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Updated: Jul 4, 2025

Optimized Griess Reaction for UV-Vis and Naked-eye Determination of Anti-malarial Primaquine
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基于结构的设计和开发基于阿米迪尼尔,阿米多克西米尔和酸的有机分子作为新型抗疟疾药物候选药物

Glory P Adebayo1,2, Gbolahan O Oduselu1, Damilola V Aderohunmu1

  • 1Covenant University Bioinformatics Research (CUBRe), Covenant University, Ota, Nigeria.

Arabian journal of chemistry
|January 29, 2024
PubMed
概括

设计和合成了针对Plasmodium falciparum 6-pyruvoyltetrahydropterin合成酶的新型抗疟疾药物候选药物. 化合物3b显示为开发新的抗叶酸抗疟药物的安全和有效头.

关键词:
有急性毒性的急性毒性.细胞毒性 细胞毒性胺酸是胺酸中的一种.疟疾:疟疾是一种疾病.压制压制是一种压制.

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The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...
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Heterocyclic amines, where the N atom is a part of an alicyclic system, are similar in basicity to alkylamines. Interestingly, the heterocyclic amine having a nitrogen atom as part of an aromatic ring has much less basicity than its corresponding alicyclic counterpart. For this reason, as presented in Figure 1, piperidine (pKb = 2.8) is significantly more basic than pyridine (pKb = 8.8).
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Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
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Direct alkylation is not a suitable method for synthesizing amines because it produces polyalkylated products. Gabriel synthesis is the most preferred method to exclusively make primary amines. The method uses phthalimide, which contains a protected form of nitrogen that participates in alkylation only once to predominantly give primary amines.
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Nitrous acid, a weak acid, is prepared in situ via the reaction of sodium nitrite with a strong acid under cold conditions. This nitrous acid prepared in situ reacts with primary arylamines to form arenediazonium salts. Such reactions are known as diazotization reactions. As shown in Figure 1, the formation of arenediazonium salts begins with the decomposition of nitrous acid in an acidic solution to give nitrosonium ions.
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