有机、药物和药物化学在药物设计中的作用:介绍

Prakash Prajapat
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Pharmacology” is derived from pharmakone = drug and logos = discourse or treatise, and hence includes allied fields such as pharmacy, pharmacognosy, toxicology, posology, chemotherapy, therapeutic and materia medica. “Pharmacy” is the study of the formulation of an active chemical entity, in the form of tablets, capsules, powders, aerosols, injections etc. The physiological activity of drugs has been found to depend upon the presence of particular functionality or structural unit.2 Part of drug which causes actual curing effect is known as “pharmacophores”. There are two major considerations that have to be discussed in any drug design project. Firsts, drugs interact with molecular targets in the body and so it is important to choose the correct target for the desired pharmaceutical effect.3 In other words a drug that will interact is powerfully and selectively as possible for that target is known as “pharmacodynamics”. Second, a drug after administration has an ability to travel through the body in order to reach its targets is known as “pharmacokinetics”. Nowadays, nanomedicine research played significant role in drug discovery. Generally, nanomedicine is a field of medicine to facilitate the information tools of nanotechnology to the prevention and cure against several lethal diseases viz.4 microbial, malaria, HIV, TB, cancer etc. The development of newer pharmaceuticals is currently a critical and challenging task to the pharmaceutical industry. The vital interest of the medicinal and agrochemical industries in organic synthesis is often related with their natural occurrence. Similarly, medicinal and pharmaceutical field, there has always been and continue to be a need for newer chemical entities with diverse biological properties.5 Many works are still needed to minimize the time, expenditure, and attrition rate in the drug discovery process simultaneously addressing the huge unmet medical need across the world. Referencing the study report, poor pharmacokinetic and preclinical toxicity were the main reasons for the failure in the drug development, in addition to the lack of efficiency and adverse effects.6 New drugs are necessitated to cure new diseases, to find less hazardous drug and to cure diseases whose drugs have become ineffective due to resistant strains of microorganisms. Besides these causes, new drug discovery and researches are required to recognize pharmacophore present in the effective drugs.7,8 We must always continue to search for drugs which exhibit clear advantages over the already existing respective drugs. 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引用次数: 2

摘要

然而,这一角色的确切性质正在发生明显的变化,这不仅是因为合成化学家和药物化学家有了新的机会,而且在几个关键领域,特别是在药物代谢和化学毒理学方面,化学家们处理影响他们日常决策的测试数据的更快的转变。药物化学的目的是设计和生产可用于预防、治疗和治愈人类或动物疾病的药物化合物。回顾意义上的药物化学包括对已有药物、药物的药理学性质及其构效关系(SAR)的研究以及前瞻意义上的研究。“Pharmacology”是由pharmakone =药物和logos =论述或论文衍生而来,因此包括相关领域,如药学,生药学,毒理学,病理学,化疗,治疗和本草。“药剂学”是研究一种活性化学实体的制剂,其形式包括片剂、胶囊、粉剂、气雾剂、注射剂等。已经发现药物的生理活性依赖于特定功能或结构单元的存在药物中产生实际疗效的部分被称为“药效团”。在任何药物设计项目中都必须讨论两个主要考虑因素。首先,药物与体内的分子靶点相互作用,因此选择正确的靶点以达到预期的药物效果是很重要的换句话说,一种药物会对目标产生强有力的选择性的相互作用,这被称为“药效学”。其次,药物在给药后具有通过身体到达目标的能力,这被称为“药代动力学”。目前,纳米医学研究在药物发现中发挥着重要作用。一般来说,纳米医学是利用纳米技术的信息工具来预防和治疗几种致命疾病,如微生物、疟疾、艾滋病毒、结核病、癌症等的医学领域。新药物的开发是当前制药行业的一项关键和具有挑战性的任务。医药和农化工业对有机合成的重要兴趣往往与有机合成的自然发生有关。同样,在医药和制药领域,一直存在并将继续需要具有不同生物特性的新型化学实体为了最大限度地减少药物发现过程中的时间、支出和损耗率,同时解决世界各地巨大的未满足的医疗需求,仍需要做许多工作。参考研究报告,药物代谢动力学差和临床前毒性是导致药物开发失败的主要原因,此外还有效率低和不良反应为了治疗新的疾病,为了寻找危险性较小的药物,为了治疗由于微生物耐药菌株而使药物无效的疾病,必须使用新药。除了这些原因外,还需要新药的发现和研究,以识别有效药物中存在的药效团。我们必须不断地寻找比现有的药物有明显优势的药物。这些优点可能是:提高生物活性,部分或完全没有不良反应,毒性小,更有营养价值,提高稳定性和降低生产成本。目前,许多有机和药物实验室的研究开发部门(R&D)正在致力于合成新的生物载体/药物载体,以提高其药物活性潜力和提高现有药物的产量。最后,从合成、医药、生物制药和工业的角度来看,这种化学对生命过程和提高生活质量的努力以及社会发展做出了贡献(图1-3)。
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Role of organic, medicinal & pharmaceutical chemistry in drug design: introduction
Submit Manuscript | http://medcraveonline.com However, the precise nature of the role is undergoing a visible change, not only because of the new available to the synthetic and medicinal chemists, but also in several key areas, particularly in drug metabolism and chemical toxicology, as chemists deal with the ever more rapid turnaround of testing data that influences their day-to-day decision. Objective of medicinal chemistry is to design and production of compounds that can be used in medicine for prevention, treatment and cure of human or animal disease. Taken in retrospective sense medicinal chemistry includes study of already existing drugs, of their pharmacological properties and their structure activity relationship (SAR) along with above prospective sense. Pharmacology” is derived from pharmakone = drug and logos = discourse or treatise, and hence includes allied fields such as pharmacy, pharmacognosy, toxicology, posology, chemotherapy, therapeutic and materia medica. “Pharmacy” is the study of the formulation of an active chemical entity, in the form of tablets, capsules, powders, aerosols, injections etc. The physiological activity of drugs has been found to depend upon the presence of particular functionality or structural unit.2 Part of drug which causes actual curing effect is known as “pharmacophores”. There are two major considerations that have to be discussed in any drug design project. Firsts, drugs interact with molecular targets in the body and so it is important to choose the correct target for the desired pharmaceutical effect.3 In other words a drug that will interact is powerfully and selectively as possible for that target is known as “pharmacodynamics”. Second, a drug after administration has an ability to travel through the body in order to reach its targets is known as “pharmacokinetics”. Nowadays, nanomedicine research played significant role in drug discovery. Generally, nanomedicine is a field of medicine to facilitate the information tools of nanotechnology to the prevention and cure against several lethal diseases viz.4 microbial, malaria, HIV, TB, cancer etc. The development of newer pharmaceuticals is currently a critical and challenging task to the pharmaceutical industry. The vital interest of the medicinal and agrochemical industries in organic synthesis is often related with their natural occurrence. Similarly, medicinal and pharmaceutical field, there has always been and continue to be a need for newer chemical entities with diverse biological properties.5 Many works are still needed to minimize the time, expenditure, and attrition rate in the drug discovery process simultaneously addressing the huge unmet medical need across the world. Referencing the study report, poor pharmacokinetic and preclinical toxicity were the main reasons for the failure in the drug development, in addition to the lack of efficiency and adverse effects.6 New drugs are necessitated to cure new diseases, to find less hazardous drug and to cure diseases whose drugs have become ineffective due to resistant strains of microorganisms. Besides these causes, new drug discovery and researches are required to recognize pharmacophore present in the effective drugs.7,8 We must always continue to search for drugs which exhibit clear advantages over the already existing respective drugs. Such advantages may be: improvement in bioactivity, partial or total absence of adverse effects, minor toxicity, more nutritive value, improved stability and decrease in production cost.9–12 Nowadays, research development department (R&D) of many organic and pharmaceutical laboratories are working for synthesis of newer biophores/pharmacophores having improved their potential in drug activity and increasing yields of existing drugs. Finally, this chemistry has contributed to life processes and to the efforts to advance the quality of life as well as to the development of society from synthetic, medicinal, biopharmaceutical and industrial point of view (Figures 1–3).
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