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Lande, Deepak
- Synthesis of Some New 3-(4-Phthalimidophenyl)-5-(Substituted Phenyl) 4- Isoxazoline Derivatives with Analgesic and Anti-Inflammatory Activities
Authors
1 Dep. of Pharmaceutical Chemistry, SGRS College of Pharmacy, Saswad, Pune, Maharashtra 412301, IN
Source
Asian Journal of Research in Chemistry, Vol 4, No 2 (2011), Pagination: 316-321Abstract
The derivatives of 3-(4-phthalimidophenyl)-5-(substituted-phenyl)-4-isoxazoline were synthesized, which were screened for their analgesic and anti-inflammatory activity in test animals. The analgesic activity of all compounds were found to be higher than their anti-inflammatory activity, Compounds 3b, 3e, 3h and 3l were found to be more active among the synthesized compounds.
Keywords
Thalidomide, Isoxazoline, Anti-Inflammatory, Hydroxylamine Hydrochloride.
- Design, Synthesis and Evaluation of Novel Phenothiazines as Antipsychotic Agents
Authors
1 Department of Pharmaceutical Chemistry, S.G.R.S College of Pharmacy, Saswad, Pune-413716, Maharashtra, IN
Source
Asian Journal of Research in Chemistry, Vol 3, No 4 (2010), Pagination: 906-910Abstract
The present work relates to novel phenothiazines derivatives as antipsychotic agents. The introduction of the Chlorpromazine (a Phenothiazine class drug) in 1952 was positive advance in the treatment of psychosis. Phenothiazines constitute one of the most active classes of compounds possessing diversified biological applications and are the most commonly used class of antipsychotic agents. Phenothiazines mainly act by antagonism of the D2 receptors and are thus useful for the treatment of the positive symptoms and have very little effect on negative symptoms or cognitive deficits.
In addition, blockade of dopamine D2 receptors leads to an increase in prolactin secretion and associated neuroendocrine disorders including gynecomastia, amenorrhea, and sexual dysfunction. The antipsychotic efficacy of typical neuroleptics is related to the D2 receptor blockade. D2 receptor is one of the G protein coupled receptors family that also includes the D3 and D4 receptor subtypes. And it was found that the D4 receptor density is elevated in schizophrenia.
About six fold increases in the D4 receptor subtype have been reported in schizophrenic brains, compared with normals. Autoradiographic analyses with the D4 selective ligand 3H-NGD 94-1 show D4 sites to be dense in rat and human hippocampus, hypothalamus, and neocortex, among other brain regions, and to be absent in the striatum. These findings suggested that a D4-specific compound might treat schizophrenia as effectively as Clozapine but without the D2 antagonist-mediated EPS or the Clozapine constellation of side effects.
We undertook a plan of building pyrazoline ring fused with the nucleus of phenothiazine. The preliminary pharmacological screening of the synthesized compounds revealed that out of the 12 compounds synthesized 6 compound (3a,3c,3d,3f,3j,3l) displayed significant activity.