Archive for November, 2011

HOT: acetylphosphonates inhibit DXP synthase in the MEP pathway

This hot article from Caren Freel Meyers and coworkers describes new inhibitors of DXP synthase, which catalyse an important precursor in the pathogen MEP pathway to isoprenoids.  Butylacetylphosphonate was able to selectively inhibit E. coli DXP synthase.

Selective inhibition of E. coli 1-deoxy-D-xylulose-5-phosphate synthase by acetylphosphonates
Jessica M. Smith, Ryan J. Vierling and Caren Freel Meyers
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C1MD00233C

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New antimalarial compounds: the class of 2011

In another step to overcome bacterial resistance to antibiotics, scientists from India have made a new class of triazines. Sixteen compounds showed excellent activity against malaria, say the researchers, preserving the potency of their parent antimalarial drug chloroquine. IC50 values ranged from 1.36 to 4.63ng ml-1.

Synthesis of hybrid 4-anilinoquinoline triazines as potent antimalarial agents, their in silico modeling and bioevaluation as Plasmodium falciparum transketolase and β-hematin inhibitors
Moni Sharma, Kuldeep Chauhan, Shikha S. Chauhan, Ashok Kumar, Shiv Vardan Singh, Jitendra K. Saxena, Pooja Agarwal, Kumkum Srivastava, S. Raja Kumar, Sunil K. Puri, Priyanka Shah, M. I. Siddiqi and Prem M. S. Chauhan
DOI: 10.1039/C1MD00188D

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Tracking immune cell migration on the cover of Issue 11

On the cover of Issue 11 is a hot article from Mark Bradley and coworkers on a method to track innate immune cell migration in vivo using dye-labelled peptoids.

Far red and NIR dye-peptoid conjugates for efficient immune cell labelling and tracking in preclinical models
Kevin Dhaliwal, Géraldine Escher, Asier Unciti-Broceta, Neil McDonald, A. John Simpson, Chris Haslett and Mark Bradley
Med. Chem. Commun., 2011, 2, 1050-1053
DOI: 10.1039/C1MD00171J

Also in this issue is Ying-Wei Yang’s review on biocompatible nanovalves for drug delivery and release:

Towards biocompatible nanovalves based on mesoporous silica nanoparticles
Ying-Wei Yang
Med. Chem. Commun., 2011, 2, 1033-1049
DOI: 10.1039/C1MD00158B

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