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Pyrrolo[2,3-d]pyrimidines and pyrido[2,3-d]pyrimidines as conformationally restricted analogues of the antibacterial agent trimethoprim.

Abstract:

Conformationally restricted analogues of the antibacterial agent trimethoprim (TMP) were designed to mimic the conformation of drug observed in its complex with bacterial dihydrofolate reductase (DHFR). This conformation of TMP was achieved by linking the 4-amino function to the methylene group by one- and two-carbon bridges. A pyrrolo[2,3-d]pyrimidine, a dihydro analogue, and a tetrahydropyrido[2,3-d]pyrimidine were synthesized and tested as inhibitors of DHFR. One analogue showed activity e...

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Publication status:
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Authors


Kuyper, LF More by this author
Garvey, JM More by this author
Baccanari, DP More by this author
Champness, JN More by this author
More by this author
Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Structural Biology
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Journal:
Bioorganic and medicinal chemistry
Volume:
4
Issue:
4
Pages:
593-602
Publication date:
1996-04-05
DOI:
EISSN:
1464-3391
ISSN:
0968-0896
URN:
uuid:d3b2050e-70c1-4f03-8cd4-50611776f0af
Source identifiers:
72680
Local pid:
pubs:72680

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