70181-28-1Relevant academic research and scientific papers
Synthesis, in silico, in vitro and in vivo evaluations of isatin aroylhydrazones as highly potent anticonvulsant agents
Emami, Saeed,Valipour, Mehdi,Kazemi Komishani, Fatemeh,Sadati-Ashrafi, Fatemehsadat,Rasoulian, Maria,Ghasemian, Majid,Tajbakhsh, Mahmood,Honarchian Masihi, Patrick,Shakiba, Aidin,Irannejad, Hamid,Ahangar, Nematollah
, (2021/05/10)
In this study, a series of new isatin aroylhydrazones (5a-e and 6a-e) was synthesized and evaluated for their anticonvulsant activities. The (Z)-configuration of compounds was confirmed by 1H NMR. In vivo studies using maximal electroshock (MES) and pentylenetetrazole (PTZ) models of epilepsy in mice revealed that while most of compounds had no effect on chemically-induced seizures at the higher dose of 100 mg/kg but showed significant protection against electrically-induced seizures at the lower dose of 5 mg/kg. Certainly, N-methyl analogs 6a and 6e were found to be the most effective compounds, displaying 100% protection at the dose of 5 mg/kg. Protein binding and lipophilicity (logP) of the selected compounds (6a and 6e) were also determined experimentally. In silico evaluations of title compounds showed acceptable ADME parameters, and drug-likeness properties. Distance mapping and docking of the selected compounds with different targets proposed the possible action of them on VGSCs and GABAA receptors. The cytotoxicity evaluation of 6a and 6e against SH-SY5Y and Hep-G2 cell lines indicated safety profile of compounds on the neuronal and hepatic cells.
Efficient synthesis of new 2,3-dihydrooxazole-spirooxindoles hybrids as antimicrobial agents
Tiwari, Shailendra,Pathak, Poonam,Sagar, Ram
supporting information, p. 2513 - 2516 (2016/07/07)
Two series of new 2,3-dihydrooxazole-spirooxindole derivatives were efficiently synthesized starting from N′-(2-oxoindolin-3-ylidene) benzohydrazide/N′-(2-oxoindolin-3-ylidene)-2-phenoxyacetohydrazide using designed synthetic route. Newly synthesized 2,3-
Facile synthesis of ninhydrin and isatin based hydrazones in water using PEG-OSO3H as a highly efficient and homogeneous polymeric acid-surfactant combined catalyst
Debnath, Kamalesh,Pathak, Sudipta,Pramanik, Animesh
, p. 4110 - 4115 (2013/07/26)
The synthesis of a series of biologically important ninhydrin and isatin based hydrazones has been carried out by refluxing easily synthesized novel N′-(chloro-aryl-methylene)-tert-butylcarbazates with ninhydrin and isatins in the presence of PEG-OSO3H as catalyst in water medium. The dual characteristic of PEG-OSO3H as a Br?nsted acid as well as a phase-transfer catalyst is successfully exploited in this synthesis. Reduced reaction time, operational simplicity, excellent yields of the products with high purity, and more importantly, easy recoverability, and reusability of the homogeneous polymeric catalyst make the reaction an attractive, economic, and sustainable green synthetic methodology.
Synthesis and fungicidal activity of some 1'-(substituted aryloxyaceto)spiro--2,2'-(1H)-diones and 2-aryl-oxadiazinoindoles
Ruab, Ali,Mishra, Bharati,Nizamuddin
, p. 526 - 528 (2007/10/02)
Several 1'-(substituted aryloxyacetamido)-spiro-3,2'(1H)-diones (III) and 2-aryl--oxadiazinoindoles (IV) have been synthesized and screened for their antifungal activity against Helminthosporium oryzae and Asperg
