Sandbox southuniversity6: Difference between revisions

← Older edit

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

Arthur Cox

@@ Line 1: / Line 1: @@
 ==Medicinal Chemistry of HIV Integrase Inhibitors==
-When AIDS was first discovered in the 1980s, an individual's prognosis was grim, with a life expectancy on the order of 10 years. With development of effective antiviral drugs, this has increased up to 50 years or more. The HIV virus encodes several enzymes that are drug targets. The first effective drugs that were developed inhibit [[reverse transcriptase]]. The next drugs that were developed inhibit another enzymes that the virus encodes, [[HIV protease]]. The drugs that are under consideration here, the [[HIV integrase]] inhibitors are the most recently available class. Using multiple classes of drugs in combination has turned out to be a vital factor in effective treatment of HIV infection. For this reason, new integrase inhibitors have been avidly pursued by medicinal chemists across the globe.
+When AIDS was first discovered in the 1980s, an individual's prognosis was grim, with a life expectancy on the order of 10 years. With development of effective antiviral drugs, this has increased up to 50 years or more. The HIV virus encodes several enzymes that are drug targets. The first effective drugs that were developed inhibit [[reverse transcriptase]]. The next drugs that were developed inhibit another enzyme that the virus encodes, [[HIV protease]]. The drugs that are under consideration here, the [[HIV integrase]] inhibitors are the most recently available class. Using multiple classes of drugs in combination has turned out to be a vital factor in effective treatment of HIV infection. For this reason, new integrase inhibitors have been avidly pursued by medicinal chemists across the globe.
-Some of the first experimental compounds that were developed were members of a class called β-diketo acids, since there are 2 carbonyl groups beta to each other, with one of them alpha to a carboxylic acid functional group. Although they are referred to as "diketo acids (DKAs)", in solution they can also exist as the tautomeric enols. This is important, since it is the enol tautomer that is proposed to be species that actually binds to the integrase enzyme.
+Some of the first experimental compounds developed were members of a class called β-diketo acids. These compounds have 2 carbonyl groups beta to each other, with one of them alpha to a carboxylic acid functional group. Although they are referred to as "diketo acids (DKAs)", in solution they can also exist as the tautomeric enols. This is important, since it is the enol tautomer that is proposed to actually bind to the integrase enzyme.