Synthesis of 5-chloro-3'-nitro-4'-substituted salicylanilides, a new series of anthelmintic and antimicrobial agents.
A number of 5-chloro-3'-nitro-4'-substituted salicylanilides (6--23) have been synthesized by treating 4',5-dichloro-3'-nitrosalicylanilide (5) with various sodium aryl oxides, alkoxides, or amines. These compounds have been tested against Hymenolepis nana infection in rats and have also been evaluated for their in vitro antimicrobial activity against various strains of bacteria and fungi. In the former test 17 was the most active cestodicidal agent showing activity at 30 mg/kg. In the antimicrobial screening, 22 inhibited the growth of all the bacteria and fungi used while 6 was active against the penicillin resistant Staphylococcus aureus at a minimum inhibitory concentration of 0.00609 microgram/mL.
D000818:Animals; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis*; D000923:Anticestodal Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects; D005658:Fungi / Q000187:drug effects; D006925:Hymenolepiasis / Q000188:drug therapy; D008826:Microbial Sensitivity Tests; D051381:Rats; D012457:Salicylamides / Q000138:chemical synthesis*; D012458:Salicylanilides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000923:Anticestodal Agents; D012457:Salicylamides; D012458:Salicylanilides