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Design and Development of Novel 2-(Morpholinyl)-N-substituted Phenylquinazolin-4-amines as Selective COX-II Inhibitor.

ABSTRACT: BACKGROUND:A novel series of 2-(Morpholin-4-yl)-N-phenylquinazolin-4- amine derivatives were synthesized and confirmed with spectral and elemental techniques. METHODS:The compounds were tested for analgesic and anti-inflammatory activity by various pain models in rodents whereas the selectivity towards COX-2 receptor is determined by in vitro assay. RESULTS:Screening results of compounds exhibited comparable biological activity with that of standard compound Indomethacin used for study. Compound 5d was found to be significantly potent with respect to its anti-inflammatory and analgesic activity with substantial COX-II selectivity. CONCLUSION:In silico analysis by molecular docking and 3D-QSAR studies justifies activity profile of compound 5d, suggesting that it may have potential for further evaluation and development as lead molecule for therapy in pain management.

SUBMITTER: Dravyakar BR

PROVIDER: S-EPMC6446527 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature

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Design and Development of Novel 2-(Morpholinyl)-N-substituted Phenylquinazolin-4-amines as Selective COX-II Inhibitor.

Dravyakar Bhushan R BR Khedekar Pramod B PB Khan Tabassum T Sherje Atul P AP Patel Kavit N KN Suvarna Vasanti V

Anti-inflammatory & anti-allergy agents in medicinal chemistry 20190101 1

<h4>Background</h4>A novel series of 2-(Morpholin-4-yl)-N-phenylquinazolin-4- amine derivatives were synthesized and confirmed with spectral and elemental techniques.<h4>Methods</h4>The compounds were tested for analgesic and anti-inflammatory activity by various pain models in rodents whereas the selectivity towards COX-2 receptor is determined by in vitro assay.<h4>Results</h4>Screening results of compounds exhibited comparable biological activity with that of standard compound Indomethacin us ...[more]

PMID: 30345927

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Project description:BackgroundWhether selective non-steroidal anti-inflammatory drugs (NSAIDs) has equally efficacy with non-selective NSAIDs in preventing heterotopic ossification (HO) after total hip arthroplasty (THA) was controversial. The purpose of this meta-analysis was to assess the efficacy and safety of selective NSAID versus non-selective NSAIDs for the prevention of HO after THA.MethodsPubMed, EMBASE, Cochrane Central Register of Controlled Trials, Web of Science, Google Search Engine, and China National Knowledge Infrastructure databases was searched for randomized controlled trials (RCTs) were comparing selective NSAID versus non-selective NSAIDs for preventing HO after THA. The primary outcomes were overall HO incidence, Brooker classification HO incidence, gastrointestinal side effects, the occurrence of excessive bleeding and discontinuation caused by gastrointestinal side effects (DGSE). Data were analyzed using Stata 12.0.ResultsA total of 8 RCTs involving 1636 patients were included in the meta-analysis. There was no significant difference between the nonselective NSAIDs group and the selective NSAIDs group in the overall incidence of HO (relative risk, RR = 0.91, 95% confidence intervals, CI 0.78-1.06, P = .203), Brooker I HO (RR = 1.02, 95% CI 0.85-1.23, P = .794), Brooker II HO (RR = 1.00, 95% CI 0.66-1.52, P = .996). Brooker III HO (RR = 0.98, 95% CI 0.37-2.62, P = .971). And the occurrence of excessive bleeding (RR = 0.67, 95% CI 0.24-1.92, P = .458). The selective NSAIDs group was associated with a significant decrease in gastrointestinal side effects (RR = 0.35, 95% CI 0.18-0.71, P = .004) and discontinuation caused by gastrointestinal side effects compared with the nonselective NSAIDs group (RR = 0.28, 95% CI 0.11-0.66, P = .004).ConclusionThe available evidence indicates selective NSAIDs were as effective as non-selective NSAIDs in preventing HO after THA. And selective NSAIDs were associated with less gastrointestinal side effects than non-selective NSAIDs. Considering the limitation of current meta-analysis, more RCTs need to identify the optimal NSAIDs drug for HO after THA.

Dataset Information

Design and Development of Novel 2-(Morpholinyl)-N-substituted Phenylquinazolin-4-amines as Selective COX-II Inhibitor.

Publications

Design and Development of Novel 2-(Morpholinyl)-N-substituted Phenylquinazolin-4-amines as Selective COX-II Inhibitor.

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