New ibuprofen derivatives as H2S and NO donors as safer anti-inflammatory agents
Aim: Nonsteroidal anti-inflammatory drugs are expansively used worldwide. However, their prolonged administration is associated with serious side effects, especially gastrointestinal ulceration. Materials & methods: New ibuprofen derivatives hybridized with H2S- or NO-donating moieties were synthesized and evaluated for their anti-inflammatory activity and ulcerogenic effect. COX-1/COX-2 isozymes selectivity test for the most promising derivatives was performed. Molecular docking studies were performed. Results: Most of the compounds showed promising anti-inflammatory activity comparable to that of ibuprofen (% edema inhibition = 76.6 and ulcer index = 21.26) with much better gastrointestinal tract tolerance (ulcer indices ranging from 0 to 14.67), especially compound 2 -H2S donor- (% edema inhibition = 75.5 and ulcer index = 11.75) and compound 16 -NO donor- (% edema inhibition = 65.4 and ulcer index = 8.66).
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2019 |
|---|---|
| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
|---|---|
| Enthalten in: |
Future medicinal chemistry - 11(2019), 23 vom: 20. Dez., Seite 3029-3045 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Hassan, Ghaneya S [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Completed 15.07.2020 Date Revised 15.07.2020 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.4155/fmc-2018-0467 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM302849033 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM302849033 | ||
| 003 | DE-627 | ||
| 005 | 20231225111606.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2019 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.4155/fmc-2018-0467 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1009.xml |
| 035 | |a (DE-627)NLM302849033 | ||
| 035 | |a (NLM)31680552 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Hassan, Ghaneya S |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a New ibuprofen derivatives as H2S and NO donors as safer anti-inflammatory agents |
| 264 | 1 | |c 2019 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 15.07.2020 | ||
| 500 | |a Date Revised 15.07.2020 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: Nonsteroidal anti-inflammatory drugs are expansively used worldwide. However, their prolonged administration is associated with serious side effects, especially gastrointestinal ulceration. Materials & methods: New ibuprofen derivatives hybridized with H2S- or NO-donating moieties were synthesized and evaluated for their anti-inflammatory activity and ulcerogenic effect. COX-1/COX-2 isozymes selectivity test for the most promising derivatives was performed. Molecular docking studies were performed. Results: Most of the compounds showed promising anti-inflammatory activity comparable to that of ibuprofen (% edema inhibition = 76.6 and ulcer index = 21.26) with much better gastrointestinal tract tolerance (ulcer indices ranging from 0 to 14.67), especially compound 2 -H2S donor- (% edema inhibition = 75.5 and ulcer index = 11.75) and compound 16 -NO donor- (% edema inhibition = 65.4 and ulcer index = 8.66) | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a COX enzyme | |
| 650 | 4 | |a H2S donors | |
| 650 | 4 | |a ibuprofen | |
| 650 | 4 | |a safer anti-inflammatory agents | |
| 650 | 4 | |a ulcer index | |
| 650 | 7 | |a Anti-Inflammatory Agents, Non-Steroidal |2 NLM | |
| 650 | 7 | |a Nitric Oxide Donors |2 NLM | |
| 650 | 7 | |a Cyclooxygenase 1 |2 NLM | |
| 650 | 7 | |a EC 1.14.99.1 |2 NLM | |
| 650 | 7 | |a Cyclooxygenase 2 |2 NLM | |
| 650 | 7 | |a EC 1.14.99.1 |2 NLM | |
| 650 | 7 | |a Ibuprofen |2 NLM | |
| 650 | 7 | |a WK2XYI10QM |2 NLM | |
| 650 | 7 | |a Hydrogen Sulfide |2 NLM | |
| 650 | 7 | |a YY9FVM7NSN |2 NLM | |
| 700 | 1 | |a Hegazy, Gehan H |e verfasserin |4 aut | |
| 700 | 1 | |a Ibrahim, Noha M |e verfasserin |4 aut | |
| 700 | 1 | |a Fahim, Samar H |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Future medicinal chemistry |d 2009 |g 11(2019), 23 vom: 20. Dez., Seite 3029-3045 |w (DE-627)NLM194822109 |x 1756-8927 |7 nnns |
| 773 | 1 | 8 | |g volume:11 |g year:2019 |g number:23 |g day:20 |g month:12 |g pages:3029-3045 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.4155/fmc-2018-0467 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 11 |j 2019 |e 23 |b 20 |c 12 |h 3029-3045 | ||