Synthesis and anticonvulsant activity of some potent 5,6-bis aryl 1,2,4-triazines

Abstract

Abstract:In the present research, a series of 5,6-bis aryl 1,2,4-triazines 5a~5f were synthesized by condensation of various benzils 4a~4f with aminoguanidine bicarbonate and were screened in vivo, for their anticonvulsant and neurotoxicity studies. Compounds 5a, 5b and 5d were found to be potent molecules of this series, when compared with the reference drugs phenytoin sodium, diazepam and lamotrigine. The structures of these compounds were established by IR, 1 H NMR, 13 C NMR and mass spectroscopic data.

Synthesis of some novel 2-substituted-5-[isopropylthiazole] clubbed 1,2,4-triazole and 1,3,4-oxadiazoles as potential antimicrobial and antitubercular agents

“…Clubbed 1,2,4-triazole and 1,3,4-oxadiazole are new classes of azole anti-mycobacterials, which are proved to be highly active both in vitro and in vivo [8,9]. In continuation of our research on clubbed triazolyl-thiazoles [10][11][12][13][14] and clubbed triazolyl-isopropylthiazole, in previous communication it was proved isopropylthiazole moiety on coupling with other heterocyclic rings provides novel biologically active compounds that could be explored as potent antimicrobial and antitubercular agents [15]. The present study illustrates the details of further structural modifications carried out on clubbed isopropylthiazole with 1,3,4-oxadiazoles and 1,2,4-triazoles, studies its cytotoxicity, antimicrobial (bacterial and fungal) and antitubercular activity against H37Rv strain.…”

“…IR (KBr) n max, cm À1 : 3357 (NH), 1654 (C]N) 1. H NMR (DMSO-d 6 , 300 MHz) d:14.49 (s, 1H, N]C-SH, disappeared on D 2 O exchange),10.63 (s, 1H, N]CH), 7.6-7.9 (4H, phenyl), 7.61 (s, 1H, thiazole-C 5 ), 3.15 (m, 1H, isopropyl), 1.23 (d, J ¼ 8.5 Hz, 6H, CH 3 ) ppm 13. C NMR (DMSO-d 6 , 300 MHz) d: 168.31 (C]S), 164.44 (HC]N), 162.21 (thiazole C 4 ), 153.14 (thiazole C 2 ), 142.51 (triazole-C 5 ), 125-132 (Ar C 1 -C 6 ), 116.19 (thiazole-C 5 ), 30.123 (tertiary-1C-isopropyl), 23.12 (terminal 2CH 3 -isopropyl) ppm.…”

Design, Synthesis, and Docking Study of Pyrimidine–Triazine Hybrids for GABA Estimation in Animal Epilepsy Models

“…. Moreover, several researchers have worked on the anticonvulsant potential of pyrimidines and triazines in subsequent years and from their studies, it has been proved that both of these moieties contain antiseizure properties. The distance range such as A, D, and HBD, between the essential pharmacophoric elements of clinically used and designed compounds 4a–t are depicted in Table .…”

Design, Synthesis, and Biological Evaluation of Hydrazone Incorporated 1,2,4‐Triazines as Anticonvulsant Agents

“…Lamotrigine is a triazine derivative, which acts through the prolongation of voltage‐sensitive Na + channel's inactivation and appears to be effective against all types of generalized seizures . Results of recent anticonvulsant drug development investigations on related triazine analogues were also encouraging . Moreover, in the course of investigations for developing structurally novel anticonvulsants, a number of hydrazones containing an azomethine NHNCH proton were found to posses interesting seizure protective properties .…”