Comprehensive Insights Into Sulfanilamido‐Based Medicinal Design and Research

The sulfanilamido skeleton is the core part of many clinical drugs with the para-aminobenzenesulfamido scaffold. Especially as the first type of synthetic antibacterial drugs, sulfanilamides have played important roles in preventing and treating infectious diseases for more than 90 years. Increasing efforts have been contributing toward the sulfanilamido skeleton with the incorporation of various unique substituents through medicinal design, which accessed great achievements that have not only broken the classical structure-activity relationship of antibacterial sulfanilamides, but also extended the other medicinal applications of sulfanilamides except for antibacterial drugs. Recently, the sulfanilamido-based medicinal design and research are becoming increasingly active, which have aroused widespread concern in the medicinal community. Thus, based on our work on sulfanilamido skeleton, this review article encompasses a robust collection of 746 references from 2008 to the present and, for the first time, provides comprehensive insights into sulfanilamido-based medicinal design and research across a wide range of medicinal potential. It is involved in antibacterial, antifungal, antitubercular, antiviral, anticancer, anti-inflammatory, antiglaucoma, antiparasitic, psychotherapeutic, antidiabetic, and other medicinal aspects. It also covers a large amount of sulfanilamido-based rich information on medicinal chemistry, including some important clinical sulfanilamido-based drugs, sulfanilamido-based medicinal molecular design strategies, structure-activity relationships, some important action targets, some important action mechanisms, as well as a multitargeting medicinal design strategy and medicinal chemicobiology. The foreseeable future research directions and trends toward medicinal design and development of sulfanilamido skeleton are prospected. This work might provide beneficial help for sulfanilamido-based rational design and development to afford sulfanilamido-based drugs with broad spectrum, high biological activity, and low toxicity to treat various diseases worldwide.