Journal cover: MedChemComm

MedChemComm

Broadening the field of opportunity for medicinal chemists. Official journal of the European Federation for Medicinal Chemistry
Impact Factor 2.722 12 Issues per Year
 
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R. Fanelli, A. S. Ressurreição, L. Dufau, J.-L. Soulier, A. Vidu, N. Tonali, G. Bernadat, M. Reboud-Ravaux and S. Ongeri
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00032C, Concise Article
A new series of naphthalene-based molecular tongs containing polar groups at the 3-position of the naphthalene scaffold was synthesized and its anti-dimerization activity was evaluated against HIV-1 protease.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00022F, Concise Article
A series of novel ligustrazine derivatives were designed, synthesized and evaluated for their anti-platelet activities and protection on Ea.hy926 cells against oxidative damage. Several compounds possessed high activities.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00053F, Concise Article
Through the use of chemical synthesis and high throughput screening, we discovered a sulfonamide hydroxamic acid inhibitor for the botulinum neurotoxin serotype A light chain. A structure activity relationship study of the parent inhibitor resulted in the synthesis of a new inhibitor with an IC50 of 0.95 ± 0.60 μM for the BoNT/A LC.
 
Prof. Athina Geronikaki , Konstantinos Liaras, Jasmina Glamocilija, Ana Ciric and Marina Sokovic
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00124A, Concise Article
A series of eight thiazole-based N-phenylpyrazolines and two aminopyrimidines having as precursors several chalcone derivatives have been synthesized and evaluated for their antimicrobial activity. All compounds showed antimicrobial activity. The...
 
silvia panseri, Laura Russo, Monica Montesi, Francesca Taraballi, Carla Cunha, Maurilio Marcacci and Laura Cipolla
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00112E, Concise Article
Osteogenic Growth Peptide (OGP) motifs were tethered to SULFHYDRYL-BIND™ polystyrene plates tuning spatial presentation of the different functional domains. The effect of the different surface-tethered OGP motifs have been evaluated...
 
VALESSA BARBIER, Michele Fiore, Nathalie Berthet and Olivier Renaudet
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00097H, Concise Article
For the first time, living Anionic Ring-Opening Polymerization (AROP) of disubstituted cyclopropane-1,1-dicarboxylates has been used together with thiol-ene addition to give new glycopolymers. Fully modified oligomers with single or geminal...
 
Jeremy N. Burrows, Richard L. Elliott, Takushi Kaneko, Charles E. Mowbray and David Waterson
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00011K, Review Article
The future of drug discovery for neglected and tropical diseases will depend on the ability of those working in the area to collaborate and will require sustained resourcing and focus.
 
Stephen Hanessian, Oscar M. Saavedra, Miguel A. Vilchis-Reyes and Ana M. Llaguno-Rueda
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00072B, Concise Article
The syntheses of 4′-deoxy-4′-fluoro neamine and 4′-deoxy-4′-fluoro 4′-epi neamine from the readily available neamine and paromamine are described.
 
Sophie Le Trionairre, Alexis Perry, Bartosz Szczesny, Szabo Csaba, Paul Winyard, Jacqueline Whatmore, Mark E. Wood and Matt Whiteman
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C3MD00323J, Concise Article
Synthesis and bioavailability of the endogenous gasomediator hydrogen sulfide (H2S) is perturbed in many disease states, including those involving mitochondrial dysfunction. There is intense interest in developing pharmacological agents to...
 
Weiwei Chen, Takahiko Matsushita, Dimitri Shcherbakov, Heithem Boukari, Andrea Vasella, Erik Bottger and D Crich
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00119B, Concise Article
A series of 4’-O-glycopyranosyl paromomycin analogs and a 4’-O-(glucosyloxymethyl) derivative were synthesized and evaluated for their ribosomal activity to determine the influence of the glycosyl moiety on drug activity and...
 
Christine Meck, Michael P. D'Erasmo, Danielle R. Hirsch and Ryan P. Murelli
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00055B, Review Article
α-Hydroxytropolones are promising leads for a diverse range of therapeutic applications. The following review will discuss the biological studies on α-hydroxytropolones and the synthetic methods available to access them.
 
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00094C, Concise Article
Dimerization is an essential step of the Hsp90 cycle. This work describes the results of a molecular dynamics and dimerization free energy analysis performed on the structure of the human...
 
Anne-Sophie Journé, Samy A.M. Habib, Bala R. Dodda, Mina N.F. Morcos, Mirna S. Sadek, Sarah A.A. Tadros, Paula Witt-Enderby, Ralf Jockers and Darius Paul Zlotos
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00079J, Concise Article
A novel series of dimeric melatonin analogues obtained by connecting two melatonin molecules through N1 with spacers of 15-24 atoms was synthesized and characterized in 2-[125-I]-iodomelatonin binding and bioluminescence resonance...
 
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00049H, Concise Article
Cortexolone-17α-propionate is a topical antiandrogen under investigation for the treatment of androgen related skin disorders. A full conformational characterization was realized, in comparison with others steroidal androgens and antiandrogens, by...
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00012A, Review Article
Infections caused by drug resistant and/or slow-growing bacteria are increasingly becoming some of the greatest challenges of health organizations worldwide.
 
Steffen van der Wal, Chantelle J. Capicciotti, Stamatia Rontogianni, Robert N. Ben and Rob M. J. Liskamp
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00013G, Concise Article
An azido/alkyne-containing glycopeptide monomer was synthesized and CuAAC-oligomerized to obtain a triazole-containing antifreeze glycopeptide analogue with moderate antifreeze activity.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00074A, Concise Article
The synthesis of 1-deoxynojirimycin (DNJ) derivatives, presenting a 2-naphthylmethyl and an alkyl amino side chain, from L-sorbose is described.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C3MD00346A, Review Article
Bacterial adhesion is an important first step towards bacterial infection and plays a role in colonization, invasion and biofilm formation.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00038B, Concise Article
Structural changes of PS A1 does not alter function.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00095A, Concise Article
Ten members of the mezzettiaside family of natural products were synthesized and evaluated for anticancer and antibacterial activity.
 
Lucas Cunha Duarte Coelho, Marcos Veríssimo de Oliveira Cardoso, Diogo Rodrigo Magalhães Moreira, Paulo André Teixeira de Moraes Gomes, Gevanio Bezerra de Oliveira Filho, Suellen Melo Tibúrcio Cavalcanti, Lucianna Rabelo Pessoa Siqueira, Miria de Oliveira Barbosa, Arsenio Rodrigues Oliveira, Elizabeth Fernanda de Oliveira Borba, Teresinha Gonçalves Silva, Belinda Kaskow, Mahdad Karimi, Lawrence J Abraham and Ana Cristina Lima Leite
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00070F, Concise Article
Modulation of the immune system is an emerging concept in the control of tumor growth. Bearing in mind the pharmacological property of Thalidomide and its phthalimide derivatives, we describe here...
 
Shuai Wang, David L Shen, Dominique Lafont, Anne-Sophie Vercoutter-Edouart, Marlène Mortuaire, Yun Shi, Ofelia Maniti, Agnes Girard-Egrot, Tony Lefebvre, B Mario Pinto, David Vocadlo and Sebastien Vidal
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00063C, Concise Article
Inhibition of glycosyltransferases calls for the design of neutral inhibitors to allow cell permeation in contrast to their natural dianionic substrates. O-GlcNAc Transferase (OGT) is a key enzyme involved in...
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00067F, Concise Article
The mycobacterial cell wall possesses a core galactan moiety composed of approximately 30 galactofuranosyl residues attached via alternating β-(1→5) and β-(1→6) linkages.
 
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00029C, Concise Article
Chemical changes leading to potency increases in structurally diverse active compounds were systematically explored. The analysis was facilitated through the application of the matched molecular pair formalism. From compounds with...
 
Arnout Voet, Akihiro Ito, Mikako Hirohama, Seiji Matsuoka, Naoya Tochio, Takanori Kigawa, Minoru Yoshida and Kam Y.J. Zhang
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C3MD00391D, Concise Article
The SUMO-SIM is a challenging protein-protein interaction drug target. We present a virtual screening approach incorporating the consensus of protein interactions that led to the discovery of non-peptidic inhibitors. The...
 

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