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Bolstad DB, Bolstad ES, Wright DL, et al. Dihydrofolate reductase inhibitors: developments in antiparasitic chemotherapy. Expert Opin Ther Pat. 2008;18(2):143-57doi: 10.1517/13543776.18.2.143.
Bolstad, D. B., Bolstad, E. S., Wright, D. L., & Anderson, A. C. (2008). Dihydrofolate reductase inhibitors: developments in antiparasitic chemotherapy. Expert opinion on therapeutic patents, 18(2), 143-57. https://doi.org/10.1517/13543776.18.2.143
Bolstad, David B, et al. "Dihydrofolate reductase inhibitors: developments in antiparasitic chemotherapy." Expert opinion on therapeutic patents vol. 18,2 (2008): 143-57. doi: https://doi.org/10.1517/13543776.18.2.143
Bolstad DB, Bolstad ES, Wright DL, Anderson AC. Dihydrofolate reductase inhibitors: developments in antiparasitic chemotherapy. Expert Opin Ther Pat. 2008 Feb;18(2):143-57. doi: 10.1517/13543776.18.2.143. PMID: 20553119.
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Expert Opin Ther Pat. 2008 Feb;18(2):143-57. doi: 10.1517/13543776.18.2.143.

Dihydrofolate reductase inhibitors: developments in antiparasitic chemotherapy.

Expert opinion on therapeutic patents

David B Bolstad, Erin Sd Bolstad, Dennis L Wright, Amy C Anderson

Affiliations

  1. University of Connecticut, Department of Pharmaceutical Sciences, 69 N Eagleville Road, Storrs, CT 06269, USA +1 860 486 6145 ; +1 860 486 6857 ; [email protected].

PMID: 20553119 DOI: 10.1517/13543776.18.2.143

Abstract

BACKGROUND: Infections caused by parasitic protozoa present a growing health concern, particularly in developing parts of the world. Although malaria is clearly the most well-known and deadly of these diseases, infections caused by other parasites, such as Toxoplasma, Cryptosporidia and Trypanosoma are emerging infectious threats. The success of inhibitors of the enzyme dihydrofolate reductase (DHFR) against malaria has encouraged further exploration of this strategy against other parasites.

OBJECTIVE: This review presents antifolate inhibitors that have appeared in the patent literature and elaborates on their potency and selectivity against the DHFR enzyme from parasitic protozoa.

METHODS: The patent literature since 1994 was surveyed for antiparasitic DHFR inhibitors.

RESULTS/CONCLUSIONS: Over the past several years, there have been a variety of novel, potent and selective inhibitors disclosed in patents, primarily from academic researchers. This review summarizes the recent development of antifolates as specific agents against parasitic protozoa.

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