New functionalized 1,2,4-trioxepanes: synthesis and antimalarial activity against multi-drug resistant P. yoelii in mice.
A series of new amino functionalized 1,2,4-trioxepanes 8-16 and ester functionalized 1,2,4-trioxepanes 17-19 have been synthesized and evaluated against multi-drug resistant Plasmodium yoelii in Swiss mice. Amino functionalized trioxepanes 14, the most active compound of the series, showed 100% clearance of parasitaemia by oral route on day 4 and 75% protection to the treated mice beyond day 28.
Singh
Chandan
C
Division of Medicinal & Process Chemistry, Central Drug Research Institute, Lucknow 226001, India. chandancdri@yahoo.com
Pandey
Shilpi
S
Kushwaha
Ambuj K
AK
Puri
Sunil K
SK
D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D018432:Drug Resistance, Multiple; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D018512:Parasitemia / Q000097:blood / Q000188:drug therapy; D010967:Plasmodium yoelii / Q000187:drug effects*; D020005:Propanols / Q000737:chemistry; D013329:Structure-Activity Relationship
C503429:1,2,4-trioxane; D000962:Antimalarials; D037621:Artemisinins; D006571:Heterocyclic Compounds; D020005:Propanols; C006463:allyl alcohol; C031327:artemisinin