Antimalarials. Synthesis and antimalarial activity of 1-(4-methoxycinnamoyl)-4-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine and derivatives.

@article{Herrin1975AntimalarialsSA,
  title={Antimalarials. Synthesis and antimalarial activity of 1-(4-methoxycinnamoyl)-4-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine and derivatives.},
  author={Thomas Raymond Herrin and J. M. Pauvlik and Evelyn V. Schuber and Adolph O. Geiszler},
  journal={Journal of medicinal chemistry},
  year={1975},
  volume={18 12},
  pages={
          1216-23
        }
}
The preparation and activity against Plasmodium berghei of derivatives of 1-(4-methoxycinnamoyl)-4-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine are described. Replacement of the cinnamoyl group was accomplished by acylation or alkylation of 1-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine. Modifications of the 5-phenyl group were prepared either by a sequence of reactions involving mandelic ester-pemoline-piperazine pemoline or by the reaction of 5-aryl-2-thio-2,4-oxazolidinedione with piperazine or… 
18 Citations
Synthesis of Some Bioactive Sulfonamide and Amide Derivatives ofPiperazine Incorporating Imidazo[1,2-B]Pyridazine Moiety
TLDR
Some new sulfonamide and amide derivatives containing piperazine ring and imidazo[1,2-b]pyridazine moiety have been synthesized by the reaction of 6-chloro-2-substituted aryl(or alkyl)imidazo-1-b pyridazines derivatives and screened for in vitro antimicrobial activity against two gram positive and two gram negative bacteria.
Approach to 2′-(Dialkylamino)-1-alkyl-4′H-spiro[indoline-3,5′- oxazole]-2,4′-diones and 1,3-Oxazin-4-ones via Cyclization of Vilsmeier Salts with α-Hydroxy and β-Carbonyl Amides
A straightforward and efficient synthetic method of 2′-(dialkylamino)-1-alkyl-4′H-spiro[indoline-3,5′- oxazole]-2,4′-diones and 2-(dialkylamino)-5,6-dihydro-4H-naphtho[2,1-e][1,3]oxazin-4-one
Approach to 2′-(Dialkylamino)-1-alkyl-4′H-spiro[indoline-3,5′- oxazole]-2,4′-diones and 1,3-Oxazin-4-ones via Cyclization of Vilsmeier Salts with α-Hydroxy and β-Carbonyl Amides
A straightforward and efficient synthetic method of 2′-(dialkylamino)-1-alkyl-4′H-spiro[indoline-3,5′- oxazole]-2,4′-diones and 2-(dialkylamino)-5,6-dihydro-4H-naphtho[2,1-e][1,3]oxazin-4-one
Synthesis of tetradeuterated buspirone
Two methods have been developed for the synthesis of tetradeuterated buspirone. Synthesis of the title compound was accomplished by the reaction of 1-(2-pyrimidinyl)piperazine-3,3,5,5-d4 or
Condensation of Vilsmeier Salts, Derived from Tetraalkylureas, with α-Hydroxy Amide Derivatives: One-pot Approach to Synthesize 2-Dialkylamino-2-oxazolin-4-ones
A novel and straightforward synthetic protocol was developed to synthesize 2-dialkylamino-2-oxazolin-4-ones from various Vilsmeier salts and α-hydroxy amides derivatives. Notably, thozalinone (3a),
Oxazolines: Their Synthesis and Biological Activity
Heterocylic chemistry have been known for many years but in recent years heteocyclics received great attention. In heterocyclic chemistry oxazoline is one of the most important moiety. Oxazoline
Synthesis and evaluation of cytotoxic activities of artemisinin derivatives
TLDR
Findings indicate that 5d activates the mitochondria‐mediated apoptotic pathway in HepG2 cells and may merit further investigation as a potential therapeutic agent for hepatocellular carcinoma.
A rearrangement of 3-hydroxyazetidines into 2-oxazolines.
TLDR
A novel rearrangement sequence of 3-hydroxyazetidines via a Ritter initiated cascade provides highly substituted 2-oxazolines in high yields and is shown to be a transformation amenable to continuous flow processing.
...
1
2
...