Synthesis of Pyrazole Derivative Incorporating Fluorine in the Aromatic Substitution for Physiological and Pharmacological Studies

R. Gautam
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Abstract

Over the past decade, drug resistance has become a growing problem in the treatment of infectious diseases caused by bacteria, fungi and viruses. In particular, resistance of bacterial pathogens to current antibiotics has emerged as a measure of health problems. This is especially true in the case of infectious diseases such as pneumonia, meningitis and tuberculosis, which would once have been easily treated with antibiotics, is no longer so readily treated. At present, all widely used antibiotic, including some of the agent such as streptogramins and new generation fluoroquinolones are subjected to bacterial resistance. The search for new antimicrobial agent is one of the most challenging tasks to the medicinal chemist. A search for new antimicrobial compounds with potent and minor toxicity continues to be a region of exploration in medicinal chemistry. It has been well recognized that nitrogen containing heterocyclic molecule is a seat of diverse medicinal activities. Heterocyclic nucleus Pyrazole constitutes an important class of compounds for new drug development. The synthesis of these derivatives and investigation of their chemical and biological behavior have gained more importance in recent decades. Owing to the pharmacological importance of Pyrazole, and its derivatives, in the present work, it has been contemplated to combine various biologically active moieties with these heterocycles through active functional systems to form new molecular framework. Prompted by the therapeutic importance of these heterocyclic derivatives, in the present research work we have synthesized Pyrazole with fluorinated aromatic rings, and its derivatives through multistep reaction. Appropriate synthetic methodologies have been developed for the synthesis of new molecules. Their purification techniques have been established. All the newly synthesized compounds have been characterized by 1H NMR, 13C NMR, mass spectral, IR and elemental analyses. Also structures of a few molecules have been confirmed by X-ray crystallographic analysis. Further, the target molecules have been evaluated for their in vitro antibacterial and antifungal activity. From the pharmacological evaluation, it has been observed that some of Pyrazole, derivatives showed good antimicrobial activity
含氟芳代吡唑衍生物的合成及其生理药理研究
在过去的十年中,在治疗由细菌、真菌和病毒引起的传染病方面,耐药性已成为一个日益严重的问题。特别是,细菌病原体对当前抗生素的耐药性已成为衡量健康问题的一项指标。在肺炎、脑膜炎和肺结核等传染病方面尤其如此,这些疾病以前可以很容易地用抗生素治疗,但现在不再那么容易治疗了。目前,所有广泛使用的抗生素,包括一些药物,如链状革兰素和新一代氟喹诺酮类药物,都存在细菌耐药性。寻找新的抗菌剂是药物化学家最具挑战性的任务之一。寻找具有强毒性和轻微毒性的新型抗菌化合物仍然是药物化学的一个探索领域。含氮杂环分子是具有多种药用活性的分子之一。杂环核吡唑是一类重要的新药开发化合物。近几十年来,这些衍生物的合成及其化学和生物行为的研究变得越来越重要。由于吡唑及其衍生物具有重要的药理作用,在本研究中,人们已经考虑通过活性功能系统将各种生物活性部分与这些杂环结合,形成新的分子框架。鉴于这些杂环衍生物具有重要的治疗意义,本研究通过多步反应合成了含氟芳香环的吡唑及其衍生物。合适的合成方法已经被开发出来用于新分子的合成。他们的净化技术已经建立。所有新合成的化合物都通过1H NMR, 13C NMR,质谱,IR和元素分析进行了表征。此外,一些分子的结构已被x射线晶体学分析证实。此外,靶分子已被评估其体外抗菌和抗真菌活性。从药理学评价来看,吡唑衍生物显示出良好的抗菌活性
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