- DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-α]IMIDAZOLE-3- CARBOXYLIC ACID AMIDES
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Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
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Page/Page column 98
(2009/07/03)
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- VIGABATRIN BIOISOTERES AND RELATED METHODS OF USE
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Compounds bioisoteric to vigabatrin and related methods of use.
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Page/Page column 7; 13-14
(2010/11/26)
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- New substrates and inhibitors of γ-aminobutyric acid aminotransferase containing bioisosteres of the carboxylic acid group: Design, synthesis, and biological activity
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A series of potential substrates of γ-aminobutyric acid aminotransferase (GABA-AT) with lipophilic bioisosteres of the carboxylic acid group (2-7) were synthesized and tested. Most of the synthesized compounds showed substrate activities with GABA-AT; 1H-tetrazole-5-propanamine (6) was the best of those tested. The potential time-dependent inhibitor of GABA-AT, 1H-tetrazole-5-(α-vinyl-propanamine) (8), was designed based on the structures of 6 and the antiepilepsy drug vigabatrin (4-aminohex-5-enoic acid, 1). The synthesized compound 8 showed time-dependent inhibition of GABA-AT, but its potency is lower than that of vigabatrin. Methylation of the tetrazole group in 8 resulted in loss of time-dependent activity, suggesting that the tetrazole ring, the carboxylate bioisostere, exists in its deprotonated form in the enzyme active site.
- Yuan, Hai,Silverman, Richard B.
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p. 1331 - 1338
(2007/10/03)
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- Synthesis of various 3-substituted 1,2,4-oxadiazole-containing chiral β3- and α-amino acids from Fmoc-protected aspartic acid
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Various 3-substituted chiral 1,2,4-oxadiazole-containing Fmoc-β 3- and α-amino acids were synthesized from FmoC-(L or D)-Asp(OtBu)-OH and Fmoc-L-Asp-OtBu, respectively, in three steps (i.e., condensation of an aspartyl derivative with different
- Hamze?, Abdallah,Hernandez, Jean-Franc?ois,Fulcrand, Pierre,Martinez, Jean
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p. 7316 - 7321
(2007/10/03)
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- Dithio and thiono esters, LVII: Synthesis of dithio and thiono esters of N-protected β- and γ-amino acids
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The N-protected β-aminonitriles 1 were transformed into the imidoester or thiolimidoester hydrochlorides 2 or 3 according to Pinner and sulfhydrolyzed with H2S to give the N-protected β-amino thiono esters 4 or dithio esters 5. Alkylation of th
- Brutsche,Hartke
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p. 271 - 276
(2007/10/02)
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- Acylation of Dibasic Compounds Containing Amino Amidine and Aminoguanidine Functions
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The site of acylation in difunctional compounds containing an amine and either an amidine or guanidine can be determined from the ultraviolet absorption spectrum of the acylated product.If the amidine or guanidine has been acylated, the product possesses a chromophore that is pH dependent, whereas if an amide was formed, the chromophore is independent of pH.
- Barker, Peter L.,Gendler, Paul L.,Rapoport, Henry
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p. 2455 - 2465
(2007/10/02)
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