58137-72-7Relevant academic research and scientific papers
Synthesis, antimicrobial and cholinesterase enzymes inhibitory activities of indeno imidazoles and X-ray crystal structure of 3a,8a-dihydroxy-1,3- diphenyl-1,3,3a,8a-tetrahydro-indeno [1,2-d]imidazole-2,8-dione
Ghalib, Raza Murad,Hashim, Rokiah,Alshahateet, Solhe F.,Mehdi, Sayed Hasan,Sulaiman, Othman,Chan, Kit-Lam,Murugaiyah, Vikneswaran,Jawad, Ali
, p. 783 - 789 (2012)
Two indeno imidazoles have been synthesized by the reaction of ninhydrin with diphenylurea and diphenylthiourea. The structures have been determined by spectral analysis. The supramolecular behavior of 3a,8a-Dihydroxy- 1,3-diphenyl-1,3,3a,8a-tetrahydro-indeno[1,2-d]imidazole- 2,8-dione (1) was thoroughly analyzed and reported using X-ray single crystal technique and concepts. The presence of oxygen and nitrogen atoms led to very interesting supramolecularmotifs interactions such as nitrogen-oxygen, nitrogen- nitrogen, oxygen-oxygen, nitrogen-hydrogen, and oxygen- hydrogen. 3a,8a-dihydroxy-1,3- diphenyl-2-thioxo-2,3,3a,8atetrahydro- 1H-indeno[1,2-d]imidazol-8-one 2 showed good antibacterial activity against B. subtilis and P. aeruginosa, while 3a,8a-dihydroxy-1,3-diphenyl-1,3,3a,8a-tetrahydroindeno[ 1,2-d]imidazole-2,8- dione 1 only showed antibacterial activity against P. aeruginosa. Both of 1 and 2 were inactive against C. albicans. Derivative 2 demonstrated good cholinesterase enzyme activity unlike derivative 1 which has weak inhibitory activity against these enzymes. Furthermore, 2 was found to be a selective butyrylcholinesterase enzyme inhibitor that has potential use for prevention of further neurodegeneration as well for symptomatic treatment of Alzheimer patients. Springer Science+Business Media, LLC 2012.
Synthesis of N-1′, N-3′-disubstituted spirohydantoins and their anticonvulsant activities in pilocarpine model of temporal lobe epilepsy
Yang, Chen,Schanne, Francis A.X.,Yoganathan, Sabesan,Stephani, Ralph A.
, p. 2912 - 2914 (2016/06/06)
Herein we report the synthesis and anticonvulsant activity of a library of eighteen new compounds that are structural mimics of phenytoin. These class of compounds contain a N-1′, N-3′-disubstituted spirohydantoin scaffold, where the N-1′ and N-3′ positions are modified with an alkyl group or aryl group. Of the eighteen compounds synthesized and tested, compound 5c showed the best anticonvulsant activity. It completely prevented the precursor events of motor seizure in the pilocarpine model of temporal lobe epilepsy. Additionally, ten of the analogs were more effective than phenytoin when compared using the Racine's score in the pilocarpine model. Based on the structure activity relationship (SAR), we concluded that alkyl groups (ethyl, propyl or cyclopropyl) at N-3′ position and 4-nitro phenyl group at N-1′ position are desirable.
Synthesis and anticonvulsant activity of some 2,4-disubstituted-2,4-benzodiazocine-1,3,5,6-tetrones, 1-mono and 1,3- disubstituted indenoimidazoles and 2-substituted imidazoisoindoles
Sarra,Stephani
, p. 81 - 91 (2007/10/03)
1-Mono and 1,3- disubstituted indeno[1,2-d] imidazolones were synthesized by reaction of appropriately mono- and disubstituted ureas with ninhydrin, in aqueous alcohol and heat. Oxidation of these with sodium metaperiodate formed the corresponding imidazo
