Download MendeleyGeneration of a long-acting fusion inhibitor against HIV-1.
Guo, Y., Zhou, P.P., Zhang, S.Y., Fan, X.W., Dou, Y.W., Shi, X.L.(2018) Medchemcomm 9: 1226-1231
- PubMed: 30109011
- DOI: https://doi.org/10.1039/c8md00124c
- Primary Citation of Related Structures:
5ZPW - PubMed Abstract:
AIDS has evolved from a fatal infectious disease to a manageable chronic disease under the treatment of anti-AIDS medications. HIV fusion inhibitors with high activity, low side effects and strong selectivity are promising drugs against HIV. Only one fusion inhibitor is currently approved, thereby highly active long-acting fusion inhibitors need to be developed for long-term AIDS treatment. Here, we synthesised MT-SC22EK (a small HIV fusion inhibitor) derivatives containing 1-2 staples to improve its stability. Antiviral activity studies showed that MT-SC22EK-2 with two staples exhibited potent inhibitory activity against HIV-1 standard strains and Chinese epidemic strains, and at the same time, MT-SC22EK-2 presented strong anti-T20 resistance. Surprisingly, MT-SC22EK-2 possessed excellent protease stability with a half-life of 3665 min. MT-SC22EK-2 is a potential HIV fusion inhibitor considered as a long-acting anti-HIV drug candidate.
Organizational Affiliation:
School of Pharmacy , Baotou Medical College , Baotou 014060 , China.
