Proglumetacin
Title: Proglumetacin
CAS Registry Number: 57132-53-3
CAS Name: 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
Additional Names: (±)-N-[2-[1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetoxy]ethyl]-N¢-[3-(N-benzoyl-N¢,N¢-di-n-propyl-DL-isoglutaminoyl)oxypropyl]piperazine
Molecular Formula: C46H58ClN5O8
Molecular Weight: 844.43
Percent Composition: C 65.43%, H 6.92%, Cl 4.20%, N 8.29%, O 15.16%
Literature References: Deriv of indomethacin, q.v. Prepn: F. Makovec et al., DE 2535799 corresp to US 3985878 (both 1976 to Rotta). Series of articles on pharmacology, mechanism of action, safety: Arzneim.-Forsch. 29, 1116-1129 (1979). Bioavailability study: A. A. Bignamini, P. L. Casula, Curr. Med. Res. Opin. 6, 299 (1979). Clinical evaluation: J. Münzenberg, S. Tachibana, Pharmatherapeutica 2, 279 (1980); P. Loizzi et al., ibid. 285. Mutagenicity study: R. Vidal y Plana et al., Farmaco Ed. Prat. 33, 543 (1978). Toxicity data for dimaleate: A. L. Rovati et al., Arzneim.-Forsch. 29, 1116 (1979).
 
Derivative Type: Dimaleate
CAS Registry Number: 59209-40-4
Additional Names: Protacine
Manufacturers' Codes: CR-604
Trademarks: Afloxan (Rottapharm); Miridacin (Taiho); Protaxon (Opfermann); Proxil (Rottapharm)
Molecular Formula: C46H58ClN5O8.2C4H4O4
Molecular Weight: 1076.58
Percent Composition: C 60.24%, H 6.18%, Cl 3.29%, N 6.51%, O 23.78%
Properties: Crystals from ethanol, mp 146-148°. LD50 in male mice, rats (mg/kg): 262, 450 orally (Rovati).
Melting point: mp 146-148°
Toxicity data: LD50 in male mice, rats (mg/kg): 262, 450 orally (Rovati)
 
Therap-Cat: Anti-inflammatory.
Keywords: Anti-inflammatory (Nonsteroidal); Arylacetic Acid Derivatives.

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