THE SYNTHESIS OF NEW ANTIMALARIAL DRUGS. ANALOGS OF PANTOTHENIC ACID
Annual rept. no. 3 (Final), 1 Mar 1968-31 Mar 1969
LITTLE (ARTHUR D) INC CAMBRIDGE MA
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The present synthetic program on antagonists of pantothenic acid was based on the demonstrated antimalarial activity of chlorophenylpantoylsulfone SN 14622, WR 29,224 in avian malaria from World War II program. During the three years of our work we have prepared and submitted for evaluation one hundred and eight compounds. Unfortunately, SN 14622 is completely inactive in the present WRAIR screens in mice, chicks and mosquitoes. It appears that the nonproductibility of the activity of SN 14622 in the present chick screen is due to the different test procedure being used. A few of our compounds were tested in Dr. Tragers in vitro screen and of these WR 54036 has been selected for advanced screening in the monkey. Three other compounds, WR 61467, AE 96096 and AF 14571 derivatives of sulfonamides have been found to be active in the Rane screen in mice at 160, 40, and 160 mgkg respectively.
- Organic Chemistry