175921-95-6Relevant articles and documents
Synthesis and Anticholinesterase Activity Evaluation of Asymmetric Azines
Figueredo, Andreza S.,Queiroz, Jaqueline E.,Dias, Lucas D.,Vidal, Hérika D. A.,Machado, Ingrid V.,Vila Verde, Giuliana M.,Aquino, Gilberto L. B.
, p. 544 - 549 (2019)
Azines or di-imines are compounds containing R1R2C=N-N=CR3R4 fragment in its structure. These compounds have received special attention due to their importance as intermediates in the synthesis of drugs and substances with diverse pharmacological activities. In this research, twelve compounds derived of asymmetric azines of aryl aldehydes and aryl ketones were synthesized by microwave assisted irradiation, and their ability to inhibit acetylcholinesterase (AChE) enzyme was tested using the Ellman method. Among the evaluated azines, five compounds were able to inhibit AChE, especially compounds (7E, 8E)-1-benzylidene-2-(1-(4-nitrophenyl)ethylidene)hydrazine (7) and (7E,8E)-2-(1-(4-nitrophenyl)ethylidene)-1-((pyridin-2-yl)methylene)hydrazine (14), which showed percentage inhibition of 18.34% and 17.43% at concentrations of 22.46 and 10 μM, respectively.
Diarylsemicarbazones: Synthesis, antineoplastic activity and topoisomerase I inhibition assay
Asis, Silvia E.,Bruno, Ana M.,Martinez, Andrea R.,Sevilla, Maria V.,Gaozza, Carlos H.,Romano, Alejandra M.,Coussio, Jorge D.,Ciccia, Graciela
, p. 517 - 523 (2007/10/03)
A series of diarylsemicarbazones was synthesized and tested against human neoplastic cell lines. The more active members have a 1-naphthyl ring at the carbamidic nitrogen, and chloro, dimethylamino or nitro group substituents at the benzylidene moiety. None of these showed affinity to DNA. One of the more active compounds was tested as a topoisomerase I inhibitor and showed a potent effect. SAR studies demonstrated linear correlation between lypophilicity and activity on the most sensitive lines and a definite conformational shape for antineoplastic action. Copyright (C) 1999 Elsevier Science S.A.