Research
Activities
As AIDS has become an increasing public
health concern in Thailand, antiviral agents are
much needed. However, due to the high cost of
classical drug development, computational
chemistry has been employed in aiding the
primary structure screening prior to synthesis
and biological evaluations. Following the in
silico screening, a number of nevirapine
derivatives have been proposed as good lead
compounds. Nevirapine is a known anti-reverse
transcriptase (RT) agent. Development of these
derivatives as drugs is extensively studied.
Structurally diverse library of nevirapine
derivatives are the subject of our research, and
efficient routes toward these compounds are
currently developed and are the focus of our
programme.
Our
interest also includes synthetic routes for some
bioactive oxygen heterocycles such as
wrighthiadione, coumestan, and diospyrol.
Wrighthiadione, a natural product isolated from
Wrighthia tomentosa has been shown to display
anti-HIV activity by inhibiting HIV-1 reverse
transcriptase (HIV-1 RT). Diospyrol is an
example of a dimeric naphthol isolated from
Diospyros mollis, locally known as Ma-Kluea. Its
use as anthelminthic agent has been documented.
Michellamines are a group of compounds having
diospyrol as their core appended with an
isoquinoline unit, collectively known as dimeric
naphthylisoquinoline alkaloid. Michellamines
were reported to possess anti-HIV property.
As a
part of our research interest in developing
synthetic methodologies, we have expanded the
horizon of our programme into the area of
organometallic chemistry and its application in
organic synthesis. Organometallic reactions are
powerful tools in developing and devising novel
organic reactions as they represent a new
frontier in catalysis and reaction selectivity.
Currently, we have successfully applied
organopalladium, organotin, organoboron,
organolithium, organocopper, and organomagnesium
to a number of organic reactions, which lead to
novel synthetic methodologies, as well as
structural diversity of the products. Besides
organometallic chemistry, the synthetic utility
of other reagents, such as hypervalent iodines,
is actively pursued.
We
have also used microwave irradiation to increase
the yield and reduce the reaction time of these
organometallic reactions based on “Green
Chemistry”. Various synthetic compounds, such as
biaryl compounds, cyclic lactone and lactam
systems, have been studied to produce a greater
number of bioactive compounds.
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