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

Kuyper, LF; Garvey, JM; Baccanari, DP; Champness, JN; Stammers, DK; Beddell, CR

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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APA Style

Kuyper, L. F., Garvey, J. M., Baccanari, D. P., Champness, J. N., Stammers, D. K., & Beddell, C. R. (1996). Pyrrolo[2,3-d]pyrimidines and pyrido[2,3-d]pyrimidines as conformationally restricted analogues of the antibacterial agent trimethoprim. Bioorganic and Medicinal Chemistry, 4(4), 593–602.

MLA Style

Kuyper, L. F., et al. “Pyrrolo[2,3-d]Pyrimidines and Pyrido[2,3-d]Pyrimidines as Conformationally Restricted Analogues of the Antibacterial Agent Trimethoprim.” Bioorganic and Medicinal Chemistry, vol. 4, no. 4, Bioorganic and medicinal chemistry, 1996, pp. 593–602.

Chicago Style

Kuyper, LF, JM Garvey, DP Baccanari, JN Champness, DK Stammers, and CR Beddell. 1996. “Pyrrolo[2,3-d]Pyrimidines and Pyrido[2,3-d]Pyrimidines as Conformationally Restricted Analogues of the Antibacterial Agent Trimethoprim.” Bioorganic and Medicinal Chemistry 4 (4): 593–602.
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