Jump to main content
Jump to site search
SCHEDULED MAINTENANCE Close the message box

Maintenance work is planned for Monday 16 August 2021 from 07:00 to 23:59 (BST).

Website performance may be temporarily affected and you may not be able to access some PDFs or images. If this does happen, refreshing your web browser should resolve the issue. We apologise for any inconvenience this might cause and thank you for your patience.


All chapters

CHAPTER 6

HIV Integrase Inhibitors

This chapter presents the discovery, development and evolution of integrase strand transfer inhibitors. A brief overview of the first‐generation inhibitors raltegravir and elvitegravir serves to describe their landmark advancement of the field and also outline areas for further improvement. The remainder of the discussion revolves around the strategy in designing a series of carbamoylpyridines that ultimately led to the discovery of dolutegravir, an investigational integrase inhibitor in late‐stage clinical development. In addition, an intriguing approach to the development of a related compound, S/GSK744, as a long‐acting parenteral agent is presented. Finally, an exciting new area of non‐catalytic site integrase inhibitors is included.

Publication details


Print publication date
10 Jun 2013
Copyright year
2013
Print ISBN
978-1-84973-657-2
PDF eISBN
978-1-84973-781-4
From the book series:
Drug Discovery