Synthesis, antimalarial and antitubercular activity of acetylenic chalcones.
A series of acetylenic chalcones were evaluated for antimalarial and antitubercular activity. The antimalarial data for this series suggests that growth inhibition of the W2 strain of Plasmodium falciparum can be imparted by the introduction of a methoxy group ortho to the acetylenic group. Most compounds were more active against non-replicating than replicating cultures of Mycobacterium tuberculosis H(37)Rv, an unusual pattern with respect to existing anti-TB agents.
Hans
Renate H
RH
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
Guantai
Eric M
EM
Lategan
Carmen
C
Smith
Peter J
PJ
Wan
Baojie
B
Franzblau
Scott G
SG
Gut
Jiri
J
Rosenthal
Philip J
PJ
Chibale
Kelly
K
D000480:Alkynes / Q000138:chemical synthesis* / Q000494:pharmacology; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D047188:Chalcones / Q000138:chemical synthesis* / Q000494:pharmacology; D009169:Mycobacterium tuberculosis / Q000187:drug effects / Q000502:physiology; D010963:Plasmodium falciparum / Q000187:drug effects / Q000502:physiology
D000480:Alkynes; D000962:Antimalarials; D000995:Antitubercular Agents; D047188:Chalcones