ANTIFOLATE SCREEN FOR DRUGS--INFECTION/AIDS

Project: Research project

Description

The objective of this project is to identify folate analogs and
analogs of p-aminobenzoic acid (PABA) with greater therapeutic
potential for the treatment of opportunistic infections in patients
with AIDS than the current clinically used agents. To accomplish
this objective folate analogs will be screened for inhibitory
activity against dihydrofolate reductase (DHFR) isolated form two
protozoans (Pneumocystis carinii and Toxoplasma gondii) and from
mammalian rat liver. Also, analogs of PABA will be tested for
inhibition of dihydropteroate synthetase (DHPS) isolated from the
two protozoans. Uptake into intact cells of selected potent
inhibitors of the DHFRs, differential inhibitors of the protozoal
DHFR and potent inhibitors of DHPS will be evaluated. Protection
of intact cells from selected potent, non-differential, inhibitors
of DHFR also may be evaluated.
StatusFinished
Effective start/end date8/15/888/14/93

Funding

  • National Institutes of Health

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Dihydropteroate Synthase
4-Aminobenzoic Acid
Folic Acid Antagonists
Anti-HIV Agents
Tetrahydrofolate Dehydrogenase
Folic Acid
Pneumocystis carinii
Opportunistic Infections
Toxoplasma
Infection
Acquired Immunodeficiency Syndrome
Liver

ASJC

  • Medicine(all)