Metal-dependent inhibition of HIV-1 integrase.

  title={Metal-dependent inhibition of HIV-1 integrase.},
  author={Nouri Neamati and Zhaiwei Lin and Rajeshri G. Karki and Ann Orr and Kiriana K. Cowansage and Dirk Strumberg and Godwin C G Pais and Johannes H. Voigt and Marc C. Nicklaus and Heather E Winslow and He Zhao and Jim A. Turpin and Jizu Yi and Anna Marie Ann Skalka and Terrence R. Burke and Yves Pommier},
  journal={Journal of medicinal chemistry},
  volume={45 26},
Human immunodeficiency virus type 1 integrase (HIV-1 IN) is an essential enzyme for effective viral replication. Therefore, IN inhibitors are being sought for chemotherapy against AIDS. We had previously identified a series of salicylhydrazides as potent inhibitors of IN in vitro (Neamati, N.; et al. J. Med. Chem. 1998, 41, 3202-3209.). Herein, we report the design, synthesis, and antiviral activity of three novel mercaptosalicylhydrazide (MSH) derivatives. MSHs were effective against the IN… CONTINUE READING