Technology ID
TAB-4848

Sidechain Functionalized S-Acylbenzamides With Anti-HIV Activity

E-Numbers
E-032-2023-0
Lead Inventor
Appella, Daniel (NIDDK)
Co-Inventors
Robello, Marco (NIDDK)
Development Stages
Discovery
Development Status
Preclinical /in vitro
ICs
NIDDK

HIV infection remains a major medical problem, with approximately 38 million people worldwide living
with HIV. Nipamovir and SAMT-247 are simple and inexpensive small molecules that inactivate HIV
virus by interference with final maturation steps of the virus. This mechanism provides a high barrier
for HIV to develop resistance. In fact, lab experiments designed to encourage HIV to develop
resistance to Nipamovir and SAMT-247 have all failed. In animal tests, Nipamovir and SAMT-247 do
not display toxic side effects. SAMT-247 is an effective microbicide that can be used to block HIV
infection in animal models. Both Nipamovir and SAMT-247 are rapidly metabolized in blood where
the sulfur of molecule is methylated, resulting in loss of antiviral activity. By attaching specific
sidechains to the S-acylbenzamide scaffold of Nipamovir and SAMT-247, NIDDK investigators have
developed new molecules that have improved anti-HIV activity and also are resistant to metabolism in
blood.

Licensing Contact:
Tong, Betty
tongb@niddk.nih.gov
Phone: 301-451-7836