyT2 isoform and display excellent selectivities...