Журнал клеточной и молекулярной фармакологии

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An Understanding of the Biological Activity and Characteristics of Structure-Based Drugs That are Sulfonylpiperazine Derivatives

Eduard Buchner

Sulfonylpiperazine derivatives have emerged as a promising class of structure-based drugs due to their diverse biological activities and unique characteristics. This study aimed to provide a comprehensive understanding of the biological activity and structural features of sulfonylpiperazine derivatives. First, an overview of the sulfonylpiperazine scaffold was presented, highlighting its synthetic accessibility and versatility in medicinal chemistry. The sulfonyl group, attached to the piperazine ring, imparts crucial physicochemical properties to these derivatives, such as improved metabolic stability and increased lipophilicity, facilitating their interactions with target proteins. The biological activities of sulfonylpiperazine derivatives were explored, focusing on their potential as therapeutic agents in various disease areas. Examples of successful applications include anti-inflammatory, antimicrobial, anticancer, and central nervous system (CNS) disorders. The mechanism of action for each activity was discussed, illustrating the importance of specific structural features in modulating target interactions and subsequent pharmacological effects. Furthermore, the structure-activity relationship (SAR) of sulfonylpiperazine derivatives was examined to elucidate the key determinants of their biological activity. Studies have demonstrated that subtle modifications in the piperazine core, such as substitution patterns, stereochemistry, and ring fusion, can significantly impact potency, selectivity, and pharmacokinetic properties. Insights into SAR can guide the rational design of novel sulfonylpiperazine derivatives with improved efficacy and reduced off-target effects. Finally, an overview of the current strategies employed in the design and synthesis of sulfonylpiperazine derivatives was provided. Structurebased drug design techniques, including molecular docking, virtual screening, and computational modeling, have facilitated the identification of novel lead compounds and optimization of their binding affinity. Additionally, advances in synthetic methodologies have enabled the efficient preparation of diverse sulfonylpiperazine analogs, further expanding the chemical space for drug discovery.