Abstract

The biological uses of 2,7-naphthyridines have sparked great attention in recent years. For this reason, we synthesized a series of novel 2,7-naphthyridines derivatives and explored their spectrum and biological properties in this study. Substituted tetrahydro-1H-thiopyrano [3,4-c] pyridine-4-carbonitrile (III) was prepared by the reaction of 1-methyl piperidin-4-one (I) with CS₂, malononitrile, and triethylamine. The condensed thiopyrane (III) be converted to three-mercapto-7-methyl-1-morpholino-5,6,7,8-tetrahydro-2,7-naphthyridine-4-carbonitrile (IV) by reaction with morpholine. Composite (IV) was used as a starter in heterocyclic compound a series, such as the thieno[2,3-c][2,7]naphthyridines moiety (VIa–i). We used 1рamino-7-methyl-5-morpholino-6,7,8,9-tetrahydrothieno[2,3-c][2,7]naphthyrid ine-2-substituted (VIb, VIe, VIi) compounds as a precursor to create original heterocyclic moieties, namely: pyrimidothienonaphthyridino and pyridothieno naphthyridino in compounds (VII, VIII, IX, X, and XIa, b). Elemental analysis and spectral techniques (Fourier Transform Infrared (FT-IR), Nuclear magnetic resonance (¹H NMR, ¹³C NMR, and mass spectrum)) were affirmed to validate chemical constructions for the recent synthesized compounds. A number of compounds for antimicrobial activity were examined against a variety of bacterial and fungal strains. In addition, some of these compounds showed anticancer activity in liver and cells of breast cancer.

中文翻译：

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新型吗啉代-噻吩并[2,3-c][2,7]萘啶作为抗癌和抗微生物剂的新合成、反应和生物学研究

摘要

近年来，2,7-萘啶的生物用途引起了极大的关注。为此，我们合成了一系列新型 2,7-萘啶衍生物，并在本研究中探索了它们的光谱和生物学特性。通过 1-甲基哌啶-4-酮 ( I ) 与 CS ₂、丙二腈和三乙胺反应制备取代的四氢-1 H-噻吩并 [3,4- c ] 吡啶-4-甲腈 ( III )。缩合的硫吡喃 ( III ) 通过与吗啉反应转化为三巯基-7-甲基-1-吗啉代-5,6,7,8-四氢-2,7-萘啶-4-甲腈( IV )。复合（四) 被用作一系列杂环化合物的起始剂，例如噻吩并[2,3- c ][2,7]萘啶部分 ( VIa – i )。我们使用 1рamino-7-methyl-5-morpholino-6,7,8,9-tetrahydrothieno[2,3- c ][2,7]naphthyridine-2-取代 ( VIb , VIe , VIi ) 化合物作为前体创造原始杂环部分，即：化合物（VII、VIII、IX、X和XIa、b中的嘧啶并噻吩并萘啶基））。元素分析和光谱技术（傅里叶变换红外 (FT-IR)、核磁共振（¹ H NMR、¹³ C NMR 和质谱））被确认以验证最近合成化合物的化学结构。针对多种细菌和真菌菌株检查了许多化合物的抗微生物活性。此外，其中一些化合物在肝脏和乳腺癌细胞中显示出抗癌活性。