Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

The Pseudo-Symmetric N-benzyl Hydroxyethylamine Core in a New Series of Heteroarylcarboxyamide HIV-1 Pr Inhibitors: Synthesis, Molecular Modeling and Biological Evaluation

Version 1 : Received: 20 September 2021 / Approved: 22 September 2021 / Online: 22 September 2021 (10:44:16 CEST)

A peer-reviewed article of this Preprint also exists.

D’Orsi, R.; Funicello, M.; Laurita, T.; Lupattelli, P.; Berti, F.; Chiummiento, L. The Pseudo-Symmetric N-benzyl Hydroxyethylamine Core in a New Series of Heteroarylcarboxyamide HIV-1 Pr Inhibitors: Synthesis, Molecular Modeling and Biological Evaluation. Biomolecules 2021, 11, 1584. D’Orsi, R.; Funicello, M.; Laurita, T.; Lupattelli, P.; Berti, F.; Chiummiento, L. The Pseudo-Symmetric N-benzyl Hydroxyethylamine Core in a New Series of Heteroarylcarboxyamide HIV-1 Pr Inhibitors: Synthesis, Molecular Modeling and Biological Evaluation. Biomolecules 2021, 11, 1584.

Journal reference: Biomolecules 2021, 11, 1584
DOI: 10.3390/biom11111584

Abstract

New series of compounds containing both heterocycle moieties and pseudo-symmetric hydroxyethylamine core were obtained using a simple synthetic path that can provide a library of compounds in few steps and high yields. Furthermore, diversity-oriented synthesis was studied to change different functionalities according to needs. The in vitro inhibition activity against recombinant HIV-1 protease was evaluated. A beneficial effect of this class of compounds can be obtained either for the presence of a bis-benzyl group into the core and for the heterocyclic moiety in P1, specifically the indole ring. Docking analysis was also reported.

Keywords

HIV-protease inhibitors; pseudo-symmetric core; heteroaryl carboxyamides; synthesis; biological screening; molecular modeling

Subject

LIFE SCIENCES, Other

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