Synthesis, analgesic and anti-inflammatory evaluation of some novel quinazoline derivatives.
Journal - European journal of medicinal chemistry
Two series of some new 2,4,6-trisubstituted-quinazoline derivatives were prepared and screened for their analgesic, anti-inflammatory activity and acute toxicity. Four compounds were more potent analgesic agents than the reference drug Indomethacin and thirteen compounds showed significant anti-inflammatory activity. Seven compounds showed combined ability to inhibit both pain and inflammation. Compounds tested for acute toxicity showed no toxic symptoms or mortality rates 24 h post-administration implying their good safety margin.Copyright © 2010 Elsevier Masson SAS. All rights reserved.
Synthesis, analgesic and anti-inflammatory evaluation of some new 3H-quinazolin-4-one derivatives.
Journal - Archiv der Pharmazie (Germany )
In this study, we have synthesized a series of 3H-quinazolin-4-ones in order to obtain new compounds with potential analgesic and anti-inflammatory activity. The structures of the newly synthesized compounds were confirmed by means of infrared, nuclear magnetic resonance and mass spectroscopy. Some compounds were evaluated for their analgesic and anti-inflammatory activities by writhing and carrageenan-induced rat paw edema tests, respectively. In comparison to the standard drug indomethacine, compounds 4, 6c, 12-14, 16, 18, 19, and 22 induced significant reduction in the writhing response while compounds 6c, 12, 14, 16, 18, and 22 produced a good dose-dependent anti-inflammatory activity. The best dual analgesic / anti-inflammatory relative activity was observed with compounds 6c, 14, 16, 18, and 22.
|ISSN : ||0365-6233|
|Mesh Heading : ||Acetic Acid Analgesics Animals Anti-Inflammatory Agents, Non-Steroidal Carrageenan Edema Female Magnetic Resonance Spectroscopy Male Mass Spectrometry Mice Pain Pain Measurement Quinazolinones Rats Rats, Wistar Spectrophotometry, Infrared Structure-Activity Relationship chemistry pharmacology chemistry pharmacology chemically induced prevention & control chemically induced prevention & control chemistry pharmacology|
|Mesh Heading Relevant : ||chemical synthesis chemical synthesis chemical synthesis|
Synthesis, analgesic and anti inflammatory activities of some new fenamate analogues.
Journal - Arzneimittel-Forschung (Germany )
A series of fenamate quinazolinyl analogues, viz acids 6a-d, esters 6e-h, carbohydrazides 7a-d, arylidenes 8a-d, oxadiazol-2-ones 13a-d and oxadiazol-2-thiones 14a-d, have been prepared and screened for their analgesic (acetic acid-induced writhing), anti-inflammatory (carrageenan-induced rat paw edema) activities as well as their ulcerogenic effects. All the final compounds except 7a-d and 8a-d showed good dual activities. Compounds 6a, 6b, 6e, 6f, 13a and 14a showed activities comparable to that of mefenamic acid (CAS 61-68-7) in the acetic acid-induced writhing model as well as in the carrageenan-induced rat paw edema test at a dose level of 100 mg/ kg.Compounds 6a and 6b were highly ulcerogenic, while compounds 6e, 6f, 13a and 14a exhibited the lowest ulcerogenic effects.
|ISSN : ||0004-4172|
|Mesh Heading : ||Acetic Acid Analgesics, Non-Narcotic Animals Anti-Inflammatory Agents, Non-Steroidal Chemistry, Physical Edema Female Fenamates Indicators and Reagents Magnetic Resonance Spectroscopy Male Mice Pain Measurement Rats Spectrophotometry, Infrared Stomach Ulcer diagnostic use toxicity chemically induced prevention & control toxicity drug effects chemically induced pathology|
|Mesh Heading Relevant : ||chemical synthesis pharmacology chemical synthesis pharmacology chemical synthesis pharmacology|