Design, synthesis and biological screening of some novel celecoxib and etoricoxib analogs with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile
Copyright © 2016 Elsevier Inc. All rights reserved..
Two new series of 4,6-diaryl-3-cyanopyridine 4a-r and 1,3,5-triaryl-2-pyrazolines 6a-f and were prepared. The new compounds were evaluated for their in vitro COX-2 selectivity and in vivo anti-inflammatory activity. Compounds 4o,r and 6d,f had moderate to high selectivity index (S.I.) compared to celecoxib (selectivity indexes of 4.5, 3.14, 4.79 and 3.21, respectively) and also, showed in vivo anti-inflammatory activity approximately equal to or higher than celecoxib (edema inhibition %=60.5, 64.5, 59.3 and 59.3, after 3h, respectively) and the effective anti-inflammatory doses were (ED50=10.1, 7.8, 8.46 and 10.7mg/kg respectively, celecoxib ED50=10.8mg/kg) and ulcerogenic liability were determined for these compounds which showed promising activity by being more potent than celecoxib with nearly negligible ulcerogenic liability compared to celecoxib (reduction in ulcerogenic liability versus celecoxib=85, 82, 74 and 67%, respectively).
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2017 |
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| Erschienen: |
2017 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:70 |
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| Enthalten in: |
Bioorganic chemistry - 70(2017) vom: 09. Feb., Seite 173-183 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Alsayed, Shahinda S R [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 30.05.2017 Date Revised 02.12.2018 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bioorg.2016.12.008 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM267721625 |
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| 100 | 1 | |a Alsayed, Shahinda S R |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Design, synthesis and biological screening of some novel celecoxib and etoricoxib analogs with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile |
| 264 | 1 | |c 2017 | |
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| 500 | |a Date Revised 02.12.2018 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2016 Elsevier Inc. All rights reserved. | ||
| 520 | |a Two new series of 4,6-diaryl-3-cyanopyridine 4a-r and 1,3,5-triaryl-2-pyrazolines 6a-f and were prepared. The new compounds were evaluated for their in vitro COX-2 selectivity and in vivo anti-inflammatory activity. Compounds 4o,r and 6d,f had moderate to high selectivity index (S.I.) compared to celecoxib (selectivity indexes of 4.5, 3.14, 4.79 and 3.21, respectively) and also, showed in vivo anti-inflammatory activity approximately equal to or higher than celecoxib (edema inhibition %=60.5, 64.5, 59.3 and 59.3, after 3h, respectively) and the effective anti-inflammatory doses were (ED50=10.1, 7.8, 8.46 and 10.7mg/kg respectively, celecoxib ED50=10.8mg/kg) and ulcerogenic liability were determined for these compounds which showed promising activity by being more potent than celecoxib with nearly negligible ulcerogenic liability compared to celecoxib (reduction in ulcerogenic liability versus celecoxib=85, 82, 74 and 67%, respectively) | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Anti-inflammatory | |
| 650 | 4 | |a Cyanopyridine | |
| 650 | 4 | |a Cyclooxygenase inhibition | |
| 650 | 4 | |a Pyrazoline | |
| 650 | 7 | |a Anti-Inflammatory Agents |2 NLM | |
| 650 | 7 | |a Cyclooxygenase 2 Inhibitors |2 NLM | |
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| 650 | 7 | |a Etoricoxib |2 NLM | |
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| 700 | 1 | |a Elshemy, Heba A H |e verfasserin |4 aut | |
| 700 | 1 | |a Abdelgawad, Mohamed A |e verfasserin |4 aut | |
| 700 | 1 | |a Abdel-Latif, Mahmoud S |e verfasserin |4 aut | |
| 700 | 1 | |a Abdellatif, Khaled R A |e verfasserin |4 aut | |
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