Pyridazinone hybrids: Design, synthesis and evaluation as potential anticonvulsant agents

Partap, Sangh and Akhtar, Md. Jawaid and Yar, Mohammed Shahar and Hassan, Mohd. Zaheen and Siddiqui, Anees Ahmad (2018) Pyridazinone hybrids: Design, synthesis and evaluation as potential anticonvulsant agents. Bioorganic Chemistry, 77. 74 - 83. ISSN 0045-2068

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Abstract|ملخص البحث

A series of new hybrid benzothiazole containing pyridazinones derivatives were designed and synthesized fulfilling all the pharmacophoric requirements essential for the anticonvulsant activity. In-silico and in vitro studies revealed that some of these hybrid derivatives demonstrated admirable GABA AT inhibitory activity. An attempt has also been made to validate the results of in vitro GABA AT inhibition of the most potent compound SPS-5F (IC50 9.10 μM) through in vivo anticonvulsant screening. Compound SPS-5F administration significantly increases the whole brain GABA level, might be through the inhibition of GABA AT enzyme.

Item Type|تصنيف النتاج العلمي: Article| منشور علمي
Uncontrolled Keywords: Anticonvulsant, Pharmacophore, Benzothiazole, Pyridazinone, GABA AT
Subjects | مجال موضوع النشر: Chemistry
Pharmaceutical Sciences
Pharmacist
Pharmacy
Divisions | الكلية: College of Pharmacy > Pharmacy
Depositing User: Mohd. Zaheen Hassan
Date Deposited: 11 Mar 2019 06:46
Last Modified: 11 Mar 2019 06:46
URI: http://eprints.kku.edu.sa/id/eprint/3624

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