Non-nucleoside reverse transcriptase inhibitors (NNRTI) are potent
inhibitors of human immunodeficiency virus type 1 (HIV-1). They inhibit
the reverse transcriptase of HIV-1 and have the advantage of being less
toxic than other antiviral agents, especially the protease inhibitors.
The currently marketed NNRTI are nevirapine, delavirdine and
efavirenz. We have developed 2-pyridinone analogues as a new
class of anti-HIV, targeting, in common with other NNRTI, the
hydrophobic pocket of reverse transcriptase. Our leader compound is
active against WT enzyme and against HIV strains bearing mutation in
RT, wich are clinically relevant. Our most promising compound is
actually as or more active than efavirenz against our panel of
resistant strains. Our compounds are minimally toxic to cells and this
translate into very high selectivity index.
AIDS, Virus, antiviral drug, reverse transcriptase, viral mutant,
pyridinone, non nucleosides
Due to its very high affinity and specificity, these inhibitors could
be used in the treatment of AIDS patients which have developed viral
mutants and are resistant to the conventional treatments.
Patent pending in Europe (EP1663977), US and Canada (CA2540329)
Available for license
Nicole MOGUILEVSKY, PhD
Technology Transfer Office
University of Namur
53 rue de Bruxelles
B-5000 Namur
BELGIUM
Phone: +32 81 72 50 47
Fax : +32 81 72 57 01
e-mail:
nicole.moguilevsky@fundp.ac.be
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