Publication in J. Med. Chem. - Transmission Blocking Antimalarials

Our latest publication in J. Med. Chem. is online

Our research on 'Structure-Activity Relationship Studies of a Novel Class of Transmission Blocking Antimalarials Targeting Male Gametes' is out in the Journal of Medicinal Chemistry:

https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b00898

Malaria is still a leading cause of mortality among children in the developing world, and despite the immense progress made in reducing the global burden, further efforts are needed if eradication is to be achieved. In this context, targeting transmission is widely recognised as a necessary intervention toward that goal. After carrying out a screen to discover new transmission-blocking agents, herein we report our medicinal chemistry efforts to study the potential of the most robust hit, DDD01035881, as a male-gamete targeted compound. We reveal key structural features for the activity of this series and identify analogues with greater potency and improved metabolic stability. We believe this study lays the groundwork for further development of this series as a transmission blocking agent.

A large amount of the synthetic work in this paper was performed by Oliver Fischer during his Erasmus project in the group and the project was in collaboration with Professor Matthew Fuchter and Professor Jake Baum. Congratulations to everyone involved.