RÉSUMÉ
AIDS is an infectious disease caused by human immunodeficiency virus (HIV) and has done great harm to human beings. The envelope glycoprotein surface subunit gp120 and its receptor CD4 and coreceptor CXCR4 play important roles in HIV-1 entry. The Phe43 pocket and Arg59 of gp120 are two important regions that interact with CD4. Recently, HIV small-molecule entry inhibitors have become a hot topic in anti-HIV drug research, which are able to inhibit the virus before the cells are infected. The Phe43 pocket is an attractive target and the study of Phe43 pocket-targeting small-molecule entry inhibitors is underway, including BMS-378806, BHS-488043 and its analogs, and NBD-556 and its analogs. Besides, CXCR4 antagonist is another important approach.