|
|
| | PROGLUMETACIN MALEATE Basic information |
| Product Name: | PROGLUMETACIN MALEATE | | Synonyms: | PROGLUMETACIN MALEATE;Proglumetacine;1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-, 2-[4-[3-[[4-(benzoylamino)-5-(dipropylamino)-1,5-dioxopentyl]oxy]propyl]-1-piperazinyl]ethyl ester (9CI);1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-, 2-[4-[3-[[4-(benzoylamino)-5-(dipropylamino)-1,5-dioxopentyl]oxy]propyl]-1-piperazinyl]ethyl ester, (+-)-;1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid 2-[4-[3-[[4-(benzoylamino)-5-(dipropylamino)-1,5-dioxopentyl]oxy]propyl]-1-piperazinyl]ethyl ester;PROGLUMETACIN | | CAS: | 57132-53-3 | | MF: | C46H58ClN5O8 | | MW: | 844.43 | | EINECS: | | | Product Categories: | | | Mol File: | 57132-53-3.mol |  |
| | PROGLUMETACIN MALEATE Chemical Properties |
| solubility | DMSO (Slightly), Methanol (Slightly, Heated, Sonicated) | | form | Solid | | color | White to Pale Yellow |
| | PROGLUMETACIN MALEATE Usage And Synthesis |
| Uses | Proglumetacin Dioxalate is a new non-steroidal anti-inflammatory drug. | | Definition | ChEBI: A carboxylic ester obtained by formal condensation of the carboxy group of indometacin with the hydroxy group of 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl N2-benzoyl-N,N-dipropy
-alpha-glutaminate. Used (as its dimaleate salt) to control pain and inflammation associated with musculoskeletal and joint disorders. Following oral administration, it is metabolised to indometacin and proglumide, a drug with antisecretor
effects that helps prevent injury to the stomach lining. | | Synthesis | The reaction of N-benzoyl-N_x0002_,
N_x0002_-di-n-propyl-dl-isoglutamin (proglumide) with 1-(3-chloropropyl)-4-(2-hydroxyethyl)-piperazine
obtained from 1-(2-hydroxyethyl)piperazine
and 1-bromo-3-chloropropane by
means of sodium methanolate in DMSO at
105C gives N--N_x0002_-(2-hydroxyethyl)
piperazine, which is then condensated
with Indomethacin (1-(p-chlorobenzoyl)-
5-methoxy-2-methylindole-3-acetic acid)
by means of dicyclohexylcabodiimide and
NaHCO3 in ethyl acetate .
 | | in vivo | Proglumetacin (Sprague-Dawley rats, 0-30 mg/kg, Orally, once) dose-dependently inhibits accumulation of pouch exudate[1]. | Animal Model: | Sprague-Dawley rats (6 weeks) | | Dosage: | 0, 0.3, 3, 9, 30 mg/kg | | Administration: | Orally, once | | Result: | Caused dose-dependent reduction of leukocyte migration into the pouch exudate, caused 49.2% inhibition at 30 mg/kg; and markedly decreased the prostaglandin E2 content of the pouch exudate, but tended to increase the leukotriene B 4 content. |
|
| | PROGLUMETACIN MALEATE Preparation Products And Raw materials |
|