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MedChemComm

Broadening the field of opportunity for medicinal chemists. Official journal of the European Federation for Medicinal Chemistry
Impact Factor 2.626 12 Issues per Year
 
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Yong Luo, Yongxia Zhu, Kai Ran, Zhihao Liu, Ningyu Wang, Qiang Feng, Jun Zeng, Lidan Zhang, Bing He, Tinghong Ye, Shirui Zhu, Xiaolong Qiu and Luoting Yu
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00573B, Concise Article
In this study, a series of novel N-(4-phenylthiazol-2-yl)-cinnamamide derivatives (7a–8n) were synthesized and evaluated for their anti-proliferative activities in vitro.
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00042D, Concise Article
The sodium 3-(4-nitro-1H-imidazolyl)propyl dithiocarbamate (N4IPDTC) was synthesized and radiolabelled with [99mTcO]3+, [99mTc≡N]2+ and [99mTc(CO)3]+cores to produce 99mTcO-N4IPDTC ,99mTcN-N4IPDTC and 99mTc(CO)3-N4IPDTC, respectively. All of the three complexes were prepared with high...
 
Shilva Kayastha, Antonio de la Vega de León, Dilyana Dimova and Jürgen Bajorath
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00051C, Concise Article
Ionization states within a chemical neighborhood. Shown are an acidic and a basic analog of a neutral compound.
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00148J, Concise Article
The phenol of 1-(3-(1H-imidazol-1-yl)propyl)-3-(4-hydroxy-3-methoxyphenyl)thiourea was selectively carbon-11 labelled to generate [11C]PBD150 in 7.3% yield from [11C]methyl triflate (non-decay corrected; radiochemical purity ≥95%, specific activity = 5.7 Ci/µmol, n=5). Evaluation of...
 
Jodi Williams, John Gatfield, Catherine Roch, Alexander Treiber, Francois Jenck, Martin Bolli, Christine Brotschi, Thierry Sifferlen, Bibia Heidmann and Christoph Boss
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00074B, Concise Article
Starting from a thienopiperidine lead compound with high intrinsic clearance in rat and human liver microsomes, and low aqueous solubility, a novel series of 1-acyl-2-benzylpyrrolidines were discovered as potent and...
 
Fang Xie, Torsten Kniess, Christin Neuber, Winnie Deuther-Conrad, Constantin Mamat, Brian P. Lieberman, BL Liu, Robert Henry Mach, Peter Brust, Jörg Steinbach, Jens Pietzsch and Hongmei Jia
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00079C, Concise Article
We report the synthesis and biological evaluation of a series of indole-based σ2 receptor ligands derived from siramesine. In vitro competition binding assays showed that these analogues possessed high to...
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00016E, Concise Article
From themed collection Identification and Optimization of GPCR Ligands in the 21st Century
Adenosine is a naturally occurring purine nucleoside that exerts a variety of important biological functions through the activation of four G protein-coupled receptors (GPCRs) isoforms, namely the A1, A2A, A2B...
 
Min Guo, Yue Zheng, Clement Opoku-Temeng, Rusty Starks, Xiaochu Ma and Herman O Sintim
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00015G, Concise Article
Synthetic molecules that modulate quorum sensing, QS, in bacteria have great potential to be used in synthetic biology applications as well as acting as anti-virulence and anti-biofilm agents. Acylhomoserine lactone...
 
Siti Munirah Mohd Faudzi, Sze Wei Leong, Faridah Abas, Mohd Fadhlizil Fasihi Mohd Aluwi, Kamal Rullah, Kok Wai Lam, Syahida Ahmad, Chau Ling Tham, Khozirah Shaari and Nordin H Lajis
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C4MD00541D, Concise Article
A series of forty-five 1,5-diphenylpenta-2,4-dien-1-one analogues were synthesized and evaluated for their nitric oxide (NO)-inhibition activity in IFN-γ/LPS-activated RAW 264.7 cells. Compounds 3h, 7a, 7d and 7e exhibited comparable or...
 
shupeng li, hailong zhang, Yuhua Jiang, Sheng-gang Zhao, Li-qin Jiang, Yan Meng, Peng Liu and Myeong Ok Kim
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00038F, Concise Article
Neuronal transmitters specifically recognize and bind to receptors and exert critical physical and pathological roles in neuronal functions. The possibility to use neurotransmitters as targeting ligand for central nervous system...
 
Michael J. Waring, David J. Baker, Stuart N. L. Bennett, Alexander G. Dossetter, Mark Fenwick, Rob Garcia, Jennie Georgsson, Sam D. Groombridge, Susan Loxham, Philip A. MacFaul, Katie G. Maskill, David Morgan, Jenny Morrell, Helen Pointon, Graeme R. Robb, David M. Smith, Stephen Stokes and Gary Wilkinson
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00037H, Concise Article
A series of 2-(pyridinyl)pyrimidines were identified as potent GPR40 antagonists.
 
Erik C. Hett, Eugene L. Piatnitski Chekler, Arindrajit Basak, Paul D. Bonin, R. Aldrin Denny, Andrew C. Flick, Kieran F. Geoghegan, Shenping Liu, Mathew T. Pletcher, Parag Sahasrabudhe, Shores C. Salter, Ingrid A. Stock, Alexandria P. Taylor and Lyn H. Jones
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00070J, Concise Article
Tropolone probes directly photoaffinity label bromodomains.
 
Enade P. Istyastono, Albert J. Kooistra, Henry F. Vischer, Martien Kuijer, Luc Roumen, Saskia Nijmeijer, Rogier A. Smits, Iwan J. P. de Esch, Rob Leurs and Chris de Graaf
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00022J, Concise Article
From themed collection Identification and Optimization of GPCR Ligands in the 21st Century
Structure-based virtual screening using H1R- and β2R-based histamine H4R homology models identified 9 fragments with an affinity ranging from 0.14 to 6.3 μm for H4R.
 
Fernanda Borges, Daniel Chavarria, Tiago Silva, Teresa Summavielle, Jorge M.P.J. Garrido, Daniel Martins and Joana Bravo
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00018A, Concise Article
New lipophilic hydroxycinnamic acid based derivatives were designed, synthesized and their antioxidant and neuroprotective activities evaluated. The chemical modification introduced in the cinnamic acid scaffold lead to compounds’ with an...
 
Zhan Wang, Qingkun Yang, Zhaoshi Bai, Jun Sun, Xuewei Jiang, Hongrui Song, Yingliang Wu and Weige Zhang
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00028A, Concise Article
A series of novel 2,3-diarylthiophene analogues of combretastatin A-4 were synthesised and evaluated for their in vitro anti-proliferative activities.
 
C. Lambertucci, M. Buccioni, D. Dal Ben, S. Kachler, G. Marucci, A. Spinaci, A. Thomas, K.-N. Klotz and R. Volpini
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00034C, Concise Article
From themed collection Identification and Optimization of GPCR Ligands in the 21st Century
New 9-propyladenines substituted at 2- or N6- and 8 positions behave as adenosine receptor antagonists with low nM affinity at the A2A subtype.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00007F, Concise Article
The impact of the configuration of enantiomeric diketopiperazines on the conformation, nanoimage, u-PA inhibition and anti-metastatic activity was explored.
 
John A. Christopher, Sarah J. Aves, Jason Brown, James C. Errey, Suki S. Klair, Christopher J. Langmead, Oliver J. Mace, Richard Mould, Jayesh C. Patel, Benjamin G. Tehan, Andrei Zhukov, Fiona H. Marshall and Miles Congreve
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00027K, Concise Article
From themed collection Identification and Optimization of GPCR Ligands in the 21st Century
A novel series of potent, selective, and orally efficacious dual antagonists of the orexin receptors is described.
 
Anna Charalambous, Maria Koyioni, Ioanna Antoniades, Despoina Pegeioti, Iro Eleftheriou, Sophia S. Michaelidou, Stanislav A. Amelichev, Lidia S. Konstantinova, Oleg A. Rakitin, Panayiotis A. Koutentis and Paris A. Skourides
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00052A, Concise Article
1,2,3-Dithiazolimines show potent and reversible inhibition of melanin synthesis in Xenopus laevis embryos.
 
Vijayanand Chandrasekaran, Shirin Kalyan, Valentina Biel, Marcus Lettau, Patrik Theodor Nerdal, Hans-Heinrich Oberg, Daniela Wesch, Thisbe K. Lindhorst and Dieter Kabelitz
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00063G, Concise Article
A novel fluorescent derivative of bisphosphonate zoledronate was synthesized and shown to have comparable functional activity as native zoledronate.
 
Graeme R. Robb, Scott Boyd, Christopher D. Davies, Alexander G. Dossetter, Frederick W. Goldberg, Paul D. Kemmitt, James S. Scott and John G. Swales
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00043B, Concise Article
Rapid and efficient lead optimisation through quantification of the molecular electrostatic potential using quantum mechanics.
 
Victoria A. Assimon, Hao Shao, Sylvie Garneau-Tsodikova and Jason E. Gestwicki
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00572D, Concise Article
There is a growing need to identify new, broad-spectrum antibiotics. Here, we report a concise route to an antibiotic based on the privileged structure of the natural product spergualin.
 
D. R. Vianna, L. Ruschel, F. Dietrich, F. Figueiró, F. B. Morrone, R. F. S. Canto, F. Corvello, A. Velho, A. Crestani, H. Teixeira, G. L. von Poser, A. M. O. Battastini and V. L. Eifler-Lima
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00039D, Concise Article
4-Methylcoumarins were synthesized by microwave-assisted synthesis via Pechmann condensation and their cytotoxic activity against human bladder cancer cell lines was investigated.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD90016F, Correction
 
M. A. Soriano-Ursúa, J. G. Trujillo-Ferrara, J. A. Arias-Montaño and R. Villalobos-Molina
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00011D, Review Article
From themed collection Identification and Optimization of GPCR Ligands in the 21st Century
Putative roles of a secondary binding region shared among beta-adrenoceptors.
 

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