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Synthetic and antimicrobial studies of N‐substituted‐pyrazoline‐based new bisheterocycles
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-03-02 , DOI: 10.1002/jhet.3910 Shehneela Nisa 1 , Mohamad Yusuf 1
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-03-02 , DOI: 10.1002/jhet.3910 Shehneela Nisa 1 , Mohamad Yusuf 1
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In the present study, the four series of N‐acetyl/N‐carbothioamide/N‐carboxamide/N‐phenyl‐based new bispyrazolines have been synthesized. These symmetrical bisheterocyclic products were prepared efficiently from the ring‐closure reactions of new bischalcones 2a‐d with appropriate cyclizing agents (hydrazine hydrate, thiosemicarbazide, semicarbazide, and phenyl hydrazine) under the alkaline ethanolic conditions. The compounds 2a‐d were obtained by treating hydroxyl‐substituted chalcone 1 with various dihalogenated reagents (α,α′‐dibromo‐o/m/p‐xylene and 4,4′‐bischloromethyl‐diphenyl) in anhydrous K2CO3/dry acetone/Bu4N+I− medium. The structures of all the newly synthesized products have been authenticated with the help of their IR, 1H‐NMR, 13C‐NMR, and ESI‐MS spectral data and their purity was corroborated with the help of elemental analysis and thin‐layer chromatography results. The in vitro antimicrobial screening of the newly synthesized intermediates and final bisheterocycles has also been performed by using the serial tube dilution technique against the selected number of microorganisms. The final bisheterocycles revealed better antibacterial and antifungal potencies as compared to their corresponding bischalcones. Among the symmetrical bisheterocyclic products, N‐acetyl and N‐carbothioamide‐substituted bispyrazolines were found to exhibit potential antimicrobial properties than the other products.
中文翻译：
基于N取代吡唑啉的新型双环杂环化合物的合成和抗菌研究
在本研究中，四个系列的ñ -乙酰基/ Ñ硫代甲酰胺/ Ñ甲酰胺/ Ñ基于苯基新bispyrazolines已经合成。这些对称的双杂环化合物是通过在碱性乙醇条件下，将新的比沙尔康酮2a-d与适当的环化剂（水合肼，硫代氨基脲，氨基脲和苯基肼）进行闭环反应而有效制备的。化合物2a-d是通过在无水K 2 CO中用各种二卤代试剂（α，α'-二溴-o / m /对二甲苯和4,4'-双氯甲基-二苯基）处理羟基取代的查尔酮1而获得的。3 /无水丙酮/卜4 Ñ +我-平台。所有新合成产物的结构均已通过IR，1 H-NMR，13 C-NMR和ESI-MS光谱数据进行了鉴定，其纯度已通过元素分析和薄层色谱法得到证实结果。通过使用连续管稀释技术针对选定数量的微生物，还对新合成的中间体和最终的双杂环化合物进行了体外抗菌筛选。与相应的比沙可康宁相比，最终的双环杂环菌具有更好的抗菌和抗真菌功效。在对称的双环产物中，N发现乙酰基和N-碳硫酰胺取代的双吡唑啉比其他产品具有潜在的抗菌特性。
更新日期：2020-03-03
中文翻译：
基于N取代吡唑啉的新型双环杂环化合物的合成和抗菌研究
在本研究中，四个系列的ñ -乙酰基/ Ñ硫代甲酰胺/ Ñ甲酰胺/ Ñ基于苯基新bispyrazolines已经合成。这些对称的双杂环化合物是通过在碱性乙醇条件下，将新的比沙尔康酮2a-d与适当的环化剂（水合肼，硫代氨基脲，氨基脲和苯基肼）进行闭环反应而有效制备的。化合物2a-d是通过在无水K 2 CO中用各种二卤代试剂（α，α'-二溴-o / m /对二甲苯和4,4'-双氯甲基-二苯基）处理羟基取代的查尔酮1而获得的。3 /无水丙酮/卜4 Ñ +我-平台。所有新合成产物的结构均已通过IR，1 H-NMR，13 C-NMR和ESI-MS光谱数据进行了鉴定，其纯度已通过元素分析和薄层色谱法得到证实结果。通过使用连续管稀释技术针对选定数量的微生物，还对新合成的中间体和最终的双杂环化合物进行了体外抗菌筛选。与相应的比沙可康宁相比，最终的双环杂环菌具有更好的抗菌和抗真菌功效。在对称的双环产物中，N发现乙酰基和N-碳硫酰胺取代的双吡唑啉比其他产品具有潜在的抗菌特性。
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