Propylthiouracil Derivatives: Synthesis and Evaluation of Antimicrobial Efficacy Against Pathogenic Strains

Hamed, Mahmoud M.; Ahmed, Mostafa; Kamal El-Dean, Adel M.; Hassan, Mohammad H. A.; Tolba, Mahmoud S.

doi:10.21608/nujbas.2025.346200.1029

Propylthiouracil Derivatives: Synthesis and Evaluation of Antimicrobial Efficacy Against Pathogenic Strains

Document Type : Original papers

Authors

¹ Chemistry Department, Faculty of Science, New Valley University, El-Kharja 72511, Egypt

² Chemistry Department, Faculty of Science, Assiut University, Assiut 71516, Egypt

³ Department of Medical Laboratory Technology, Higher Technological Institute for Applied Health Sciences in Minya

10.21608/nujbas.2025.346200.1029

Abstract

This manuscript details the synthesis and evaluation of novel bioactive derivatives of propylthiouracil (PTU), highlighting their pharmacological significance. We synthesized several PTU derivatives through various chemical transformations, notably derivatives 2 and 3 from 4-chloro-2-oxo-2H-chromene-3-carbaldehyde and chloroacetyl chloride, respectively. Derivative 4 was produced by reacting PTU derivative 1 with chloroacetic acid and 4-chlorobenzaldehyde, while hydrazinyl product 5 was obtained by treating PTU derivative 1 with hydrazine hydrate. Further reactions led to triazolopyrimidinone derivatives 6 and Schiff’s base derivative 7. Antimicrobial testing revealed that derivative 2 showed significant efficacy against Gram-positive bacteria, particularly Staphylococcus aureus and Bacillus subtilis, but none were effective against Gram-negative strains or Candida albicans. These results highlight the potential of PTU derivatives as antimicrobial agents while indicating the need for structural modifications to enhance effectiveness against resistant pathogens. This study contributes to the understanding of PTU's synthetic versatility and biological potential in medicinal chemistry. This study presents a novel approach to the synthesis of bioactive derivatives of propylthiouracil (PTU), expanding the existing knowledge of this compound’s pharmacological potential. The innovative chemical transformations employed to create derivatives 2 to 7 highlight the versatility of PTU as a scaffold for developing new antimicrobial agents.

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