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Editor-in-Chief: Natalia Ortúzar
Impact Factor: 3.046
ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 74/254 (Pharmacology & Pharmacy)
Online ISSN: 1860-7187
August 21, 2014
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Recently Published Articles
- Position and Length of Fatty Acids Strongly Affect Receptor Selectivity Pattern of Human Pancreatic Polypeptide Analogues
Veronika Mäde, Dr. Kathrin Bellmann-Sickert, Anette Kaiser, Prof. Dr. Jens Meiler and Prof. Dr. Annette G. Beck-Sickinger
Article first published online: 22 AUG 2014 | DOI: 10.1002/cmdc.201402235
Fatty acids against obesity: Pancreatic polypeptide was lipidated at different sites using diverse fatty acid lengths to improve its stability and selectivity for prospective anti-obesity therapy. [K30(E-Prop)]hPP2−36 (15) was uncovered as a new ligand with superior Y receptor selectivity and enhanced in vitro stability.
- Structure-Guided Design of Thiazolidine Derivatives as Mycobacterium tuberculosis Pantothenate Synthetase Inhibitors
Parthiban Brindha Devi, Ganesh Samala, Jonnalagadda Padma Sridevi, Shalini Saxena, Mallika Alvala, Elena G. Salina, Prof. Dharmarajan Sriram and Prof. Perumal Yogeeswari
Article first published online: 22 AUG 2014 | DOI: 10.1002/cmdc.201402171
Let sleeping cells lie: Mycobacterium tuberculosis pantothenate synthetase (Mtb PS) has become a target for new therapeutics to treat tuberculosis. Nanomolar thiazolidine inhibitors of Mtb PS were developed by rational inhibitor design involving modelling, in vitro screening and optimisation. Hit expansion of the lead by synthesis led to an improved inhibitor with an IC50 value of 350 nM and an Mtb MIC value of 1.55 μM. Some of these compounds also showed good activity against dormant Mtb cells.
- Synthesis and Structure–Activity Relationship Studies of 2-(1,3,4-Oxadiazole-2(3H)-thione)-3-amino-5-arylthieno[2,3-b]pyridines as Inhibitors of DRAK2
Dr. Piotr Leonczak, Dr. Ling-Jie Gao, Dr. Anna Teresa Ramadori, Prof. Eveline Lescrinier, Prof. Jef Rozenski, Dr. Steven De Jonghe and Prof. Piet Herdewijn
Article first published online: 21 AUG 2014 | DOI: 10.1002/cmdc.201402234
Autoimmunity rejected: Efforts to improve the potency of a benzothiophene analogue for its DRAK2 inhibitory activity afforded a series of 2-(1,3,4-oxadiazole-2(3H)-thione)-3-amino-5-arylthieno[2,3-b]pyridines with high affinity for DRAK2. Moreover, our results show that these compounds are endowed with functional, inhibitory DRAK2 activity.
- Structure–Activity Relationship, Biological, and Pharmacological Characterization of the Proline Sulfonamide ACT-462206: a Potent, Brain-Penetrant Dual Orexin 1/Orexin 2 Receptor Antagonist
Dr. Christoph Boss, Dr. Catherine Roch-Brisbare, Dr. Michel A. Steiner, Dr. Alexander Treiber, Dr. Hendrik Dietrich, Dr. Francois Jenck, Dr. Markus von Raumer, Dr. Thierry Sifferlen, Dr. Christine Brotschi, Dr. Bibia Heidmann, Dr. Jodi Williams, Dr. Hamed Aissaoui, Dr. Romain Siegrist and Dr. John Gatfield
Article first published online: 21 AUG 2014 | DOI: 10.1002/cmdc.201402258
Rest assured: Orexin neuropeptides (orexins A and B) and their receptors (orexin 1 and 2) are heavily involved in the regulation of arousal, wakefulness, and stress. We describe the effects of a dual competitive brain-penetrant orexin receptor antagonist, represented by the proline sulfonamide based compound ACT-462206 (24), in rat and dog sleep experiments as well as stress and anxiety-related pharmacological settings.
- Non-natural Acetogenin Analogues as Potent Trypanosoma brucei Inhibitors
Dr. Gordon J. Florence, Andrew L. Fraser, Dr. Eoin R. Gould, Elizabeth F. B. King, Stefanie K. Menzies, Dr. Joanne C. Morris, Dr. Lindsay B. Tulloch and Prof. Terry K. Smith
Article first published online: 21 AUG 2014 | DOI: 10.1002/cmdc.201402272
Sleeping sickness under fire: A series of novel bis-tetrahydropyran 1,4-triazole analogues based on the acetogenin framework display low micromolar trypanocidal activities towards both bloodstream and insect forms of Trypanosoma brucei, the causative agent of African sleeping sickness.