3 research outputs found
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus
Respiratory infections caused by human rhinovirus are responsible
for severe exacerbations of underlying clinical conditions such as
asthma in addition to their economic cost in terms of lost working
days due to illness. While several antiviral compounds for treating
rhinoviral infections have been discovered, none have succeeded, to
date, in reaching approval for clinical use. We have developed a potent,
orally available rhinovirus inhibitor <b>6</b> that has progressed
through early clinical trials. The compound shows favorable pharmacokinetic
and activity profiles and has a confirmed mechanism of action through
crystallographic studies of a rhinovirusācompound complex.
The compound has now progressed to phase IIb clinical studies of its
effect on natural rhinovirus infection in humans
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus
Respiratory infections caused by human rhinovirus are responsible
for severe exacerbations of underlying clinical conditions such as
asthma in addition to their economic cost in terms of lost working
days due to illness. While several antiviral compounds for treating
rhinoviral infections have been discovered, none have succeeded, to
date, in reaching approval for clinical use. We have developed a potent,
orally available rhinovirus inhibitor <b>6</b> that has progressed
through early clinical trials. The compound shows favorable pharmacokinetic
and activity profiles and has a confirmed mechanism of action through
crystallographic studies of a rhinovirusācompound complex.
The compound has now progressed to phase IIb clinical studies of its
effect on natural rhinovirus infection in humans
Discovery and Synthesis of CāNucleosides as Potential New Anti-HCV Agents
Nucleoside analogues have long been
recognized as prospects for
the discovery of direct acting antivirals (DAAs) to treat hepatitis
C virus because they have generally exhibited cross-genotype activity
and a high barrier to resistance. C-Nucleosides have the potential
for improved metabolism and pharmacokinetic properties over their
N-nucleoside counterparts due to the presence of a strong carbonācarbon
glycosidic bond and a non-natural heterocyclic base. Three 2ā²CMe-C-adenosine
analogues and two 2ā²CMe-guanosine analogues were synthesized
and evaluated for their anti-HCV efficacy. The nucleotide triphosphates
of four of these analogues were found to inhibit the NS5B polymerase,
and adenosine analogue <b>1</b> was discovered to have excellent
pharmacokinetic properties demonstrating the potential of this drug
class