Synthesis and biological evaluation of imidazoline derivatives as potential CNS and CVS agents

[Display omitted] A series of substituted imidazoline derivatives were synthesized and characterized. Compounds were tested in-vivo for their antihypertensive, analgesic, antiaggressive, depressant, antidepressant, and ALD50 activities. The compounds 3a, 3c, 4c, 5a, and 6c showed cardiovascular as w...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2020-12, Vol.30 (23), p.127595-127595, Article 127595
Hauptverfasser: Malhotra, Vineet, Vats, Monika, Nath, Rajendra, Mehta, Simpi, Kumar, Rakesh, Bhalla, Manish, Sinha, J.N., Shanker, K., Pathak, Seeema R.
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Sprache:eng
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Zusammenfassung:[Display omitted] A series of substituted imidazoline derivatives were synthesized and characterized. Compounds were tested in-vivo for their antihypertensive, analgesic, antiaggressive, depressant, antidepressant, and ALD50 activities. The compounds 3a, 3c, 4c, 5a, and 6c showed cardiovascular as well as central nervous system activities and are potential candidate as drug among all fifteen compounds tested. All these compounds have shown better activity for antihypertensive, analgesic, antiaggressive, and depressant-antidepressant, properties than reference compounds clonidine, morphine, diazepam, and imipramine respectively. Most of the compounds have shown ALD50 > 500 mg/kg with maximum in 4a and 5a (>1000 mg/kg).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2020.127595