Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Editor-in-Chief: Natalia Ortúzar
Impact Factor: 3.046
ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 75/256 (Pharmacology & Pharmacy)
Online ISSN: 1860-7187
December 22, 2014
Editor's Picks: Issue 01/2015
As part of ChemMedChem's Volume 10 celebrations, our Editor will select two articles per issue of particular interest, highlighting them in the Table of Contents. These articles will be free to access for the month of the issue, so sign up for e-mail alerts or follow us on Facebook or Twitter to avoid missing out!
Editor's picks for issue 01: A Communication by Renslo et al. and a Full Paper by Douse, Tate, and co-workers highlight the importance of continued drug discovery efforts against malaria. Read more...
Recently Published Articles
- Novel Tacrine-Grafted Ugi Adducts as Multipotent Anti-Alzheimer Drugs: A Synthetic Renewal in Tacrine–Ferulic Acid Hybrids
Mohamed Benchekroun, Dr. Manuela Bartolini, Dr. Javier Egea, Dr. Alejandro Romero, Dr. Elena Soriano, Dr. Marc Pudlo, Vincent Luzet, Prof. Vincenza Andrisano, Dr. María-Luisa Jimeno, Dr. Manuela G. López, Sarah Wehle, Prof. Tijani Gharbi, Prof. Bernard Refouvelet, Lucía de Andrés, Clara Herrera-Arozamena, Prof. Barbara Monti, Prof. Maria Laura Bolognesi, Prof. María Isabel Rodríguez-Franco, Prof. Dr. Michael Decker, Prof. José Marco-Contelles and Dr. Lhassane Ismaili
Article first published online: 23 DEC 2014 | DOI: 10.1002/cmdc.201402409
Multicomponent reaction for a multifactorial disease: new multipotent tacrine–ferulic acid hybrids (TFAHs) were synthesized by the Ugi four-component reaction and evaluated in vitro for the treatment of Alzheimer’s disease. Among them, TFAH 10 n was found to selectively inhibit human butyrylcholinesterase. It also demonstrated good profiles in terms of toxicity, neuroprotection, antioxidant, and blood–brain barrier penetration.
- You have free access to this contentChemMedChem has reached…The Big TEN! (pages 11–15)
Dr. Scott D. Williams and Dr. Natalia Ortúzar
Article first published online: 23 DEC 2014 | DOI: 10.1002/cmdc.201402483
Hitting double figures! ChemMedChem has entered its 10th volume. In this Editorial, read about the journal's activities and find out more about the people behind it. Over the course of the year ahead, keep an eye out for more heavyhitting special issues, opinion pieces by ChemMedChem Board members, as well as Editor's Picks: articles deemed particularly notable, which will be free to access while the issue is current. Enjoy volume 10!
- “Squalenoylcurcumin” Nanoassemblies as Water-Dispersible Drug Candidates with Antileishmanial Activity
Dr. Zakaria Cheikh-Ali, Dr. Joachim Caron, Dr. Sandrine Cojean, Dr. Christian Bories, Prof. Patrick Couvreur, Prof. Philippe M. Loiseau, Dr. Didier Desmaële, Prof. Erwan Poupon and Prof. Pierre Champy
Article first published online: 18 DEC 2014 | DOI: 10.1002/cmdc.201402449
Curing with curcumin: Two squalenoyl conjugates of the dietary polyphenol curcumin were synthesized by esterification of one or two phenol groups. The polyisoprenoyl appendage allowed self-assembly into nanoparticles 100–150 nm in size that are dispersible in water, show better activity against Leishmania donovani promastigotes than curcumin, and are active against intramacrophagic amastigotes.
- Discovery of Mono- and Disubstituted 1H-Pyrazolo[3,4]pyrimidines and 9H-Purines as Catalytic Inhibitors of Human DNA Topoisomerase IIα
Barbara Pogorelčnik, Dr. Matjaž Brvar, Prof. Bojana Žegura, Prof. Metka Filipič, Prof. Tom Solmajer and Prof. Andrej Perdih
Article first published online: 17 DEC 2014 | DOI: 10.1002/cmdc.201402459
Anticancer target revisited: In a two-stage virtual screening campaign, we discovered novel catalytic inhibitors that target the human DNA topoisomerase IIα ATP binding site. The binding of a new class of pyrazolopyrimidines was fully characterized by surface plasmon resonance experiments. In subsequent optimization, compounds with promising cytotoxicity against HepG2 and MCF-7 cancer cell lines were identified.
- Rational Design, Synthesis, and Biological Evaluation of Lactam-Bridged Gramicidin A Analogues: Discovery of a Low-Hemolytic Antibacterial Peptide
Dr. Ji Mao, Dr. Takefumi Kuranaga, Dr. Hiroshi Hamamoto, Prof. Dr. Kazuhisa Sekimizu and Prof. Dr. Masayuki Inoue
Article first published online: 15 DEC 2014 | DOI: 10.1002/cmdc.201402473
Channel your inner helix: The antibiotic gramicidin A (GA) folds into a β6.3 helix and functions as an ion channel in the cell membrane. We describe the rational design, synthesis, and biological evaluation of lactam-bridged GA analogues. One of them, with a 27-membered macrolactam ring, not only adopts a stable β6.3-helical conformation, but also exhibits high antibacterial activity and significantly decreased hemolytic/cytotoxic activities. This study charts a rational path forward for the development of new ion-channel-based antibiotics.