Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Exploring New Scaffolds for the Dual Inhibition of HIV-1 Rt Polymerase and Ribonuclease Associated Functions

Version 1 : Received: 22 February 2021 / Approved: 23 February 2021 / Online: 23 February 2021 (15:51:40 CET)

How to cite: Meleddu, R.; Corona, A.; Distinto, S.; Cottiglia, F.; Deplano, S.; Sequeira, L.; Secci, D.; Onali, A.; Sanna, E.; Esposito, F.; Cirone, I.; Ortuso, F.; Alcaro, S.; Tramontano, E.; Matyus, P.; Maccioni, E. Exploring New Scaffolds for the Dual Inhibition of HIV-1 Rt Polymerase and Ribonuclease Associated Functions. Preprints 2021, 2021020525 (doi: 10.20944/preprints202102.0525.v1). Meleddu, R.; Corona, A.; Distinto, S.; Cottiglia, F.; Deplano, S.; Sequeira, L.; Secci, D.; Onali, A.; Sanna, E.; Esposito, F.; Cirone, I.; Ortuso, F.; Alcaro, S.; Tramontano, E.; Matyus, P.; Maccioni, E. Exploring New Scaffolds for the Dual Inhibition of HIV-1 Rt Polymerase and Ribonuclease Associated Functions. Preprints 2021, 2021020525 (doi: 10.20944/preprints202102.0525.v1).

Abstract

Current therapeutic protocols for the treatment of HIV infection consist of the combination of diverse anti-retroviral drugs in order to reduce the selection of resistant mutants and to allow for the use of lower doses of each single agent to reduce toxicity. However, avoiding drugs interactions and patient compliance are issues not fully accomplished so far. In this respect the identification of single agents with multitarget potential might represent the ideal solution. Accordingly, a small library of biphenylhydrazo 4-arylthiazoles derivatives has been synthesised and evaluated to investigate the ability of the new derivatives to simultaneously inhibit both associated functions of HIV reverse transcriptase. All compounds were active towards the two functions, although at different concentrations. The substitution pattern on the biphenyl moiety appears relevant to determine the activity.

Subject Areas

HIV-RT; ribonuclease H; dual inhibitors; docking; putative binding

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