Elgemeie Galal, Altalbawy Farag, Alfaidi Mohammed, Azab Rania, Hassan Atef
Department of Chemistry, Faculty of Science, Helwan University, Helwan.
National Institute of Laser Enhanced Sciences (NILES), Cairo University, Giza, Egypt.
Drug Des Devel Ther. 2017 Nov 28;11:3389-3399. doi: 10.2147/DDDT.S149615. eCollection 2017.
The present research describes the synthesis of novel 5-benzoyl--substituted-amino- and 5-benzoyl--sulfonylamino-4-alkylsulfanyl-2-pyridones - and - via the reaction of 2-benzoyl-3,3-bis(alkylthio)acrylonitriles - with -cyanoacetohydrazide and cyanoaceto--phenylsulfonylhydrazide , respectively. Also, the reactivity of the compounds - toward hydrazine hydrate to give product 1-pyrazolo[4,3-]pyridine derivative was studied. In addition, the reactivity of the - toward 1-cyanoacetyl-4 arylidenesemicarbazides - afforded 3,5-dihydro[1,2,4]triazolo[1,5-]pyridine-6-carbonitrile derivatives (-)-, which reacted with hydrazine hydrate to give 3-pyrazolo[4,3-][1,2,4]triazolo[1,5-]pyridine-6-carbonitrile derivatives -. The structures of the new products were characterized based on H nuclear magnetic resonance, C nuclear magnetic resonance, infrared, mass-spectroscopy, and elemental analyses. The products were screened in vitro for their antibacterial and antifungal activity properties.
本研究描述了新型5-苯甲酰基 - 取代氨基 - 和5-苯甲酰基 - 磺酰氨基 - 4-烷硫基 - 2-吡啶酮 - 和 - 的合成，分别通过2-苯甲酰基-3,3-双（烷硫基）丙烯腈 - 与 - 氰基乙酰肼和氰基乙酰 - 苯磺酰肼的反应。此外，还研究了化合物 - 对水合肼的反应性，以得到产物1-吡唑并[4,3 - ]吡啶衍生物 。另外， - 对1-氰基乙酰基-4-亚芳基氨基脲的反应性得到了3,5-二氢[1,2,4]三唑并[1,5 - ]吡啶-6-腈衍生物（ - ） - ，其与水合肼反应得到3-吡唑并[4,3 - ][1,2,4]三唑并[1,5 - ]吡啶-6-腈衍生物 - 。基于氢核磁共振、碳核磁共振、红外光谱、质谱和元素分析对新产品的结构进行了表征。对产物进行了体外抗菌和抗真菌活性筛选。
