Central Nervous System Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Central Nervous System Agents)

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Synthesis and Antihypertensive Activity of Novel Quinazolin-4(3H)-one Derivatives

Author(s): Seema R. Pathak, Vineet Malhotra, Rajendra Nath, Kripa Shanker.

Graphical Abstract:


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.

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Article Details

VOLUME: 14
ISSUE: 1
Year: 2014
Page: [34 - 38]
Pages: 5
DOI: 10.2174/1871524914666140825144729