International Journal For Multidisciplinary Research
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Volume 8 Issue 2
March-April 2026
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Pyrazoles and Dihydropyrazoles (Pyrazolines) in Medicinal Chemistry: Structures and Pharmacological Activities
| Author(s) | Mr. Rajesh Roshan, Dr. Mithilesh Kumar Singh |
|---|---|
| Country | India |
| Abstract | Heterocyclic frameworks dominate the chemical space of biologically active small molecules, largely because heteroatoms introduce directional hydrogen bonding, tunable electronics, and conformational constraints that collectively improve target engagement and drug-like behavior. Nitrogen heterocycles are especially enriched among approved medicines, and five-membered azoles remain a recurring motif across therapeutic classes. Within this family, pyrazoles (aromatic 1,2-diazoles) and their partially saturated congeners, dihydropyrazoles (pyrazolines), have sustained attention as “privileged” scaffolds with exceptional pharmacological breadth. This review consolidates key concepts underpinning heterocycle relevance in medicinal chemistry and provides a focused survey of pyrazoline bioactivity across antimicrobial, antitubercular, antiprotozoal, antiviral, anti-inflammatory/analgesic, anticancer, CNS, and cannabinoid CB₁ receptor modulation landscapes. Mechanistic themes-COX/LOX pathway interference, KSP inhibition, P-gp modulation, GLI signaling disruption, monoamine oxidase inhibition, and receptor antagonism-emerge repeatedly across structurally diverse analogues. The historical arc from antipyrine and phenylbutazone to modern pyrazole therapeutics underscores how dihydropyrazole chemistry helped seed contemporary heterocycle-driven drug discovery. Overall, pyrazolines offer a distinctive combination of synthetic accessibility and 3D topology that can complement the planarity of aromatic pyrazoles, warranting continued exploration in lead generation and optimization. |
| Keywords | heterocycles; pyrazole; pyrazoline; dihydropyrazole; medicinal chemistry; privileged scaffold; antimicrobial; |
| Field | Chemistry |
| Published In | Volume 8, Issue 2, March-April 2026 |
| Published On | 2026-03-11 |
| DOI | https://doi.org/10.36948/ijfmr.2026.v08i02.70669 |
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E-ISSN 2582-2160
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