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Chloroquine and hydroxychloroquine screened for antiviral activity against Hepatitis C virus in Huh-5-2 cells. Chloroquine and hydroxychloroquine reduces the HCV RNA and promote the cell growth with respect to untreated control at concentration of 10.75 µM and 6.6 µM respectively.

New derivatives of azidothymidine (AZT) substituted by alkyl and alkylsulphonyl groups at N-3 and C-5', respectively, have been synthesized. The new synthesized derivatives showed remarkable anti-HIV-1 and HIV-2 activity in MT-4 cells. Compounds 8 and 10 have IC(50) values of 0.83 and 0.31 microg/mL against HIV-1 with therapeutic index of 83 and 403, respectively, and IC(50) values of 0.93 and 0.29 microg/mL against HIV-2 with therapeutic index of 74 and 431, respectively. This means that compounds 8 and 10 were cytotoxic to MT-4 cells at CC(50) of 69.2 microg/mL and 125 microg/mL, respectively.

Objective: To investigate the in vitro microbicidal and cytocidal potency of monocaprin dissolved in pharmaceutical hydrogel formulations and to evaluate their potential use as vaginal microbicides against sexually transmitted pathogens such as herpes simplex virus type 2 (HSV2), human immunodeficiency virus type 1 (HIV-1), Chlamydia trachomatis, and Neisseria gonorrhoeae. Methods: Gel formulations were mixed with equal volumes of virus/bacteria suspensions in culture medium and incubated for 1 and 5 minutes. The reduction in virus/bacteria titre was used as a measure of microbicidal activity. Similarly, gels were mixed with human semen to study their eVect on leucocytes. The toxicity of the gels was tested in rabbits by the standard vaginal irritation test. Results: Gels containing 20 mM of monocaprin caused a greater than 100 000-fold inactivation of HSV-2 and Neisseria in 1 minute and of Chlamydia in 5 minutes. Similarly, the gels caused a greater than 10 000-fold inactivation of HIV-1 in semen in 1 minute. They caused more than a 10 000-fold reduction in the number of viable leucocytes in semen in 1 minute. No toxic eVect on the vaginal mucosa of rabbits was observed after daily exposure for 10 days. Conclusions: Hydrogels containing monocaprin are potent inactivators of sexually transmitted viruses and bacteria in vitro. This simple lipid seems to be a feasible choice as a mucosal microbicide for prevention of sexually transmitted infections. It is a natural compound found in certain foodstuVs such as milk and is therefore unlikely to cause harmful side eVects in the concentrations used. (Sex Transm Inf 1999;75:181‐185)

A series of novel S-DABO derivatives with the substituted 1,2,3-triazole moiety on the C-2 side chain were synthesized using the simple and efficient CuAAC reaction, and biologically evaluated as inhibitors of HIV-1. Among them, the most active HIV-1 inhibitor was compound 4-((4-((4-(2,6-dichlorobenzyl)-5-methyl-6-oxo-1,6-dihydropyrimidin-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)methyl)benzenesulfonamide (B5b7), which exhibited similar HIV-1 inhibitory potency (EC50 = 3.22 μm) compared with 3TC (EC50 = 2.24 μm). None of these compounds demonstrated inhibition against HIV-2 replication. The preliminary structure-activity relationship (SAR) of these new derivatives was discussed briefly.

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An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.