biostudies-literatureRakshit GBirkbeck, University of LondonCouncil of Scientific and Industrial Research, IndiaCommonwealth Scholarship Commission31360-31401https://www.ebi.ac.uk/biostudies/studies/S-EPMC12401172biostudies-literatureUnknown15(38)Pyrazoline scaffolds have attracted significant interest in medicinal chemistry due to their broad spectrum of pharmacological activities. Pyrazole-based drugs are either already approved or are currently undergoing clinical trials across a range of therapeutic areas. Pyrazolines (Δ²-pyrazolines or 2-pyrazoline or 4,5-dihydropyrazoles) evolved as cyclic analogues of thioacetazone and were explored for enhanced antitubercular activity over the past five decades. The scope of this review focused on how extensively the chemical space around pyrazolines has been explored in relation to their antitubercular activity, rather than presenting a general structure-activity relationship (SAR) account. In this exercise, we covered key molecular modifications, including rationale substitutioRSC advancesAdvancements in the design and development of pyrazoline-based antimycobacterial agents: an update and future perspectives.PMC12401172CSC INCN-2024-27209/0554(18070)/2024-EMR-IRakshit GJayaprakash VBhakta SChakraborty SfalseAdvancements in the design and development of pyrazoline-based antimycobacterial agents: an update and future perspectives.Pyrazoline scaffolds have attracted significant interest in medicinal chemistry due to their broad spectrum of pharmacological activities. Pyrazole-based drugs are either already approved or are currently undergoing clinical trials across a range of therapeutic areas. Pyrazolines (Δ²-pyrazolines or 2-pyrazoline or 4,5-dihydropyrazoles) evolved as cyclic analogues of thioacetazone and were explored for enhanced antitubercular activity over the past five decades. The scope of this review focused on how extensively the chemical space around pyrazolines has been explored in relation to their antitubercular activity, rather than presenting a general structure-activity relationship (SAR) account. In this exercise, we covered key molecular modifications, including rationale substitutio2025-01-01T00:00:00Z2025 Aug2026-07-15T14:15:29.578Z2026-07-05T03:12:32.139ZS-EPMC124011724090145910.1039/d5ra03759j