68944-99-0Relevant academic research and scientific papers
Design and synthesis of some new 1-phenyl-3/4-[4-(aryl/heteroaryl/alkyl-piperazine1-yl)-phenyl-ureas as potent anticonvulsant and antidepressant agents
Mishra, Chandra Bhushan,Kumari, Shikha,Tiwari, Manisha
, p. 603 - 617 (2016/07/06)
A series of 1-phenyl-3/4-[4-(aryl/heteroaryl/alkyl-piperazine1-yl)-phenyl-urea derivatives (29–42) were designed, synthesized and evaluated for their anticonvulsant activity by using maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) seizure tests. The acute neurotoxicity was checked by rotarod assay. Most of the test compounds were found effective in both seizure tests. Compound 30 (1-{4-[4-(4-chloro-phenyl)-piperazin-1-yl]-phenyl}-3-phenyl-urea) exhibited marked anticonvulsant activity in MES as well as scPTZ tests. The phase II anticonvulsant quantification study of compound 30 indicates the ED50value of 28.5?mg/kg against MES induced seizures. In addition, this compound also showed considerable protection against pilocarpine induced status epilepticus in rats. Seizures induced by 3-mercaptopropionic acid model and thiosemicarbazide were significantly attenuated by compound 30, which suggested its broad spectrum of anticonvulsant activity. Interestingly, compound 30 displayed better antidepressant activity than standard drug fluoxetine. Moreover, compound 30 appeared as a non-toxic chemical entity in sub-acute toxicity studies.
Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents
Kumari, Shikha,Mishra, Chandra Bhushan,Tiwari, Manisha
, p. 1092 - 1099 (2015/02/19)
A series of alkyl/aryl/heteroaryl piperazine derivatives (37-54) were designed and synthesized as potential anticonvulsant agents. The target compounds are endowed with satisfactory physicochemical as well as pharmacokinetic properties. The synthesized compounds were screened for their in vivo anticonvulsant activity in maximal electroshock (MES) and subcutaneous pentylenetetrazole (sc-PTZ) seizure tests. Further, neurotoxicity evaluation was carried out using rotarod method. Structure activity relationship studies showed that compounds possessing aromatic group at the piperazine ring displayed potent anticonvulsant activity. Majority of the compounds showed anti-MES activity whereas compounds 39, 41, 42, 43, 44, 50, 52, and 53 exhibited anticonvulsant activity in both seizure tests. All the compounds except 42, 46, 47, and 50 did not show neurotoxicity. The most active derivative, 45 demonstrated potent anticonvulsant activity in MES test at the dose of 30 mg/kg (0.5 h) and 100 mg/kg (4 h) and also delivered excellent protection in sc-PTZ test (100 mg/kg) at both time intervals. Therefore, compound 45 was further assessed in PTZ-kindling model of epilepsy which is widely used model for studying epileptogenesis. This compound was effective in delaying onset of PTZ-evoked seizures at the dose of 5 mg/kg in kindled animals and significantly reduced oxidative stress better than standard drug phenobarbital (PB). In result, compound 45 emerged as a most potent and safer anticonvulsant lead molecule.
Compounds Acting on CVS : Part I - Synthesis of 1-(p-Substituted-benzylaminophenyl)-4-arylpiperazines
Agarwal, Jagdish C.,Gupta, Y. K.,Bhargava, K. P.,Shanker, K.
, p. 512 - 514 (2007/10/02)
1-(p-Nitrophenyl)-4-arylpiperazines (II), prepared by the reaction of various arylpiperazines with p-chloronitrobenzene, on reduction with Raney nickel give the corresponding 1-(p-aminophenyl)-4-arylpiperazines (III) which are converted into 1-(p-arylideneaminophenyl)-4-arylpiperazines (IV) by condensation with appropriate araldehydes.Reduction of IV with Pd/C im DMF furnishes the title compounds.Some of these compounds have been found to possess marked cardiovascular activity.Compound IVk exhibits maximum hypotensive activity (38.2 percent) and blocks the carotid occlu-sion response without affecting noradrenaline response indicating a neural (central/peripheral) origin for the hypotensive action.
New indolic hypotensive agents.
Dubey,Verma,Shanker,Sinha,Bhargava,Kishor
, p. 640 - 641 (2007/10/04)
Seven substituted piperazino indoles were synthesized by the condensation of substituted piperazines with substituted indole-3-aldehyde, and evaluated for hypotensive activity. Only compound 2 exhibited promising hypotensive activity.
