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"Toxoplasmosis is an ubiquitous anthropozoonosis induced by Toxoplasma gondii  Despite of several researchs  the whole stock of drugs remain restricted  The aim of the works in this report is the synthesis of carbazolequinones and valuation of efficacy against T  gondii  Natural carbazolequinones like Calothrixines exhibit antiparasitic et cytoxotoxic properties  The para- and ortho-quinones like benzo-  isoxazolo- and triazolo-carbazolequinones synthesis was investigate by regioselective  4 2  or 1 3-dipolar cycloaddition  The strategy of synthesis from monobromide dipolarophile can in fact have an access to required regioisomer with selectivity  Proofs of regiochemistry was made by NMR 1H NOE and study of correlation by 1H-13C HMBC  Concerning biological assessment  compounds inhibit the growth of T  gondii like sulfadiazine and pyrimethamine with cytotoxicity against myelomonocytic THP1 cells  Any synthesised compounds inhibit PNP  key enzyme of purine salvage pathway  unique way for the parasit to have access to puric basis  The inhibition of growth of T  gondii by our compounds isn t due to inhibition of PNP   La toxoplasmose est une anthropozoonose ubiquitaire caus  e par Toxoplasma gondii  Malgr   de nombreuses recherches  l arsenal th  rapeutique reste tr  s restreint  L objectif des travaux pr  sent  s dans ce m  moire est la synth  se de carbazolequinones et l   valuation de leur efficacit   sur T  gondii  Les carbazolequinones naturelles comme les calothrixines ont des propri  t  s antiparasitaires et cytotoxiques  La synth  se de para- et ortho-quinones de type benzo-  isoxazolo- et triazolo-carbazolequinones a   t   r  alis  e par application des r  actions de cycloaddition  4 2  ou 1 3-dipolaires r  gios  lectives  La strat  gie de synth  se    partir de dipolarophiles monobrom  s permet en effet  d acc  der s  lectivement au r  gioisom  re souhait    Les attributions de structure des r  giosiom  res ont   t   confirm  es par RMN 1H NOE et par une   tude des corr  lations 1H -13C HMBC  Concernant l   valuation biologique in vitro  les compos  s inhibent la croissance de T  gondii comme la sulfadiazine et la pyrim  thamine  avec une cytotoxicit   sur les cellules my  lomonocytiques THP1  Aucun des compos  s synth  tis  s n inhibent la PNP  enzyme cl   de la voie de sauvetage des purines  seule voie d acc  s pour le parasite aux bases puriques  L inhibition de la croissance de T  gondii par nos compos  s n est pas li  e directement li  e    l inhibition de la PNP   LYON1-BU Sciences  692662101    Sudoc   Sudoc   France   FR"
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