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Preparation of N-2-alkoxyvinylsulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
Comprehensive Insights Into Sulfanilamido-Based Medicinal Design and Research
Yi-Xin Wang1, Juan Wang1, Lin-Li Mou1
1Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Institute of Bioorganic & Medicinal Chemistry, Southwest University, Chongqing, China.
Sulfanilamide drugs, initially antibacterial agents, are now explored for diverse medicinal applications beyond infection treatment. This review details their expanded therapeutic potential and design strategies.
Area of Science:
- Medicinal Chemistry
- Drug Design
- Pharmacology
Background:
- Sulfanilamide derivatives, based on the para-aminobenzenesulfamido scaffold, represent a foundational class of synthetic antibacterial agents with a 90-year history.
- Recent medicinal chemistry efforts have introduced novel substituents, significantly altering the classical structure-activity relationships of antibacterial sulfanilamides.
- These modifications have unlocked a broader spectrum of therapeutic applications beyond their traditional antibacterial roles.
Purpose of the Study:
- To provide a comprehensive review of sulfanilamido-based medicinal design and research from 2008 to the present.
- To consolidate insights into the diverse medicinal potential of sulfanilamido scaffolds.
- To prospect future research directions in the development of sulfanilamido-based therapeutics.
Main Methods:
- Systematic literature review encompassing 746 references from 2008 to the present.
- Analysis of medicinal chemistry data, including drug design strategies, structure-activity relationships, and action mechanisms.
- Compilation of information on clinical sulfanilamido-based drugs and their therapeutic targets.
Main Results:
- The sulfanilamido skeleton demonstrates broad medicinal potential, extending to antifungal, antitubercular, antiviral, anticancer, anti-inflammatory, antiglaucoma, antiparasitic, psychotherapeutic, and antidiabetic applications.
- Significant advancements in molecular design strategies and understanding of structure-activity relationships have been achieved.
- The review highlights multitargeting design strategies and medicinal chemicobiology approaches.
Conclusions:
- Sulfanilamido-based research is a rapidly expanding field with significant therapeutic promise.
- The scaffold's versatility allows for the development of drugs with broad-spectrum activity, high efficacy, and low toxicity.
- Future research should focus on rational design and development to address various global diseases.
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