报告了2024年批准的新药的结构-财产关系
1Department of Chemistry, Korea University, Seoul 02841, Korea (ROK).
Mini reviews in medicinal chemistry
|July 23, 2025
概括
本综述探讨了2024年批准的七种新药的结构修改如何改善其特性. 关键策略包括使用异循环和优化组,以获得更好的溶解性和有针对性的输送.
科学领域:
- 药用化学 医学化学
- 药物发现 药物发现 药物发现
- 药理学 药理学是指药理学的学科.
背景情况:
- 小分子药物是关键的治疗剂.
- 优化药物特性对于成功的临床转化至关重要.
- 了解结构-属性关系 (SPRs) 引导药物设计.
研究的目的:
- 审查2024年批准的七种小分子药物的SPR.
- 确定有效的领先到候选人优化策略.
- 为未来药物开发提供见解.
主要方法:
- 分析了七种已批准的药物的结构变化.
- 专注于药物,包括阿普罗西坦,弗勒皮里达斯F-18,伊纳沃利西布,沃拉西迪尼布,恩西特雷尔维尔,戈利多西提尼布和佐里费尔提尼布.
- 对增强类似药物的特性策略的评估.
主要成果:
- 战略性地使用五和六个成员的含异环作为生物异构体和溶解组.
- 对于golidocitinib,精确定位溶解组可以提高选择性和物理化学性质.
- 对于透中枢神经系统的药物,如 zorifertinib,控制可旋转的键,H键捐赠者和脂性是 BBB 透和口服生物可用性的关键.
结论:
- SPR分析揭示了药物优化的关键修改.
- 异环是提高溶解性和药物样性质的宝贵工具.
- 定制分子性质对于实现所需的药理动力学和药理动力学特征至关重要.
相关概念视频
Structure-Activity Relationships and Drug Design
1.1K
Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
1.1K
Drug Nomenclature
2.3K
During the development of a new pharmaceutical, the manufacturer initially assigns a code name to the drug. Once approved, the drug receives a United States Adopted Name (USAN)—a generic, nonproprietary designation. Upon being listed in the United States Pharmacopeia, this nonproprietary name becomes the drug's official name. Additionally, the manufacturer assigns a proprietary name or trademark, which serves as the brand name under which the drug is marketed. It is worth noting that...
2.3K
Drug Classes and Categories
2.2K
Drugs can be classified according to their chemical composition or their intended therapeutic application. For instance, anti-infective agents that possess the ability to eliminate pathogens or suppress their growth and reproduction can be grouped based on the organisms they target or their chemical structure. Furthermore, drugs can be divided into prescription, nonprescription, or controlled substances. Prescription medications, such as antibiotics, require oversight from a licensed healthcare...
2.2K
Drug Regulation
1.9K
Drug regulation encompasses the management of drug usage by evaluating its safety and efficacy through assessments conducted by regulatory authorities. Regrettably, the history of drug regulation is marred by several catastrophic events. One such incident is the Elixir Sulfanilamide tragedy, in which the toxic compound diethyl glycol was included in a sweet-tasting medication, leading to numerous fatalities. This event prompted the enactment of the Food, Drug, and Cosmetic Act in 1938. Under...
1.9K
Prodrugs
2.9K
Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...
Prodrugs help overcome...
2.9K
Drug Administration and Therapy Phases: Overview
761
Drugs, the chemical agents used in diagnosing, treating, or preventing diseases, undergo a four-phase process of development: pharmaceutic, pharmacokinetics, pharmacodynamics, and therapeutic.
The pharmaceutical phase focuses on leveraging the physicochemical properties of the drug to design and manufacture an effective product. Variants include orally administered tablets or capsules, topical creams or ointments, and parenteral-delivery solutions or emulsions.
The pharmacokinetic phase...
The pharmaceutical phase focuses on leveraging the physicochemical properties of the drug to design and manufacture an effective product. Variants include orally administered tablets or capsules, topical creams or ointments, and parenteral-delivery solutions or emulsions.
The pharmacokinetic phase...
761


