In Vitro: HIV-1 inhibitor-50 (compound 36a) protects MT-4 cells from HIV-1 IIIB and RES056 with EC50s of 2.22 nM and 53.3 nM, respectively. HIV-1 inhibitor-50 inhibits MT-4 cells viability with an CC50 value of 45.6 μM. HIV-1 inhibitor-50 (hydrochloride; ) shows a lower intrinsic clearance rates in microsomes (CL=87.6 μL/min/mg) and liver (CL=16.6 μL/min/mg), and leads to a higher metabolic stability (T1/2=11.3 min).
In Vivo: HIV-1 inhibitor-50 (compound 36a) (hydrochloride; 2 mg/kg; i.v.; single dose) has a high clearance (CL=103 L/h/kg) and a modest half-life (T1/2=1.43 h). HIV-1 inhibitor-50 (hydrochloride; 2000 mg/kg; p.o.; single dose) doesn’t result any abnormal behaviors or significant changes in body weight compared with the control in 7 days, indicating no acute toxicity.