Novel Antitubercular(新型抗结核药)研究综述
Novel Antitubercular 新型抗结核药 - Moreover, the molecular docking study of template compound 23j provides new insight into the discovery of novel antitubercular agents targeting DprE1. [1] BACKGROUND AND PURPOSE Translational efforts in the evaluation of novel antitubercular drugs demand better integration of pharmacokinetic-pharmacodynamic data arising from preclinical protocols. [2] These interesting results warrant further investigation, which may allow identification of novel antitubercular candidates based on this scaffold. [3] The search for novel antitubercular chemotherapeutics from underexplored natural sources is therefore of paramount importance. [4] Furthermore, in the pathogen Mycobacterium tuberculosis, the distribution of G4 motifs and their potential role in the regulation of gene transcription advocate for the use of G4 ligands to develop novel antitubercular therapies. [5] Hence, in our pursuit of developing novel antitubercular compounds, we are reporting the e-Pharmacophore-based design of DprE1 (decaprenylphosphoryl-ribose 2′-oxidase) inhibitors. [6] tb) are evolving at an alarming rate, and this indicates the urgent need for the development of novel antitubercular drugs. [7] Novel antitubercular drugs can be developed by identifying diversiform targets in M. [8] We believe that this study provides an important initial guidance to medicinal chemists and biochemists to synthesize and test an enriched set of compounds that have the potential to inhibit Mtb USP (Rv1636), thereby aiding the development of novel antitubercular lead candidates. [9] Extensive biological and physicochemical profiling of this series revealed first structure-activity relationships and set the basis for further optimization and development of this novel antitubercular scaffold. [10] The present study assessed a novel antitubercular mechanism of of galangal through M. [11] This review provides an update on the progress of these novel antitubercular agents. [12] Employing circular dichroism (CD) and UV/VIS absorption spectroscopic methods, we demonstrated and evaluated the AAG binding properties of novel antitubercular drug candidates developed against sensitive and multidrug-resistant strains of M. [13] Thiosemicarbazide derivative 8n is a candidate for the development of novel antitubercular agents. [14] 1,3,5-Oxadiazole derivatives 1c-e are candidates for the development of novel antitubercular agents. [15] Conventional treatments to combat the tuberculosis (TB) epidemic are falling short, thus encouraging the search for novel antitubercular drugs acting on unexplored molecular targets. [16] This newly developed drug screening assay offers an easy, safe, image based high content screening tool to search for novel antitubercular inhibitors against both active and dormant state intracellular mycobacteria. [17] , ability to grow and multiply inside macrophages and to induce delayed hypersensitivity reactions) and to the emergence and spread of multidrug and extended-drug resistant Mycobacterium tuberculosis strains, correlated with the paucity of novel antitubercular drugs, the objectives of decreasing of incidence, prevalence and mortality rates, and to successfully detect and treat TB are threatened. [18]此外，模板化合物 23j 的分子对接研究为发现靶向 DprE1 的新型抗结核药物提供了新的见解。 [1] 背景和目的 评价新型抗结核药物的转化努力需要更好地整合临床前方案产生的药代动力学-药效学数据。 [2] 这些有趣的结果值得进一步研究，这可能允许基于该支架鉴定新的抗结核候选物。 [3] 因此，从未充分开发的天然资源中寻找新的抗结核化疗药物至关重要。 [4] 此外，在病原体结核分枝杆菌中，G4 基序的分布及其在基因转录调控中的潜在作用提倡使用 G4 配体开发新的抗结核疗法。 [5] 因此，在我们追求开发新型抗结核化合物的过程中，我们报告了基于电子药效团的 DprE1（十癸烯基磷酸核糖 2'-氧化酶）抑制剂设计。 [6] tb) 正在以惊人的速度发展，这表明迫切需要开发新型抗结核药物。 [7] 通过识别 M. [8] 我们相信，这项研究为药物化学家和生物化学家合成和测试一组有可能抑制 Mtb USP (Rv1636) 的丰富化合物提供了重要的初步指导，从而有助于开发新型抗结核先导候选药物。 [9] 该系列的广泛生物和物理化学分析揭示了第一个结构-活性关系，并为进一步优化和开发这种新型抗结核支架奠定了基础。 [10] 本研究评估了高良姜通过 M. [11] 本综述提供了这些新型抗结核药物的最新进展。 [12] 我们采用圆二色性 (CD) 和 UV/VIS 吸收光谱方法，展示并评估了针对敏感和耐多药结核分枝杆菌菌株开发的新型抗结核药物候选物的 AAG 结合特性。 [13] 氨基硫脲衍生物 8n 是开发新型抗结核药物的候选药物。 [14] 1,3,5-恶二唑衍生物 1c-e 是开发新型抗结核药物的候选药物。 [15] 对抗结核病 (TB) 流行病的常规治疗方法不足，因此鼓励寻找作用于未探索的分子靶点的新型抗结核药物。 [16] 这种新开发的药物筛选试验提供了一种简单、安全、基于图像的高内涵筛选工具，可用于寻找针对活性和休眠状态细胞内分枝杆菌的新型抗结核抑制剂。 [17] 、在巨噬细胞内生长和繁殖以及诱导迟发性超敏反应的能力）以及多药和长期耐药结核分枝杆菌菌株的出现和传播，这与新型抗结核药物的缺乏、降低发病率、流行率和死亡率，以及成功检测和治疗结核病的威胁。 [18]
novel antitubercular drug 新型抗结核药
BACKGROUND AND PURPOSE Translational efforts in the evaluation of novel antitubercular drugs demand better integration of pharmacokinetic-pharmacodynamic data arising from preclinical protocols. [1] tb) are evolving at an alarming rate, and this indicates the urgent need for the development of novel antitubercular drugs. [2] Novel antitubercular drugs can be developed by identifying diversiform targets in M. [3] Employing circular dichroism (CD) and UV/VIS absorption spectroscopic methods, we demonstrated and evaluated the AAG binding properties of novel antitubercular drug candidates developed against sensitive and multidrug-resistant strains of M. [4] Conventional treatments to combat the tuberculosis (TB) epidemic are falling short, thus encouraging the search for novel antitubercular drugs acting on unexplored molecular targets. [5] , ability to grow and multiply inside macrophages and to induce delayed hypersensitivity reactions) and to the emergence and spread of multidrug and extended-drug resistant Mycobacterium tuberculosis strains, correlated with the paucity of novel antitubercular drugs, the objectives of decreasing of incidence, prevalence and mortality rates, and to successfully detect and treat TB are threatened. [6]背景和目的 评价新型抗结核药物的转化努力需要更好地整合临床前方案产生的药代动力学-药效学数据。 [1] tb) 正在以惊人的速度发展，这表明迫切需要开发新型抗结核药物。 [2] 通过识别 M. [3] 我们采用圆二色性 (CD) 和 UV/VIS 吸收光谱方法，展示并评估了针对敏感和耐多药结核分枝杆菌菌株开发的新型抗结核药物候选物的 AAG 结合特性。 [4] 对抗结核病 (TB) 流行病的常规治疗方法不足，因此鼓励寻找作用于未探索的分子靶点的新型抗结核药物。 [5] 、在巨噬细胞内生长和繁殖以及诱导迟发性超敏反应的能力）以及多药和长期耐药结核分枝杆菌菌株的出现和传播，这与新型抗结核药物的缺乏、降低发病率、流行率和死亡率，以及成功检测和治疗结核病的威胁。 [6]
novel antitubercular agent
Moreover, the molecular docking study of template compound 23j provides new insight into the discovery of novel antitubercular agents targeting DprE1. [1] This review provides an update on the progress of these novel antitubercular agents. [2] Thiosemicarbazide derivative 8n is a candidate for the development of novel antitubercular agents. [3] 1,3,5-Oxadiazole derivatives 1c-e are candidates for the development of novel antitubercular agents. [4]此外，模板化合物 23j 的分子对接研究为发现靶向 DprE1 的新型抗结核药物提供了新的见解。 [1] 本综述提供了这些新型抗结核药物的最新进展。 [2] 氨基硫脲衍生物 8n 是开发新型抗结核药物的候选药物。 [3] 1,3,5-恶二唑衍生物 1c-e 是开发新型抗结核药物的候选药物。 [4]