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SYNTHESIS OF NOVEL 4,6-DIPHENYLPYRIMIDINE SUBSTITUTED BENZAMIDE DERIVATIVES ITS CHARACTERIZATION AND EVALUATION FOR ANTI-OXIDANT AND ANTI-MICROBIAL ACTIVITIES
Journal of Advanced Scientific Research Pub Date : 2023-12-07 , DOI: 10.55218/jasr.202314404 Dr. AJITHA MAKULA , SANA TABASSUM
Journal of Advanced Scientific Research Pub Date : 2023-12-07 , DOI: 10.55218/jasr.202314404 Dr. AJITHA MAKULA , SANA TABASSUM
The research work involves the estimation and evaluation of pharmacological activity of designed 4, 6-diphenylpyrimidine substituted benzamide derivatives that act as HDAC inhibitors. The Histone deacetylases inhibitors are a new class of cytostatic agents that exhibits promising results cancer treatment. The four HDAC inhibitors approved by FDA for cancer chemotherapy is SAHA (Vorinostat), Belinostat (PXD-101), Panobinostat (LBH-589), and Romidepsin (FK-228). The six novel 4, 6-diphenylpyrimidine substituted benzamide derivatives were synthesized, characterized and evaluated for anti-microbial and anti-oxidant activities. The designed molecule with cap group as substituted 4, 6-diphenylpyrimidine of functional groups adjacent to the metal-binding benzamide was evaluated for the pharmacological activity evaluation. Prior to this, the work was done on in-silico studies by molecular docking and confirmed the anti-cancer activity. The Anti-oxidant and Anti-microbial activity was evaluated as per standard methods. Anti-microbial activities involve the Anti-bacterial and Anti-fungal activity estimation. Hence, based on the pharmacological activity results, it is confirmed that the designed and characterized novel 4, 6-diphenylpyrimidine substituted benzamide exhibited the biological activity of Anti-oxidant and Anti-microbial activity.
中文翻译:
新型4,6-二苯基嘧啶取代苯甲酰胺衍生物的合成、表征及抗氧化和抗微生物活性评价
该研究工作涉及对设计的作为 HDAC 抑制剂的 4, 6-二苯基嘧啶取代的苯甲酰胺衍生物的药理活性进行估计和评价。组蛋白脱乙酰酶抑制剂是一类新型细胞抑制剂,在癌症治疗方面显示出良好的效果。FDA 批准用于癌症化疗的四种 HDAC 抑制剂是 SAHA (Vorinostat)、Belinostat (PXD-101)、Panobinostat (LBH-589) 和 Romidepsin (FK-228)。合成、表征并评估了六种新型 4, 6-二苯基嘧啶取代的苯甲酰胺衍生物的抗微生物和抗氧化活性。对所设计的具有与金属结合苯甲酰胺相邻的官能团的取代的4,6-二苯基嘧啶的帽基的分子进行药理活性评价。在此之前,该工作通过分子对接进行了计算机模拟研究,并证实了其抗癌活性。根据标准方法评估抗氧化和抗微生物活性。抗微生物活性涉及抗细菌和抗真菌活性评估。因此,根据药理活性结果,证实所设计和表征的新型4,6-二苯基嘧啶取代的苯甲酰胺表现出抗氧化和抗微生物活性的生物活性。
更新日期:2023-12-07
中文翻译:
新型4,6-二苯基嘧啶取代苯甲酰胺衍生物的合成、表征及抗氧化和抗微生物活性评价
该研究工作涉及对设计的作为 HDAC 抑制剂的 4, 6-二苯基嘧啶取代的苯甲酰胺衍生物的药理活性进行估计和评价。组蛋白脱乙酰酶抑制剂是一类新型细胞抑制剂,在癌症治疗方面显示出良好的效果。FDA 批准用于癌症化疗的四种 HDAC 抑制剂是 SAHA (Vorinostat)、Belinostat (PXD-101)、Panobinostat (LBH-589) 和 Romidepsin (FK-228)。合成、表征并评估了六种新型 4, 6-二苯基嘧啶取代的苯甲酰胺衍生物的抗微生物和抗氧化活性。对所设计的具有与金属结合苯甲酰胺相邻的官能团的取代的4,6-二苯基嘧啶的帽基的分子进行药理活性评价。在此之前,该工作通过分子对接进行了计算机模拟研究,并证实了其抗癌活性。根据标准方法评估抗氧化和抗微生物活性。抗微生物活性涉及抗细菌和抗真菌活性评估。因此,根据药理活性结果,证实所设计和表征的新型4,6-二苯基嘧啶取代的苯甲酰胺表现出抗氧化和抗微生物活性的生物活性。