Antimalarials. 4. Trichloronaphthalene amino alcohols.
An improved procedure for the synthesis of naphthalene amino alcohols is described. Four new compounds were prepared and tested by Rane Laboratories for activity vs. Plasmodium berghei in mice. All compounds were active, the most active being 1-[3-(4-chlorophenyl)-5,7-dichloro-1-naphthyl]-3-(di-n-butylamino)propanol hydrochloride (16b). Structure--activity relationships between the naphthalene and quinoline isosteres are discussed.
D000605:Amino Alcohols / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D010962:Plasmodium berghei; D013329:Structure-Activity Relationship
D000605:Amino Alcohols; D000962:Antimalarials; D009281:Naphthalenes