Abstract
A series of novel substituted quinazolin-4(3H)-one derivatives were synthesized and screened in vivo for their antihypertensive activities. Out of eighteen synthesized compounds, seven i.e. 2a, 2c, 4a, 4d, 5d, 6a & 6b compounds have shown hypotensive effect and produced bradycardia. These compounds have shown better activity than reference drug Prazosin (which acts as anti-hypertensive agent by α1 blocking action). All the compounds have shown ALD50>1000mg/kg with maximum in 2c & 4d (>1200mg/kg).
Keywords: Antihypertensive, alpha adrenoceptors, bradycardia, ALD50, N, N’ dimethyl amine, NE response, piperazine, quinazolinone.
Graphical Abstract
Central Nervous System Agents in Medicinal Chemistry
Title:Synthesis and Antihypertensive Activity of Novel Quinazolin-4(3H)-one Derivatives
Volume: 14 Issue: 1
Author(s): Seema R. Pathak, Vineet Malhotra, Rajendra Nath and Kripa Shanker
Affiliation:
Keywords: Antihypertensive, alpha adrenoceptors, bradycardia, ALD50, N, N’ dimethyl amine, NE response, piperazine, quinazolinone.
Abstract: A series of novel substituted quinazolin-4(3H)-one derivatives were synthesized and screened in vivo for their antihypertensive activities. Out of eighteen synthesized compounds, seven i.e. 2a, 2c, 4a, 4d, 5d, 6a & 6b compounds have shown hypotensive effect and produced bradycardia. These compounds have shown better activity than reference drug Prazosin (which acts as anti-hypertensive agent by α1 blocking action). All the compounds have shown ALD50>1000mg/kg with maximum in 2c & 4d (>1200mg/kg).
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Cite this article as:
Pathak R. Seema, Malhotra Vineet, Nath Rajendra and Shanker Kripa, Synthesis and Antihypertensive Activity of Novel Quinazolin-4(3H)-one Derivatives, Central Nervous System Agents in Medicinal Chemistry 2014; 14 (1) . https://dx.doi.org/10.2174/1871524914666140825144729
DOI https://dx.doi.org/10.2174/1871524914666140825144729 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
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