Novel Wild Type and Mutate HIV-1 Protease Inhibitors Containing Heteroaryl Carboxamides in P2: Synthesis, Biological and ADME Evaluations

Maria Francesca Armentano; Paolo Lupattelli; Faustino Bisaccia; Rosarita D’Orsi; Rocchina Miglionico; Ilaria Nigro; Alessandro Santarsiere; Federico Berti; Maria Funicello; Lucia Chiummiento

doi:10.20944/preprints202305.1103.v1

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preprints.org > engineering > bioengineering > doi: 10.20944/preprints202305.1103.v1

Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Novel Wild Type and Mutate HIV-1 Protease Inhibitors Containing Heteroaryl Carboxamides in P2: Synthesis, Biological and ADME Evaluations

Maria Francesca Armentano

^‡ ,

^‡ ,

Alessandro Santarsiere

Federico Berti

^* ,

Maria Funicello

^* ,

Lucia Chiummiento

^‡

Authors have the same importance

Version 1 : Received: 15 May 2023 / Approved: 16 May 2023 / Online: 16 May 2023 (05:32:28 CEST)

How to cite: Armentano, M.F.; Lupattelli, P.; Bisaccia, F.; D’Orsi, R.; Miglionico, R.; Nigro, I.; Santarsiere, A.; Berti, F.; Funicello, M.; Chiummiento, L. Novel Wild Type and Mutate HIV-1 Protease Inhibitors Containing Heteroaryl Carboxamides in P2: Synthesis, Biological and ADME Evaluations. Preprints 2023, 2023051103. https://doi.org/10.20944/preprints202305.1103.v1 Armentano, M.F.; Lupattelli, P.; Bisaccia, F.; D’Orsi, R.; Miglionico, R.; Nigro, I.; Santarsiere, A.; Berti, F.; Funicello, M.; Chiummiento, L. Novel Wild Type and Mutate HIV-1 Protease Inhibitors Containing Heteroaryl Carboxamides in P2: Synthesis, Biological and ADME Evaluations. Preprints 2023, 2023051103. https://doi.org/10.20944/preprints202305.1103.v1

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MDPI and ACS Style

Armentano, M.F.; Lupattelli, P.; Bisaccia, F.; D’Orsi, R.; Miglionico, R.; Nigro, I.; Santarsiere, A.; Berti, F.; Funicello, M.; Chiummiento, L. Novel Wild Type and Mutate HIV-1 Protease Inhibitors Containing Heteroaryl Carboxamides in P2: Synthesis, Biological and ADME Evaluations. Preprints 2023, 2023051103. https://doi.org/10.20944/preprints202305.1103.v1

APA Style

Armentano, M.F., Lupattelli, P., Bisaccia, F., D’Orsi, R., Miglionico, R., Nigro, I., Santarsiere, A., Berti, F., Funicello, M., & Chiummiento, L. (2023). Novel Wild Type and Mutate HIV-1 Protease Inhibitors Containing Heteroaryl Carboxamides in P2: Synthesis, Biological and ADME Evaluations. Preprints. https://doi.org/10.20944/preprints202305.1103.v1

Chicago/Turabian Style

Armentano, M.F., Maria Funicello and Lucia Chiummiento. 2023 "Novel Wild Type and Mutate HIV-1 Protease Inhibitors Containing Heteroaryl Carboxamides in P2: Synthesis, Biological and ADME Evaluations" Preprints. https://doi.org/10.20944/preprints202305.1103.v1

Abstract

The Virus HIV-1 infection still represents a serious disease even if actually it is transformed in chronic pathology. Considering the crucial role of the enzyme Protease in life cycle of HIV many efforts have been made in the research of new organic compounds showing inhibitory activity. After development of several series of non peptidic inhibitors we report here the synthesis of novel simple HIV-Protease inhibitors containing heteroaryl carboxamides and their antiviral activity in vitro and in HEK293 cells. Benzofuryl- benzothienyl- and indolyl rings as well as aryl sulfonamides with different electronic properties have been introduced by efficient synthetic procedures. All compounds showed inhibitory activity similar to the commercial drug Darunavir, effective against both wild-type HIV-1 protease and that containing the V32I or V82A mutations. ADME properties were also evaluated, showing the potential of such compounds to be developed as drugs.

Keywords

mutate HIV protease inhibitors; carboxamides; heteroarenes; mammalian cells essay; ADME

Subject

Engineering, Bioengineering

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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