Synthesis and antimicrobial activity of 1-(benzo[b]thiophen-4-yl)-4-(2-(oxo, hydroxyl, and fluoro)-2-phenylethyl)piperazine and 1-(benzo[d]isothiazole-3-yl)-4-(2-(oxo, hydroxy, and fluoro)-2-phenylethyl)piperazine derivatives

VAIBHAV MISHRA; TEJPAL SINGH CHUNDAWAT

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Synthesis and antimicrobial activity of 1-(benzo[b]thiophen-4-yl)-4-(2-(oxo, hydroxyl, and fluoro)-2-phenylethyl)piperazine and 1-(benzo[d]isothiazole-3-yl)-4-(2-(oxo, hydroxy, and fluoro)-2-phenylethyl)piperazine derivatives

机译：1-（苯并[b]噻吩-4-基）-4-（2-（氧代，羟基和氟代）-2-苯基乙基）哌嗪和1-（苯并[d]异噻唑-3-的合成及其抗菌活性yl）-4-（2-（氧代，羟基和氟代）-2-苯基乙基）哌嗪衍生物

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Twenty-two compounds in a series of 1-(benzo[$b$]thiophen-4-yl)-4-(2-(oxo, hydroxy, and fluoro)-2-phenylethyl) piperazine and 1-(benzo[$d$]isothiazole-3-yl)-4-(2-(oxo, hydroxy, and fluoro)-2-phenylethyl)-piperazine derivatives were synthesized through nucleophilic substitution reaction of phenacyl bromides with hetero arylpiperazine, reduction, and then fluorination. Compound K2 showed potent activity against gram-negative bacterial stain P. aeruginosa with minimum inhibitory concentration (MIC) value of 12.5 μg/mL. This compound showed better inhibitory activity than the standard drug chloramphenicol. K4 against S. aureus , H2 against P. aeruginosa , and F4 against E. coli showed good inhibitory activity with MIC values of 62.5 μg/mL. Compounds K1, K2, K4, K8, F1, and F3 showed good inhibitory activity against fungal stain C. albicans with MIC values of 250 μg/mL. The crystal structure of F1 was determined by single-crystal XRD (CCDC 1832090).

机译：一系列1-（苯并[$ b $]噻吩-4-基）-4-（2-（氧，羟基和氟）-2-苯基乙基）哌嗪和1-（苯并[$]化合物通过苯甲酰溴与杂芳基哌嗪的亲核取代反应，合成d []异噻唑-3-基）-4-（2-（氧代，羟基和氟代）-2-苯基乙基）-哌嗪衍生物，还原，然后氟化。化合物K2显示出对革兰氏阴性细菌染色质P的有效活性。最小抑菌浓度（MIC）值为12.5μg/ mL的铜绿假单胞菌。该化合物显示出比标准药物氯霉素更好的抑制活性。 K4对抗 S。金黄色葡萄球菌，H2对 P。铜绿和F4对抗 E。大肠杆菌表现出良好的抑制活性，MIC值为62.5μg/ mL。化合物K1，K2，K4，K8，F1和F3显示出对真菌污点C的良好抑制活性。 MIC值为250μg/ mL的白色。 F1的晶体结构通过单晶XRD（CCDC 1832090）确定。

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《Turkish journal of chemistry》 |2019年第2期|共17页
作者
VAIBHAV MISHRA; TEJPAL SINGH CHUNDAWAT;
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中图分类化学;
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Piperazinebenzo$b$thiophenebenzo$d$isothiazolesynthesisantimicrobialcrystal structure;

机译：哌嗪苯并[$ b $]噻吩苯并[$ d $]异噻唑合成抗菌晶体结构;

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Synthesis and antimicrobial activity of 1-(benzo[b]thiophen-4-yl)-4-(2-(oxo, hydroxyl, and fluoro)-2-phenylethyl)piperazine and 1-(benzo[d]isothiazole-3-yl)-4-(2-(oxo, hydroxy, and fluoro)-2-phenylethyl)piperazine derivatives

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