Aminothiols: synthesis and effect on chicken brain aminopeptidases

Weiss, B.; Hui, K.S.; Hui, M.; Lajtha, A.

Research Communications in Chemical Pathology and Pharmacology 62(1): 113-123

1988


ISSN/ISBN: 0034-5164
PMID: 3205972
Document Number: 308364
An amino acid derivative, leucinethiol, was reported to be a strong inhibitor of aminopeptidase activity. In order to obtain selective inhibitors of various brain aminopeptidases, we tested the inhibition by amino acid analogs of brain aminopeptidase activity. In particular, we synthesized the trifluoroacetyl derivatives of phenylalaninol, tyrosinol, and leucinol; leucinethiol; and phenylalaninethiol and measured their effect on soluble puromycin-sensitive aminopeptidase SI and SII purified in our laboratory. Two of the compounds, L-bis (1-thio-2-amino-4-methylpentane) dihydrochloride (TAMP) and L-bis (l-thio-2-amino-3-phenylpropane) dihydrochloride (TAPP), caused significant inhibition.

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