Medicinal Chemistry 3

Since there is a significant difference between the HIV protease enzyme and mammalian protease enzymes in terms of symmetry, it is feasible to design inhibitors that show selectivity for the viral enzyme over the mammalian enzymes.
Although the viral protease enzyme is symmetrical, there is no reason why substrates or inhibitors must be symmetrical.

Chloramphenicol does not belong to any general class of antibiotics. Doxycycline is a tetracycline. Erythromycin is a macrolide. Streptomycin is an aminoglycoside.

The hydroxyethylamine moiety mimics the transition state for the catalytic reaction, but it is stable to the reaction. A bioisostere is a moiety that can be used in place of another group, whilst retaining the desired pharmaceutical activity.

The ideal target should be important to the early stages of the virus life cycle so that the virus has less chance of spreading through the body.

Penicillins are bactericidal agents and not bacteriostatic agents. Benzylpenicillin has good activity against certain types of bacterial species, but not all. It is also susceptible to attack by bacterial β-lactamases which makes it ineffective against these bacterial strains. It is true to say that certain individuals can be allergic to benzylpenicillin.

The two main targets currently used in anti-HIV therapy are reverse transcriptase and protease. However, integrase and the viral glycoproteins gp120 and gp41 are newer, alternative targets for anti-HIV therapy.