title: Synthesis, antimalarial and antitubercular activity of acetylenic chalcones.
abstract: 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.
authors.affiliation: Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
authors.forename: Renate H
authors.initials: RH
authors.lastname: Hans
authors.forename: Eric M
authors.initials: EM
authors.lastname: Guantai
authors.forename: Carmen
authors.initials: C
authors.lastname: Lategan
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Smith
authors.forename: Baojie
authors.initials: B
authors.lastname: Wan
authors.forename: Scott G
authors.initials: SG
authors.lastname: Franzblau
authors.forename: Jiri
authors.initials: J
authors.lastname: Gut
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Rosenthal
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
mesh_terms: 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
chemical_list: D000480:Alkynes; D000962:Antimalarials; D000995:Antitubercular Agents; D047188:Chalcones