In-Vitro Anti-Hiv Evaluation of Novel Amide and Ether Conjugates of 2, 3-Diaryl-1, 3-Thiazolidin-4-Ones
Posted: 11 Feb 2020 Last revised: 28 Apr 2020
Date Written: February 9, 2020
Abstract
Human immunodeficiency virus type 1 (HIV-1) was identified as the causative agent in the transmission and development of acquired immune deficiency syndrome (AIDS) in the late 80s. With the aim to evaluate compounds for its anti-HIV activity, 20 novel compounds have been screened against for anti-HIV and cytotoxicity against wild strain of HIV-1IIIB in T lymphocyte cells by syncytia formation assay. The assay is based upon the cytopathic effect (CPE) of HIV-1 and measured the viability of HIV-1 infected T lymphocyte cells. The cytotoxicity of the synthesized compounds on T cell lines was also assessed by MTT colorimetric assay method. The cytotoxicity of most of tested compounds on C8166 were low, the CC50 value of them were higher than 200µM, except few compounds（5b, 5h, 5i, 9i, 9j). Compounds 5a, 5b, 5c and 5f showed weak anti-HIV-1 activity, the therapeutic index values were over 10. As a positive control drug, 3TC (Lamivudine) has the best anti-HIV-1 activity (EC50=0.017µM) in vitro and the CC50 was higher 200μM, its therapeutic index was higher than 11764.71.
Keywords: Human Immunodeficiency Virus (HIV), Acquired Immune Deficiency Syndrome (AIDS), Syncytia formation, Cytopathic effect, Thiazolidin-4-ones
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