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Ph.D.
                                                                                     (Pharmacy)
          STUDIES IN VARIOUS FORMULATION APPROACHES FOR
          DISSOLUTION ENHANCEMENT OF POSACONAZOLE

          Ph.D. Scholar : Gurjar Riteshkumar Baldevbhai
          Research Supervisor : Dr. Rakesh P. Patel



                                                                                Regi. No.: 18276011003
          Abstract :
          Discovering  new  drugs  with  novel  targets  is  vital  for  the  success  of  treatment  of
          tuberculosis  as  antibiotic  resistance  is  increasing  among  the  TB  population.
          Mycobacterium tuberculosis cytochrome P450 CYP121A1 is a promising drug target for
          the treatment of tuberculosis owing to its essential role in mycobacterium growth. Using
          a  rational  approach,  that  includes  molecular  docking  studies  of  some  substituted
          pyrazole  derivatives  a  series  of  pyrazole  analogue  were  designed  and  pass  through
          computational  studies.  Compound  with  good  docking  score  and  ADME  profile  were
          synthesized using two step reaction and biologically evaluated for their inhibitory activity
          towards M. tuberculosis. All compounds were analyzed by IR, LCMS, 1H-NMR and 13C-
          NMR.  Among  them  5  compounds  shows  significant  activity  having  MIC  (3.12  to
          6.25µg/ml). Synthesized compound were re-docked with MmpL3 protein to identify dual
          inhibitory  approach.  All  synthesized  compounds  gives  good  docking  score  and  shows
          dual inhibition acts on cellular metabolism and cell wall synthesis.
          Key  words:  Mycobacterium  tuberculosis,  Pyrazole,  CYP121A1,  Molecular  docking,
          MmpL3





























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