Accession Number : AD0704710

Title :   THE SYNTHESIS OF NEW ANTIMALARIAL DRUGS DERIVATIVES OF BENZOTHIOPYRANS.

Descriptive Note : Annual rept. no. 1, 1 Jan-31 Dec 69,

Corporate Author : LITTLE (ARTHUR D) INC CAMBRIDGE MASS

Personal Author(s) : Razdan,Raj K. ; Bruni,Robert J. ; Mehta,Avinash C.

Report Date : MAR 1970

Pagination or Media Count : 52

Abstract : The present synthetic program on benzothiopyran derivatives is based on a lead compound WR 95214. Of the compounds tested so far, fourteen compounds are active in the mice screen and five of which have produced cures at a dose level of 640 mg/kg. At present the most potent compound seems to be AT 89470 (N-N-diethyl-N'-(6-chloro-2-phenyl-4H-1-benzothiopyran-4-ylidene-1-4-pentanediamine dihydrochloride) (160 mg/kg - 14 day) but the data is not yet complete. To date only seven target compounds have been tested in the chick screen out of which five are active. Two compounds are curative in mice as well as active in the chick screen. (Author)

Descriptors :   (*ANTIMALARIALS, SYNTHESIS(CHEMISTRY)), (*SULFUR HETEROCYCLIC COMPOUNDS, ANTIMALARIALS), IMINES, CHLORINE COMPOUNDS, HALOGENATED HYDROCARBONS, BIOASSAY

Subject Categories : Pharmacology
      Organic Chemistry

Distribution Statement : APPROVED FOR PUBLIC RELEASE