TRIAZOLE AS A PRIVILEGED STRUCTURE IN THE DISCOVERY OF NEW ANTIFUNGAL DRUGS

TRIAZOLE AS A PRIVILEGED STRUCTURE IN THE DISCOVERY OF NEW ANTIFUNGAL DRUGS

• Author
• Nathalya Patricia dos Santos Soares
• Co-authors
• Alejandra Marigia Fragoso dos Santos , Allan moraes Silva , Camile Rodrigues de Siqueira , Beatriz Silva de Arruda Cardoso , Robert da Silva Tiburcio
• Abstract

• INTRODUCTION 

  Heterocyclic compounds an important class of organic molecules, have atoms in their rings bonded to at least one non-carbon atom. Five and six-membered rings are predominant due to their stability. These molecules are essential in synthetic chemistry, serving as a foundation and inspiration for new bioactive structures. 1,2 In this context of privileged structures in drug desing, the Triazole nucleus holds significant prominence.

  Triazoles linked to hybrid molecules containing natural compounds are becoming strong candidates for drugs to be used the tratment of various diseases. 2 

  AIMS 

  To demonstrate the various ways to enhance drug desing and synthesis, starting from the heterocyclic triazole, as well as to analyze the different possibilities of the utility of this heterocycle. 

  METHODS

  This research relates to a narrative literature review, based on articles on the topic. To guide and menage the study, the following guiding question was developed: "To what extent can the Triazole nucleus optimize the process of designing and optimizing new antifungal drug candidates?". 

  RESULTS AND DISCUSSION 

  Treatment with imidazole-based drugs has become restricted due to side effects, leading to the replacement of these derivatives with triazole ring compounds. 3

  The Triazole is a heterocycle of great relevance to medicinal chemistry, as its use is not solely confined to the pharmacophore group but also acts as a bridge between biomolecules, which is of utmost importance for the formation of hybrid compounds. Additionally, Triazole can enhance the pharmacological and pharmacokinetic properties of drugs, serving as a molecule optimizer. 4 Asignificant health problem is the resistance to the major antifungals currently in use, primarily due to the growth of fungal infections in recent decades. Triazole can be highly potent structure against fungi. 5

  Triazole compounds can be used as both surface and invasive fungicides. This molecule will act by reducing ergosterol biosynthesis, thereby decreasing fungal growth. Thus, it can be considered that triazole represents a significant advancement in medical mycology, serving as a broad-spectrum fungicide. 6 The antifungal activity of these compounds is related to the genera of Aspergillus, including various species, and Candida spp.7

  CONCLUSION 

  Among the mentioned facts, it is evident that there is a wide range of uses for Triazole in the desing and optimization of antifungal drugs, aiming to achive better adherence to treatments and greater effectiveness in addressing observed fungal resistance.

  ACKNOWLEDGMENT

  We firstly thank God giving us the light of knowledge, strngth, and determination to carry out this research. We also express our gratitude to Professor Ms. Robert Tibúrcio for guiding us in this work.

  CITATIONS AND REFERENCES

  1. Mulla, A; A Review: Biological Importance of Heterocyclic Compounds. Der Pharma Chemica2017,9, 141.

  2. Mermer, A; Keles, T; Sirin, Y; Recent studies of nitrogen containing heterocyclic compounds as novel antiviral agents; A review. Bioorganic Chemistry2021,105076.

  3. NETT, J. E.; ANDES, D. R. Antifungal agents: Spectrum of Activity, Pharmacology, and Clinical Indications. Infectious Disease Clinics of North America, v. 30, n. 1, p. 51-83, 2016.

  4. BRITTO, Karolinni B. et al. Evaluation of the herbicidal activity of new triazoles derived from isatin. PROCEEDINGS OF THE 4TH PHARMACEUTICAL SCIENCES WEEK innovation in pharmaceutical practice, p. 89.

  5. LIMA NETO, Reginaldo Gonçalves de. In vitro antifungal activity of thienyl and triazolic derivatives and in vivo liposomal formulations containing triazole against Candida Isolates characterized by MALDI-TOF ICMS. 2011.

  6.  WANI, M. Y.; AHMAD, A.; SHIEKH, R. A.; AL-GHAMDI, K. J.; SBRAL, A. J. F. N. Imidazole Clubbed 1,3,4-Oxadizole Derivatives as Potential Antifungal Agents. Bioorganic and Medicinal Chemistry, v. 23, n 15, p. 4172-4180, 2015.

  7. SHU,Yishuo et al. Progress of the triazole antifungal agent posoconazole in individualized therapy. Journal of Clinical and therapeutic Pharmacy, v. 12, p. 1966-1981, 2022.

   

• Keywords
• Triazole, Drugs, Diseases, Planning.
• Modality
• Pôster
• Subject Area
• Drug Design and Discovery, Synthesis and Natural Products