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									 REGISTRATION OF SUBJECT FOR DISSERTATION


A PROTOCOL FOR THE PROJECT WORK ENTITLED




“SYNTHESIS AND BIOLOGICAL ACTIVITY STUDIES OF
          SUBSTITUTED PYRAZOLINES”




                        By,
                   Lakshmi.T.N.
                 M.Pharm, Part- I
     Department of Pharmaceutical Chemistry
    N.G.S.M. Institute of Pharmaceutical Science
                Paneer, Deralakatte
                Mangalore – 574160




                         1
           RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES, BANGALORE
                                       KARNATAKA.


                                      ANNEXURE II


     PROFORMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION


1.   NAME OF THE LAKSHMI.T.N.
     CANDIDATE           N.G.S.M INSTITUTE OF PHARMACEUTICAL SCIENCES
     AND ADDRESS DERALAKATTE, MANGALORE – 574160.
2.   NAME OF THE N.G.S.M. INSTITUTE OF PHARMACEUTICAL SCIENCES,
     INSTITUTION         DERALAKATTE, MANGALORE – 574160.
3.   COURSE OF            M.PHARM
     STUDY AND           [PHARMACEUTICAL CHEMISTRY]
     SUBJECT
4.   DATE OF             JUNE 2007
     ADMISSION
5.   Title of the Topic :
     COURSE
         “SYNTHESIS AND BIOLOGICAL ACTIVITY STUDIES OF
     SUBSTITUTED PYRAZOLINES”
6.   Brief resume of the intended work :
      6.1 Need for the study:
             Various heterocyclic compounds posses wide range of biological and
     pharmacological activities. Among a wide variety of heterocycles that have been
     explored for developing pharmaceutically important molecules such as chalcones
     and pyrazolines have played an important role in the present medicinal chemistry.
                Literature survey reveals that the nitrogen containing heterocycles
     posses a wide range of activities. In the present work it has been observed that
     substituted chalcones are the best starting compound for the preparation of
     substituted pyrazolines.


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           Pyrazolines are the dehydrate form of pyrazoles and are well known
nitrogen containing heterocyclic compound. Various procedures have been
developed for their synthesis.
         Formation of pyrazolines has been reported by the action of nucleophiles
like hydrazine hydrate or phenyl hydrazine etc on chalcones in solvents like acetic
acid, pyridine, alcohol etc.
         Chalcones1 show impressive physiological properties and some of them
posses wide range of activities such as anti bacterial2, antitubercular3etc.
         Pyrazoline derivatives posses various activities like antibacterial 4,
antifungal4,    antitubercular4,    anti-inflammatory5,     herbicidal6,       anticancer7
antidepressant7and antioxidant8 etc.
          Prompted by the varied biological and pharmacological activities of
chalcones and pyrazolines, it was contemplated to synthesise pyrazolines starting
from 2-thiophene carboxaldehyde.




6.2 Review of Literature:

   1. Sangapure SS, et al9. (2001) Synthesized 1-acetyl and 1-benzoyl

      pyrazolines by the acetylation and benzoylation of 5-aryl-3-(5-chloro-3-

      methyl benzofuran -2-yl)-1H-pyrazolines which is prepared by the

      condensation of 5-chloro-3-methyl-2-acetyl benzofuran with aromatic

      aldehyde in presence of alkali gave 2-cinnamoyl-5-chloro-3-methyl

      benzofuran which then reacted with hydrazine hydrate.The invitro

      antibacterial activity of the final synthesized compound was evaluated.




                                          3
2. Shivarama Holla B, et al10. (2001) Synthesized some fluorine containing

   N-phenyl pyrazolines starting from aryl furyl propanones. Some of the

   selected 2-pyrazolines screened for their antibacterial activity.

3. Parekh HH, et al11. (2003) Synthesized a series of pyrazoline and isoxazole

   by the action of hydrazine hydrate and hydroxylamine hydrochloride

   respectively on 1-aryl-3-(2’-chloro-7’-methyl quinoline-3’-yl)-2-propen-1-

   ones and the later compounds are prepared by the condensation of 2-chloro-

   7-methyl-quinoline-carboxaldehyde with different aromatic ketones.All the

   compounds have been characterized on the basis of elemental analysis and

   spectral data.

4. Ashok Kumar, et al12. (2004) Synthesized chalcones and their

   corresponding product; pyrazolines and azo compounds.The most active

   compound of this series was 3-[1-acetyl-5-(p-hydroxy phenyl)-2-pyrazolin-

   3-yl] indole was found to be more potent.

5. Bhagat PR, et al13. (2004) Synthesized 1-(3-chloro phenyl)/carboxamido-3-
                                                           2
   {3-[(4-chloro phenyl)sulphonamido]phenyl}-5-aryl-           -pyrazolines by

   refluxing chalcones with 3-chloro phenyl hydrazine

   hydrochloride/semicarbazide hydrochloride in pyridine solvent. The

   structures of these compounds were established by elemental analysis and

   spectral analysis (IR, NMR).




                                      4
 6. Anjani Solankee, et al14. (2004) Synthesized pyrazolines, amino

     pyrimidines and pyrimidinethiones by cyclization of chalcones with

     hydrazine hydrate, guanidine nitrate and thiourea respectively. The

     synthesized compounds were screened for their antibacterial activity.

 7. Pande PS, et al15. (2005) Synthesized a series of N-aroyl-3,5-diaryl

     pyrazolines and N-aroyl-3,5-diaryl pyrazoles by the action of acid

     hydrazides and on 1,3-diaryl-prop-2-ene-1-ones and substituted diaryl

     propane-1,3-dione respectively.

 8. Havaldar H Freddy, et al16. (2007) Synthesized 2-(3-carboxy phenyl)-5-(4-

     substituted phenyl)-1-acetyl-2-pyrazolines by cyclization of chalcones with

     hydrazine hydrate in glacial acetic acid. Substituted chalcones were obtained

     by condensation of 3-carboxy acetophenone with various aromatic aldehydes

     in hydrotopes. The final compounds were screened for antibacterial and

     antifungal activity.The constitution of the compound was supported by IR,

     NMR and MASS Spectra.

6.3 Objectives of the study:
      The present studies were performed with the following objectives.
  1. Synthesis of chalcones from 2-thiophene carboxaldehyde with substituted
     acetophenones.
  2. Synthesis of substituted 2-pyrazolines.
  3. Screening for the antibacterial activity by using gram positive and gram
     negative bacteria.
  4. Screening for the antifungal activity by using A.niger and C.albicans.




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Materials and methods:
7.1 Sources of data.
        Journals and publications.
        CD ROM and internet.
        Laboratory based studies.


7.2 Methods of collection of data.
          From available literature.
          From library based books.
          Websites.
              -www.pubmed.com
              -www.google.com
              -www.sciencedirect.com


7.3 Does the study require any investigations or interventions to be
conducted on patients or other humans or animals?
  If so please describe briefly
                         No.
7.4 Has ethical clearance been obtained your institution in case of 7.3?
                       Not applicable



LIST OF REFERENCE.



    1. Chem. Abs. 1994; 120 : 208071

    2. Chem. Abs. 1973; 78 : 119650n

    3. Chem. Abs. 1987; 106 : 32503a




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4. Chetan BP, Sreenivas MT, Bhat AR. Synthesis and evaluation of certain

   pyrazolines and related compounds for their antitubercular, antibacterial

   and antifungal activities. Ind J Het Chem 2004 Jan.-March; 13 : 225-8.

5. Harinadha VB, Manna SK, Sneha, Srinivasan KK, Varadaraj Bhat G.

   Synthesis and biological evaluation of 1,3,5-trisubstituted pyrazolines

   bearing benzofuran. Ind J Het Chem 2004 Jan.-March; 13 : 253-6.

6. Verma BL, Mamta S. Synthesis, antibacterial and herbicidal activities of

   some new 3-[4’-(4’’-nitrophenoxy)-phenyl]-5-substituted phenyl-2-

   pyrazolines and 2-isoxazolines. Ind J Het Chem 2005

   April-June; 14 : 343-6.

7. Joshi HS, Popat KH, Nimavat KS. Synthesis, anticancer , antitubercular and

   antimicrobial activity of 1-substituted 3-aryl-5-(3’-bromo phenyl)-

   pyrazolines. Ind J Het Chem 2003 Jan.-March; 12 : 225-8.

8. Nagarajan G, Suthakaran R, Somasekhar G, Marikannan M. Synthesis, anti-

   inflammatory, antioxidant and antibacterial activities of 7-methoxy

   benzofuran pyrazoline derivatives. Asian J Chem 2007 May; 19 : 3353-62.

9. Sangapure SS, Raga B , Bodke Y. Synthesis of some 1H-pyrazolines

   bearing benzofuran as biologically active agents.

   Ind J Het Chem 2001 July-Sept; 11 : 31-4

10. Shivarama Holla B, Shivananda MK, Akberali PM. Synthesis of some

   fluorine containing aryl furyl-N-phenyl pyrazolines and their antibacterial

   activity studies. Ind J Het Chem 2001 April-June; 10 : 305-6.



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11. Parekh HH, Patel JR, Dobaria AV. Synthesis of pyrazolines and isoxazole

    derivatives bearing chloro quinoline nucleus as potential antimicrobial

    agents. Ind J Chem 2003 August; 42B : 2019-22.

12.Ashok Kumar, Srivastava VK, Preeti Rani. Synthesis and antiinflammatory

   activity of heterocyclic indole derivatives. Eur J Med Chem 2004; 39 :

   449-52.

13.Bhagat PR, Jamode VS, Chandak HS. Synthesis and antimicrobial activity of
                                                            2
   3-{3-[(4-chlorophenyl)-sulphonamido]phenyl}-5-aryl-          - pyrazolines. Asian J

   Chem 2004 March-April; 16 : 1837-41.

14.Anjani Solankee, Patel J. Synthesis of chalcones, pyrazolines,amino

   pyrimidines and pyrimidine thiones as antibacterial agent.

   Ind J Chem 2004 July; 43B : 1580-84.

15.Pande PS, Wadodkar KN, Wadhal SA. Synthesis of N-aroyl pyrazolines

   and pyrazoles. Ind J Het Chem 2005 July-Sept; 15 : 11-4.

16.Havaldar H Freddy, Navinchandra K Khatri. Synthesis and biological

   activity of 2-(3-carboxy phenyl)-5-(4-substitudted phenyl)-1-acetyl-2-

   pyrazolines. Asian J Chem 2007; 19 : 5093-97.




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                                     SCHEME




                                      +        R-CO-CH3
                               CHO
              S
     2-thiophene carboxaldehyde.                Substituted acetophenone


                                                          O

                                     CH        CH         C     R
                           S
                                      Chalcones




NH2-NH2 /                                                             NH2- NH2 /
C2H5OH                                                               CH3COOH

                       R                                                       R
                                                                                   O

                    N H                                                    N       C   CH3
     S          N                                          S         N




TITLE OF THE TOPIC.
“SYNTHESIS AND BIOLOGICAL ACTIVITY STUDIES OF
SUBSTITUTED PYRAZOLINES”




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