It is well demonstrated that bacteria have become resistant to common medications recently and it is considered to be one of the major threats to human health. The research on innovative antimicrobial agents explores a vast and interesting subject area. Therefore, a series of new carbamate derivatives of sulfathiazole 6a-e, a common oral antimicrobial drug and methyl tryptophanate 8a-e, N-methyl α-amino acid ester containing indole moiety have been synthesized. Structures of the title products have been elucidated by spectral analyses like IR, NMR (¹H and ¹³C), mass and elemental composition. The compounds have been evaluated for their in vitro antimicrobial activity including minimum inhibitory concentrations (MICs). Whereas, three carbamate derivatives of sulfathiazole 6a, 6b and 6e and one derivative of methyl tryptophanate 8a show promising antibacterial activity in the range of MIC 2.88-8.14 µg/mL and it is a comparable activity of streptomycin (MIC = 3.14-7.43 µg/mL). Most of the compounds provide potent activity against E. coli which is equivalent to streptomycin (MIC = 3.14 µg/mL). The title compounds have been docked into the active site of E. coli DNA gyrase A enzyme to ensure the binding mode and the results demonstrate that a few compounds show better binding energies with enzyme than that of standard, streptomycin and associated with antibacterial activity.

中文翻译：

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磺胺噻唑和色氨酸甲酯的氨基甲酸酯：对抗DNA促旋酶A的合成，抗菌活性和对接研究

充分证明细菌最近已对常用药物产生抗药性，被认为是对人类健康的主要威胁之一。创新抗菌剂的研究探索了一个广阔而有趣的主题领域。因此，合成了一系列新的氨基甲酸酯噻唑6a-e（一种常用的口服抗菌药物）和色氨酸甲酯8a-e（含吲哚部分的N-甲基α-氨基酸酯）的一系列氨基甲酸酯衍生物。通过光谱分析，例如IR，NMR（¹ H和¹³ C），质量和元素组成，阐明了标题产物的结构。这些化合物已经过体外评估抗菌活性，包括最低抑制浓度（MIC）。磺胺噻唑6a，6b和6e的三种氨基甲酸酯衍生物和色氨酸8a的一种衍生物在MIC 2.88-8.14 µg / mL的范围内显示出令人鼓舞的抗菌活性，与链霉素的活性相当（MIC = 3.14-7.43 µg / mL）。毫升）。大多数化合物提供了对大肠杆菌的有效活性，相当于链霉素（MIC = 3.14 µg / mL）。标题化合物已停靠在大肠杆菌的活性位点中 DNA回旋酶一种确保结合模式的酶，结果表明，与标准链霉素相比，少数化合物与酶的结合能更好，并具有抗菌活性。