Synthesis and biological activity of 10-thia-10-deaza analogs of folic acid, pteroic acid, and related compounds
- 1 August 1975
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 18 (8) , 776-780
- https://doi.org/10.1021/jm00242a002
Abstract
The 10-thia analogs of pteroic acid, folic acid, their esters, and their 4-amino analogs were synthesized through a reaction sequence involving, as a key step, the condensation of 2-amino-3-cyano-5-chloromethylpyrazine with appropriately substituted thiols. The abilities of the products to inhibit the growth of methotrexate (MTX)-sensitive and MTX-resistant microorganisms were investigated as were their abilities to inhibit dihydrofolic acid reductase and thymidylic acid synthetase. Several compounds had high activity.Keywords
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