92513-17-2Relevant academic research and scientific papers
A new n-substituted 1h-isoindole-1,3(2h)-dione derivative— synthesis, structure and affinity for cyclooxygenase based on in vitro studies and molecular docking
Szkatu?a, Dominika,Krzy?ak, Edward,Stanowska, Paulina,Duda, Magdalena,Wiatrak, Benita
, (2021/07/19)
Isoindoline-1,3-dione derivatives constitute an important group of medicinal substances. In this study, nine new 1H-isoindole-1,3(2H)-dione derivatives and five potential pharmacophores were obtained in good yield (47.24–92.91%). The structure of the new
Synthesis and in vivo Anti-inflammatory Evaluation of Piperazine Derivatives Containing 1,4-Benzodioxan Moiety
Liu, Zhi-Ping,Gong, Chang-Da,Xie, Long-Yan,Du, Xiu-Li,Li, Yang,Qin, Jie
, p. 421 - 426 (2019/07/12)
Six piperazine derivatives 6a–f containing 1,4-benzodioxan moiety have been synthesized and characterized by 1H NMR, ESI-MS and elemental analysis. The structure of 6d was further confirmed by single crystal X-ray diffraction. All these novel c
Design, synthesis, in vitro and in vivo evaluation of novel pyrrolizine-based compounds with potential activity as cholinesterase inhibitors and anti-Alzheimer's agents
El-Sayed, Nehad Abou-Elmagd,Farag, Awatef El-Said,Ezzat, Manal Abdel Fattah,Akincioglu, Hulya,Gül?in, ?lhami,Abou-Seri, Sahar Mahmoud
, (2019/10/05)
Novel series of pyrrolizine based compounds (4–6 and 9–11) were designed, synthesized and evaluated as potential anti-Alzheimer agents. Most of the tested compounds showed selectivity to hAChE over hBChE and effectively inhibited self–induced amyloid beta
3-Nitrotriazole-based piperazides as potent antitrypanosomal agents
Papadopoulou, Maria V.,Bloomer, William D.,Rosenzweig, Howard S.,O'Shea, Ivan P.,Wilkinson, Shane R.,Kaiser, Marcel
supporting information, p. 325 - 334 (2015/09/22)
Novel linear 3-nitro-1H-1,2,4-triazole-based piperazides were synthesized and evaluated as antitrypanosomal agents. In addition, some bisarylpiperazine-ethanones which were formed as by-products were also screened for antiparasitic activity. Most 3-nitrotriazole-based derivatives were potent and selective against Trypanosoma cruzi parasites, but only one displayed these desired properties against Trypanosoma brucei rhodesiense. Moreover, two 3-nitrotriazole-based chlorophenylpiperazides were moderately and selectively active against Leishmania donovani. Although the bisarylpiperazineethanones were active or moderately active against T. cruzi, none of them demonstrated an acceptable selectivity. In general, 3-nitrotriazole-based piperazides were less toxic to host L6 cells than the previously evaluated 3-nitrotriazole-based piperazines and seven of 13 were 1.54-to 31.2-fold more potent antichagasic agents than the reference drug benznidazole. Selected compounds showed good ADMET characteristics. One potent in vitro antichagasic compound (3) was tested in an acute murine model and demonstrated antichagasic activity after a 10-day treatment of 15 mg/kg/day. However, neither compound 3 nor benznidazole showed a statistically significant P value compared to control due to high variability in parasite burden among the untreated animals. Working as prodrugs, 3-nitrotriazole-based piperazides were excellent substrates of trypanosomal type I nitroreductases and constitute a novel class of potentially effective and more affordable antitrypanosomal agents.
Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)
Steinhagen, Henning,Gerisch, Michael,Mittendorf, Joachim,Schlemmer, Karl-Heinz,Albrecht, Barbara
, p. 3187 - 3190 (2007/10/03)
A new class of PARP-1 inhibitors, namely substituted fused uracil derivatives were synthesised. Starting from a derivative with an IC50=2 μM the chemical optimisation program led to compounds with more than a 100-fold increase in potency (ICsu
