- (α-aminoacyl)amino-substituted heterocycles and related compounds
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(Chemical Equation Presented) N-Protected-(aminoacyl)benzotriazoles 1a-e,g,i,j,1a′-c′ convert heterocyclic amines of the following series: thiazoles (3a and 3a′), benzothiazoles (3b and 3b′), benzimidazoles (3c and 3c′), thiadiazoles (3d), pyrimidones (9a
- Katritzky, Alan R.,El-Gendy, Bahaa El-Dien M.,Todadze, Ekaterina,Abdel-Fattah, Ashraf A. A.
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p. 5442 - 5445
(2008/12/20)
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- 6-Amino-2,4-lutidine carboxamides: α-aminoamide derivatives as systemic and topical inflammation inhibitors
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The development of new potential anti-inflammatory compounds resulting from the incorporation of α-aminoacid residues into 6-amino-2,4-lutidine afforded (N-protected) aminoamides with interesting inhibitory activity. Out of 28 tested compounds, 10 (5a, 5b, 7d, 8a, 8b, 8d, 10a, 11b, 12a and 12b) exerted potent (> 90%) inhibition in the carrageenan foot edema (CFE) rat model after oral administration or 0.4 mmol kg-1. Except for Cbz-glycyl, Cbz-alanyl, Fmoc-valyl and Cbz-alanyl-glycyl derivatives (5a, 5b, 7d and 11b), N-deprotection afforded more active compounds. Introduction of a glycyl residue in the previously studied highly active 3-fluorobenzamide 2, which led to 10a, maintained potent peripheral edema inhibition but had a detrimental effect in the acute TPA-induced mouse ear-swelling model. Glycylglycinamide 12a, which had an ID50 of 9.0 mg kg-1 in the CFE test, appeared to be the most efficient compound tested in this new series of non-carboxylic nonsteroidal anti-inflammatory drugs. Glycinamide 8a, although less potent in the same assay (14.3 mg kg-1), exerted a significant inhihitory effect in acute and chronic ear-swelling tests after topical application of 3 mg/ear.
- Duflos, Muriel,Courant, Jacqueline,Le Baut, Guillaume,Grimaud, Nicole,Renard, Pierre,Manechez, Dominique,Caignard, Daniel-Henri
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p. 635 - 645
(2007/10/03)
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- Synthesis and hypolipidemic activity of N-pyridinyl borodipeptidylamides
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A series of borodipeptide derivatives 7-9, which contain a 6-amino-2,4-dimethylpyridine moiety, was prepared in 3 steps.They were evaluated as hypolipidemic agents in rodents at 20 mg/kg per day.The methioninamide and phenylalaninamide derivatives were th
- Duflos, M.,Robert-Piessard, S.,Robert, J. M.,Andriamanamihaja, M.,Baut, G. Le,et al.
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p. 883 - 888
(2007/10/02)
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