DABCO beta-Lactamse Inhibitors

It looks like not only the old BLI tazobactam (approved in 1993) found new combinations,  such as ceftolozane-tazobactam from Cubist, the new DABCO combinations are also getting approvals or progressing into clinical trials. AZ, Merck,  and now Roche (Fedora) are all in the game, is this a renaissance of the long-lasting field? Personally, my medchem project started with BLI on the old tazo-type structure 20 years ago (BMCL, 1995, 5, 1513-18) and also recently I worked on DABCO series (WO2013150296). It's a truly unique class of enzymes to design inhibitors around. 

NBTI Antibacterials

As a medicinal chemist who worked on the NBTI Antimicrobial Agents, I am really excited to see that GSK is still pushing a candidate forward for the treatment of conventional and biothreat pathogens, such as methicillin-resistant Staphylococcus aureus. Based on the pioneer works at GSK and Aventis in late 1990’s, the last fifteen years has witnessed extraordinary efforts from GSK, Aventis, Johnson and Johnson, Biovertis, AstraZeneca, Actelion, Toyama, Pfizer, Merck and Daiichi. There have accumulated well over 100 patents and patent applications. As many candidates failed to progress, the works out of a few hundred chemists worldwide are gradually getting to see the light. I hope that GSK2140944 will eventually make it, so that all our work will not be in vain! I draw a few representative structures to show the genuine creativity during these true international competitions. I also wish that the antibacterial world will see this kind of race again!