Medicinal Chemistry Aspects of Thiazole and Thiazolidine Derivatives as Fundamental Building Blocks to Design New NNRTIs Against HIV‐1 Reverse Transcriptase

The therapy to treat the Human Immunodeficiency virus (HIV) and decrease the viral load has been a challenge since its discovery due to its ability to mutate, escape from drug therapies, and immunologic system. Consequently, the development of new therapies, especially potential molecules that focus on specific viral mechanisms to block viral replication, became a critical challenge in recent decades. The Reverse Transcriptase (RT) is an RNA‐ and DNA‐dependent DNA polymerase enzyme that is responsible for transcribing viral RNA into double‐stranded DNA. Non‐nucleoside RT Inhibitors perform important role in HIV therapy, and they are responsible for inhibiting RT by blocking its allosteric site, which shows physico‐chemical properties such as high hydrophobicity and key amino acid‐to‐hydrogen bond interactions. For this reason, designing new molecules with innovative heterocycles compatible with these characteristics can provide new potential inhibitors. For example, pentacyclic heterocycles like thiazole and its derivatives like thiazolidinedione, which have physico‐chemical properties that can interact with the allosteric site of RT, can be a new perspective in designing new Non‐nucleoside RT Inhibitors. This work reviews the scientific literature concerning these compounds and can help the design of new antiviral therapeutics.

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Publication Details

Journal
ChemMedChem
Published
2026-09-30
DOI
https://doi.org/10.1002/cmdc.70494
Primary Topic
HIV/AIDS drug development and treatment
Type
article
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article

Medicinal Chemistry Aspects of Thiazole and Thiazolidine Derivatives as Fundamental Building Blocks to Design New NNRTIs Against HIV‐1 Reverse Transcriptase

Marie‐Line Andréola, Michelly Cristiny Pereira, Marina Galdino da Rocha Pitta, José Arion da Silva Moura et al.
ChemMedChem
HIV/AIDS drug development and treatment
article

Medicinal Chemistry Aspects of Thiazole and Thiazolidine Derivatives as Fundamental Building Blocks to Design New NNRTIs Against HIV‐1 Reverse Transcriptase

Marie‐Line Andréola, Michelly Cristiny Pereira, Marina Galdino da Rocha Pitta, José Arion da Silva Moura, Maíra Galdino da Rocha Pitta, Mathieu Métifiot, Thaynara Paula Warren Bezerra, Patrícia Recordon-Pinson, DIANE REGIS SANTOS DO NASCIMENTO, Matheus Vinicius Guimarães de Melo
article en

Abstract

The therapy to treat the Human Immunodeficiency virus (HIV) and decrease the viral load has been a challenge since its discovery due to its ability to mutate, escape from drug therapies, and immunologic system. Consequently, the development of new therapies, especially potential molecules that focus on specific viral mechanisms to block viral replication, became a critical challenge in recent decades. The Reverse Transcriptase (RT) is an RNA‐ and DNA‐dependent DNA polymerase enzyme that is responsible for transcribing viral RNA into double‐stranded DNA. Non‐nucleoside RT Inhibitors perform important role in HIV therapy, and they are responsible for inhibiting RT by blocking its allosteric site, which shows physico‐chemical properties such as high hydrophobicity and key amino acid‐to‐hydrogen bond interactions. For this reason, designing new molecules with innovative heterocycles compatible with these characteristics can provide new potential inhibitors. For example, pentacyclic heterocycles like thiazole and its derivatives like thiazolidinedione, which have physico‐chemical properties that can interact with the allosteric site of RT, can be a new perspective in designing new Non‐nucleoside RT Inhibitors. This work reviews the scientific literature concerning these compounds and can help the design of new antiviral therapeutics.

ChemMedChemVol. 21(19)
Centre National de la Recherche Scientifique (FR), Université de Bordeaux (FR), Universidade Federal de Pernambuco (BR), Institut Polytechnique de Bordeaux (FR), Universidade Federal Rural de Pernambuco (BR)
Good health and well-being
Openalex Percentile: Top 12%
HIV/AIDS drug development and treatment
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