Folate antagonists.  17 . Synthesis and biological properties of a 2,4‐diamino‐6‐thioquinazoline analog of aminopterin | Zendy

Werbel Leslie M. | Zendy; Newton Linda | Zendy; Elslager Edward F. | Zendy

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Folate antagonists. 17 . Synthesis and biological properties of a 2,4‐diamino‐6‐thioquinazoline analog of aminopterin

Author(s) -

Werbel Leslie M.,

Newton Linda,

Elslager Edward F.

Publication year - 1980

Publication title -

journal of heterocyclic chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.321

H-Index - 59

eISSN - 1943-5193

pISSN - 0022-152X

DOI - 10.1002/jhet.5570170315

Subject(s) - aminopterin , chemistry , plasmodium berghei , dihydrofolate reductase , folic acid , folic acid antagonists , biochemistry , pharmacology , stereochemistry , methotrexate , enzyme , immunology , malaria , medicine , biology

A multistep route for the synthesis of N ‐[4‐[(2,4‐diamino‐6‐quinazolinyl)thio]benzoyl]‐L‐glutamic acid (2) from 4‐mercaptobenzoic acid and 5‐chloro‐2‐nitrobenzonitrile is described. Although this aminopterin analog lacked significant antimalarial activity, it was a potent inhibitor of dihydrofolate reductase from Trypanosoma cruzi. The pteroic ester analog 11 , however, was active against Plasmodium berghei infections in mice at high doses.

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