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首页> 外文期刊>Journal of King Saud University >Synthesis, biological screening of novel long chain derivatives of 1,3-disubstituted-1H-pyrazol-5(4H)-one and 2-substituted-3H-1,4-phthalazin-1,4-dione: Structure-activity relationship studies
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Synthesis, biological screening of novel long chain derivatives of 1,3-disubstituted-1H-pyrazol-5(4H)-one and 2-substituted-3H-1,4-phthalazin-1,4-dione: Structure-activity relationship studies

机译：1,3-二取代-1H-吡唑-5（4H）-一和2-取代-3H-1,4-酞嗪-1,4-二酮的新型长链衍生物的合成，生物学筛选：构效关系研究

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The main purpose of this study is to synthesize novel heterocyclic derivatives of fatty acids which are also biologically important. The simple, efficient and one-pot synthesis of two novel series of 1-long chain alkanoyl/alkenoyl/hydroxyalkenoyl-3-methyl-1H-pyrazol-5(4H)-ones 2(a–e) and 2-long chain alkenoyl/hydroxyalkenoyl-3H-phthalazin-1,4-diones 3(b–e) is achieved by the reaction of ethylacetoacetate/phthalic anhydride and long chain alkyl/alkenyl/hydroxyalkenyl hydrazides 1(a–e) . Although some methods are available for the synthesis of phthalazindiones and pyrazolones, the development of a new synthetic method for the efficacious build up of heterocycles (phthalazindiones and pyrazolones) substituted with long alkanoyl/alkenoyl/hydroxyalkenoyl chain is an interesting challenge in the field of synthesis of novel compounds of fatty acids that includes heterocyclization and derivatization of fatty acids. Compounds 2(a–e) were synthesized by the cyclization reaction between ethylacetoacetate and long alkyl/alkenyl/hydroxyalkenyl chain hydrazides 1(a–e) . Compounds 3(b–e) were synthesized by the reaction of phthalic anhydride and long alkenyl/hydroxyalkenyl chain hydrazides 1(b–e) in absolute ethanol/glacial AcOH. Structures of all the newly synthesized compounds have been elucidated by means of IR, 1 H NMR, 13 C NMR and MS. Newly synthesized compounds were evaluated for in vitro antibacterial and antifungal activities and their structure–activity relationship studies have been carried out.
机译：这项研究的主要目的是合成新的脂肪酸杂环衍生物，它们在生物学上也很重要。简单，高效且一锅合成两个新颖的1长链烷酰基/链烯酰基/羟基链烯酰基-3-甲基-1H-吡唑-5（4H）-ones 2（a-e）和2长链链烯酰基通过羟基乙酰乙酸乙酯/邻苯二甲酸酐与长链烷基/烯基/羟基烯基酰肼1（a-e）的反应获得/羟基链烯酰基-3H-酞嗪-1,4-二酮3（b-e）。尽管有一些方法可用于合成邻苯二氮杂二酮和吡唑啉酮，但有效合成被长链烷酰基/链烯酰基/羟基链烯酰基链取代的杂环化合物（邻苯二氮杂酮和吡唑啉酮）的新方法的开发是一个有趣的挑战。新型脂肪酸化合物，包括脂肪酸的杂环化和衍生化。通过乙酰乙酸乙酯与长烷基/烯基/羟基烯基链酰肼1（a-e）之间的环化反应合成了化合物2（a-e）。化合物3（b-e）是由邻苯二甲酸酐与长链烯基/羟基烯基链酰肼1（b-e）在无水乙醇/冰醋酸中反应制得的。已经通过IR，1 H NMR，13 C NMR和MS阐明了所有新合成的化合物的结构。对新合成的化合物的体外抗菌和抗真菌活性进行了评估，并对其结构-活性关系进行了研究。

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