ABSTRACT
This chapter shows that several of the integrase (IN) inhibitor molecules could act as dual inhibitors. It provides a novel insight into the distinct chemical features of the human immunodeficiency virus (HIV) IN inhibitors. Discovery of novel inhibitors that are structurally and/or mechanistically different is required to inhibit viral strains resistant to the approved drugs. Intense research efforts directed to find a potent HIV IN inhibitor drug identified several classes of catechol-and non-catechol-based inhibitors. Hydrazides and coumarins were among the first promising class of inhibitors synthesized without a catechol ring. A review of structure–activity relationship data has shown that research efforts from different groups have resulted in the development of several second-generation inhibitors with nanomolar potency. IN inhibitor drugs act selectively on HIV IN and have no risk of developing crossresistance against other classes of HIV inhibitor drugs. However, these inhibitors are susceptible to developing drug-resistant mutant viral strains.
