Quality of clinical trials for selected priority mental and neurological disorders in sub Saharan Africa: A systematic review

IF 1.4 Q4 MEDICINE, RESEARCH & EXPERIMENTAL Open Access Journal of Clinical Trials Pub Date : 2016-12-07 DOI:10.2147/OAJCT.S117162
A. Mulugeta, G. Medhin, G. Yimer, Rahimush Jemal, A. Fekadu
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Abstract

I medicinal chemistry, purine motifs have attracted a great deal of research interest due to their preponderance in pharmaceutically indispensable compounds. Substituted purine especially 2, 6-disubstituted purine known to be very important medicinal and pharmaceutical intermediate. benzimidazoles are categorized in the important pharmacophores and privileged sub-structures in medicinal chemistry owing to their involvement as a key component for various biological activities. Therefore, introduction of benzimidazole at C-6 position of 2, 6-dichloropurine is supposed to improve its activity and thereby selectivity. Due to individual importance of purine and benzimidazole in living cells, we will present their synthesis as hybrids of benzimidazole at 6-position of purine and evaluated in vitro anticancer activities. Thus, a series of purine/benzimidazole hybrids were prepared by introduction of aromatic, aliphatic and heterocyclic moieties at the 2-position of purine to improve its potency and selectivity. Specifically, these hybrids were substituted with different secondary amines to remarkably increase their activity beyond their normal scope. Synthesized compounds were well characterized by 1H and 13C NMR as well as mass spectroscopy. The newly synthesized compounds were screened for in vitro anticancer activities against 60 tumor cell lines panel assay. These results open up new opportunities for other biological activities.
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撒哈拉以南非洲选定重点精神和神经疾病临床试验的质量:系统评价
在药物化学中,嘌呤基序因其在药学上不可或缺的化合物中的优势而引起了广泛的研究兴趣。取代嘌呤特别是2,6 -二取代嘌呤是非常重要的医药中间体。苯并咪唑作为多种生物活性的关键成分,在药物化学中被归类为重要的药效团和特殊的亚结构。因此,在2,6 -二氯嘌呤的C-6位上引入苯并咪唑可以提高其活性,从而提高其选择性。由于嘌呤和苯并咪唑在活细胞中的单独重要性,我们将在嘌呤的6位上合成它们作为苯并咪唑的杂种,并评估它们的体外抗癌活性。因此,通过在嘌呤的2位上引入芳香族、脂肪族和杂环基团,制备了一系列嘌呤/苯并咪唑杂合体,以提高其效力和选择性。具体地说,这些杂交种被不同的仲胺取代,显著提高了它们的活性,超出了它们的正常范围。通过1H、13C NMR和质谱对合成的化合物进行了表征。对新合成的化合物进行了体外抗肿瘤活性筛选。这些结果为其他生物活动开辟了新的机会。
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来源期刊
Open Access Journal of Clinical Trials
Open Access Journal of Clinical Trials MEDICINE, RESEARCH & EXPERIMENTAL-
CiteScore
3.90
自引率
0.00%
发文量
2
审稿时长
16 weeks
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