- N-ALKYLATED AMINO ACIDS AND OLIGOPEPTIDES, USES THEREOF AND METHODS FOR PROVIDING THEM.
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The invention relates to the synthesis of amphiphilic amino acid derivatives, in particular to a method for the N-alkylation of an unprotected amino acid or the N-terminus of an oligopeptide substrate, comprising reacting said unprotected amino acid or oligopeptide substrate with an alcohol, e.g. a fatty alcohol, in the presence of a homogeneous transition metal catalyst.
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Page/Page column 17-19; 34-36; 47; 48
(2018/10/25)
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- New insights into molecular recognition of 1,1-bisphosphonic acids by farnesyl diphosphate synthase
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As part of our project pointed at the search of new antiparasitic agents against American trypanosomiasis (Chagas disease) and toxoplasmosis a series of 2-alkylaminoethyl-1-hydroxy-1,1-bisphosphonic acids has been designed, synthesized and biologically evaluated against the etiologic agents of these parasitic diseases, Trypanosoma cruzi and Toxoplasma gondii, respectively, and also towards their target enzymes, T. cruzi and T. gondii farnesyl pyrophosphate synthase (FPPS), respectively. Surprisingly, while most pharmacologically active bisphosphonates have a hydroxyl group at the C-1 position, the additional presence of an amino group at C-3 resulted in decreased activity towards either T. cruzi cells or TcFPPS. Density functional theory calculations justify this unexpected behavior. Although these compounds were devoid of activity against T. cruzi cells and TcFPPS, they were efficient growth inhibitors of tachyzoites of T. gondii. This activity was associated with a potent inhibition of the enzymatic activity of TgFPPS. Compound 28 arises as a main example of this family of compounds exhibiting an ED50 value of 4.7 μM against tachyzoites of T. gondii and an IC50 of 0.051 μM against TgFPPS.
- Ferrer-Casal, Mariana,Li, Catherine,Galizzi, Melina,Stortz, Carlos A.,Szajnman, Sergio H.,Docampo, Roberto,Moreno, Silvia N.J.,Rodriguez, Juan B.
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p. 398 - 405
(2014/01/17)
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- Benzolactam derivatives
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A benzolactam derivative represented by the following formula (I): STR1 wherein n represents an integer of from 1 to 3; R 1 represents a straight- or branched-chain alkyl group or an aralkyl group; R 2 represents a straight- or branched-chain alkyl group; R 3 and R 4 independently represent a hydrogen atom or a straight- or branched-chain alkyl group, and when R 3 and R 4 are adjacent each other on the phenyl group, they may be combined to form a cycloalkyl ring together with two carbon atoms of the phenyl group to which R 3 and R 4 bind, and said cycloalkyl ring may optionally have one or more substituents; and a anti-retroviral agent comprising the same as an active ingredient.
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