Sulfonamides in Drug Discovery: A Review of Synthetic Approaches and Biological Activities.

Authors

Emmanuel Chinedu Nnadi, Vivian Ifeoma Okonkwo, Faith Temitope Elijah, Anulika Ruphina Phil-Mba, Vivian Chinenye Odo, Blessing Kenechi Amujiogu, Blessing Ginika Eke, Chidinma Eucharia Ikwelle

Published in

Mini reviews in medicinal chemistry. Jul 06, 2026. Epub Jul 06, 2026.

Abstract

Sulfonamides represent one of the most versatile scaffolds in medicinal chemistry. Since their introduction as the first synthetic antibacterial agents in the 1930s, the sulfonamide functional group (-SO₂NR₂) has enabled extensive structural diversification, leading to compounds with broad therapeutic applications. In recent years, sulfonamide derivatives have gained renewed attention in drug discovery due to their roles in antimicrobial, anticancer, antimalarial, antiviral, antiinflammatory, antidiabetic, and antioxidant therapies. This review provides a comprehensive and structured overview of modern synthetic strategies for sulfonamide construction, including classical sulfonyl chloride-amine coupling, metal-catalyzed synthesis of sulfonamides, microwave-assisted synthesis, and other advanced methodologies that enable efficient access to structurally diverse derivatives. In parallel, recent advances in the biological evaluation of sulfonamide analogues are discussed, with emphasis on emerging pharmacological targets and mechanistic insights, such as enzyme inhibition, metabolic interference, and receptor modulation. By correlating synthetic approaches with observed biological activities, this review highlights the structure-activity relationships that guide rational drug design. Current challenges, research gaps, and future perspectives for sulfonamide-based therapeutics are also outlined. Collectively, the adaptability of the sulfonamide scaffold, combined with continued advances in synthetic chemistry and biological screening, underscores its sustained importance in the development of next-generation therapeutic agents.

PMID:
42411225
Bibliographic data and abstract were imported from PubMed on 07 Jul 2026.

Read full publication at:
Please sign in to see all details.

Stats

1-terrible, 9-excellent. How would you rate this publication? Sign in in to submit your rating.

Post a comment

You need to be signed in to post comments. You can sign in here.

Comments

There are no comments yet.