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Synthesis and Antimalarial Activity of Pyrazolo and Pyrimido Benzothiazine Dioxide Derivatives by Arthur Barazarte; Gricela Lobo; Neira Gamboa; Juan R. Rodrigues; Mario V. Capparelli; Ángel Álvarez-Larena; Simón E. López; Jaime E. Charris is a Chemistry article available to read on EtoBox.
What is Synthesis and Antimalarial Activity of Pyrazolo and Pyrimido Benzothiazine Dioxide Derivatives about?
A series of phenylsubstituted pyrazolo and pyrimido benzothiazine dioxide derivatives were synthesized and investigated for their abilities to inhibit b-hematin formation, hemoglobin hydrolysis and in vivo for their antimalarial efficacy in rodent Plasmodium berghei. Compounds 3-amino-7-chloro-9-(2 0 -methylpheyl)-1,9-dihydro-pyrazolo-[4,3-b]benzothiazine 4,4-dioxide 2b and 2,4-diamino-8-chloro-10Hphenyl-pyrimido-[5,4-b]benzothiazine 5,5-dioxide 3a were the most promising as inhibitors of hemoglobin hydrolysis, however, their effect as inhibitors of b-hematin formation was marginal, except for compound 3-amino-7-chloro-9-(3 0 -chlorophenyl)-1,9dihydro-pyrazolo-[4,3-b]benzothiazine 4,4-dioxide 2g. The most active compound to emerge from the in vitro and in vivo murine studies was 2b, suggesting an antimalarial activity via inhibition of hemoglobin hydrolysis, however, not as efficient as chloroquine.
Who reads Synthesis and Antimalarial Activity of Pyrazolo and Pyrimido Benzothiazine Dioxide Derivatives?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Arthur Barazarte; Gricela Lobo; Neira Gamboa; Juan R. Rodrigues; Mario V. Capparelli; Ángel Álvarez-Larena; Simón E. López; Jaime E. Charris
- Publisher
- Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)
- Published
- 2009
- Language
- EN
- Field
- Chemistry (Physical Sciences)