ChemInform Abstract: 2‐Acetylpyridine Thiosemicarbazones. Part 12. Derivatives of 3‐Acetylisoquinoline as Potential Antimalarial Agents.

Abstract

Das 3‐Acetylisochinolin (I) kondensiert mit dem Dithiocarbazidsäuremethylester (II) zum Hydrazon (III), das sich mit NaBH4 zum Hydrazinodithiocarbonsäureester (IV) hydrieren läßt. Die sekundären Amine (VI) liefern mit (III) die Thiosemicarbazone (V); mit (IV) entstehen die Thiosemicarbazide (VII).

Antimalarial Activities of Polyhydroxyphenyl and Hydroxamic Acid Derivatives

“…Not only does this identify benzohydroxamate as a potential antimalarial, but in addition and perhaps more importantly, it provides evidence of a difference between P. falciparum and human RNRs. This evidence supports that of Klayman et al (9,10), who cured Plasmodium berghei malaria in mice with RNR inhibitors, suggesting a possible difference between the P. berghei and mouse forms of reductase. Unlike the P. berghei data, the P. falciparum result presented here could not be explained by a difference in drug permeability, since benzohydroxamate was more effective in inhibiting the P. falciparum reductase enclosed within the parasite than the human enzyme, which was free in solution.…”

Synthesis, Structure−Activity Relationships, and Antitumor Studies of 2-Benzoxazolyl Hydrazones Derived from Alpha-(N)-acyl Heteroaromatics

“…The following ketones utilized as starting materials were obtained according to the literature cited: methyl 3-pyridazinyl ketone ( 12a ), methyl 3-(6-methylpyridazinyl) ketone ( 12b ), methyl 2-pyrimidinyl ketone ( 12c ), methyl 4-pyrimidinyl ketone ( 12d ), methyl 4-(6-methylpyrimidinyl) ketone ( 12e ), methyl 2-(5-methylpyrazinyl) ketone ( 12h ), 2-acetylquinoline ( 12i ), 1-acetylisoquinoline ( 12j ), and 3-acetylisoquinoline ( 12k ) . Methyl 2-pyrazinyl ketone ( 12f ) and methyl 2-(3-methylpyrazinyl) ketone ( 12g ) were purchased from Maybridge Co. 2-Benzoylpyridine ( 10g ) and di-(pyridin-2-yl)-methanone ( 10h ) were purchased from Sigma-Aldrich Co.…”

Novel 1-acyl-4-substituted semicarbazide derivatives of primaquine − synthesis, cytostatic, antiviral and antioxidative studies

“…Hydroxyurea is a useful drug in therapy of leukaemia and other malignant tumour diseases and its derivative zileuton is an orally active inhibitor of 5-lipoxygenase which is used for the maintenance treatment of asthma 12 . Hydroxyurea is an inhibitor of ribonucleotide reductase, the enzyme described as a target for the chemotherapy of both malignant diseases and malaria 13,14 . Mahajan et aldescribed 7-chloroquinolyl thioureas as potential antimalarial and anticancer agents 15 .…”