New thiourea and 1,3-thiazolidin-4-one derivatives effective on the HIV-1 virus

Abstract

Thiourea derivatives have been reported to possess many biological activities, among them antiviral and antitumoral properties. As part of our continuing effort to develop new active compounds, we report the synthesis and the evaluation of new fifteen thiourea derivatives with 1,3-benzothiazol-2-yl moiety, among them a group of biologically active (1-7) also underwent cyclisation to 1,3-thiazolidin-4-ones. Molecular structure of four compounds (4, 13, 15 and 3a) was determined by an X-ray crystallography. We here report the evaluation of their cytotoxicity against human leukaemia/lymphoma- and solid tumour-derived cell lines and of their antiviral activity against HIV-1 and representatives of ssRNA and dsDNA viruses. Derivative 5 showed an interesting activity against HIV-1 wild type and against variants carrying clinically relevant mutations. A colorimetric enzyme immunoassay clarified its mode of action as a non-nucleoside inhibitor of the reverse transcriptase.

This article is protected by copyright. All rights reserved.

A class of novel 1,3-benzothiazol-2-yl derivatives of thiourea has been synthesized.The 3-(1-phenylethyl)thiourea showed interesting antiviral activity against HIV-1,as nonnucleoside inhibitor of the reverse transcriptase.7 derivatives showed antiproliferative properties against cells from human tumours.

from #MedicinebyAlexandrosSfakianakis via xlomafota13 on Inoreader http://ift.tt/2p5C9kD
via IFTTT