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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
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Antibacterial and antifungal pyrazoles based on different construction strategies

Muneeb Ur Rehman1, Fang He1, Xi Shu1

  • 1Key Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Hubei Engineering Research Center for Advanced Fine Chemicals, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei, 430205, China.

European Journal of Medicinal Chemistry
|November 28, 2024
PubMed

Insights

Novel pyrazole compounds show promise as antimicrobial agents against drug-resistant bacteria and fungi. This review highlights recent advancements in developing these agents to combat antimicrobial resistance (AMR).

Area of Science:

  • Medicinal Chemistry
  • Organic Chemistry
  • Microbiology

Background:

  • Rising prevalence of microbial infections and antimicrobial resistance (AMR) necessitates novel therapeutic agents.
  • Pyrazole, a versatile heterocyclic scaffold, is a key structural component in many existing drugs with therapeutic effects.
  • Overuse and misuse of antibiotics contribute significantly to the global AMR crisis.

Purpose of the Study:

  • To review and update the development of pyrazole-based antibacterial and antifungal agents from 2016 to 2024.
  • To discuss strategies for integrating functional groups with the pyrazole ring for enhanced antimicrobial activity.
  • To highlight structure-activity relationships of pyrazole derivatives against resistant microbial strains.

Main Methods:

  • Literature review of pyrazole-based antimicrobial agents developed between 2016 and 2024.
  • Analysis of molecular hybridization, bioisosterism, scaffold hopping, multicomponent reactions, and catalyst-free synthesis strategies.
  • Examination of structure-activity relationships (SAR) for pyrazole derivatives.

Main Results:

  • Compilation of diverse pyrazole derivatives combined with pharmacophores like coumarin, thiazole, oxadiazole, isoxazole, and indole.
  • Discussion of various synthetic strategies employed to create novel pyrazole-based antimicrobials.
  • Identification of key structural modifications influencing selectivity and potency against bacterial and fungal pathogens.

Conclusions:

  • Pyrazole derivatives represent a promising class of compounds for developing next-generation antimicrobials.
  • Understanding SAR is crucial for designing effective agents to combat antimicrobial resistance.
  • This review offers valuable insights for researchers in heterocyclic chemistry and drug discovery.
Keywords:
Antibacterial agentsAntifungal agentsAntimicrobial resistanceConstruction strategiesPharmacophoresPyrazoleStructure-activity relationship

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