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Synthesis and antihypertensive activity of some ester progenitors of methyldopa.

Abstract：

:A variety of esters of methyldopa was synthesized with the objective of obtaining derivatives that would be more efficiently absorbed from the gastrointestinal tract than the free amino acid and would undergo conversion to methyldopa readily in the blood or target tissues. Two of the esters, alpha-pivaloyloxyethyl (4u) and alpha-succinimidoethyl (4w), were found to be more potent antihypertensive agents than methyldopa in animal models and were selected for further study in man. The amino esters were prepared by three different methods, including direct esterification of methyldopa without the use of N- or O-protecting groups.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Saari WS,Freedman MB,Hartman RD,King SW,Raab AW,Randall WC,Engelhardt EL,Hirschmann R,Rosegay A,Ludden CT,Scriabine A

doi

10.1021/jm00206a006

subject

Has Abstract

pub_date

1978-08-01 00:00:00

pages

746-53

issue

8

eissn

0022-2623

issn

1520-4804

journal_volume

21

pub_type

杂志文章

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