RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES, by gM9zk03g

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									     RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,
               BANGALORE, KARNATAKA.


                             ANNEXURE- II


     PROFORMA FOR REGISTRATION OF SUBJECT FOR
                  DISSERTATION



                                     KIRAN KUMAR.M.
1.     Name of the Candidate and
                                     Dept of pharmaceutical chemistry,
       Address:
                                     Govt. College of pharmacy,
                                     # 2, P. Kalinga Rao Road ,
                                     Subbaiah Circle,
                                     Bangalore – 560 027



2.     Name of the Institute:            Government College of Pharmacy.



3.     Course of Study and             Master of Pharmacy in Pharmaceutical

       Subject:                                     Chemistry


4.     Date of admission to course                 31st May2007


5.     Title of the Topic:

       “SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL
           EVALUATION OF TRIAZOLE DERIVATIVES”.
6.   Brief Resume of Intended Work:

     6.1: Need for the Study:

         Since time immemorial, disease has played an important impact in human

     life. Indeed the impact of disease can be far greater than better-known

     calamities.

     The course of a disease -that is, the path it follows from onset to end can vary

     tremendously from individual to individual depending on organism.

     The ability of mankind to prepare medicinally important molecules during the

     past centuary has allowed a continued decrease in the mortality rate from

     numerous diseases however, many disease and infection continues to prosper

     in mankind and escape suitable and long -lasting treatments or cure.

     Modern drug discovery focuses on synthesizing promising and potent drug.

     A key challenge in the synthesis of such targets continues to be the

     development of new pathways and improvement of existing pathways and

     improvement of existing pathways to biologically important and promising

     potent molecules

     There are two basic approaches to develop new drugs.

           Synthesis of analogues, modification or derivatisation of existing

            compounds for shortening and improving the treatment

           Searching novel structure with diverse activities against multi-resistant

            organisms

     Special importance was paid to Triazole derivatives that have attention as
potential moiety with diverse biological activity.

The triazoles refers to heterocyclic 5-membered ring system containing two

carbon atoms and three Nitrogen atoms with molecular formula C2H3N3.

    1,2,4-triazoles,1,3,4-triazoles and N-bridged heterocyclic derived from

them are found to be associated with diverse pharmacological activity such as

analgesic,antiinflamatory,antibacterial,antifungal,antitubercular,anticonvulsant

action.



3-amino-1,2,4-triazole(Amitrol,Amizol,ATA,Citra,ENT25445,weedazole)was

the first 1,2,4-triazole to be manufactured on the large scale from amino

guanidine for use as a herbicide & defoliant of cotton.

The aim of the current study is to synthesize triazole derivatives and to screen

the synthesized derivatives for their biological activities.

6.2: Review of literature



         Kallury KMRR, Surendranath TG and Srinivasan VR1., studied the

          mass spectra of 3-Chloro-4,5-diphenyl-4H-1,2,4-Triazole , 3-amino-

          4,5-diphenyl-4H-1,2,4-Triazole and3-Chloro-5-(5-chloro-2-thienyl)-4-

          phenyl-4H-1,2,4 triazoles revealed a novel skeletal rearrangement

          involving the migration of 3-substituent to the C 5 of carbon of the

          triazole ring followed by a concerted loss of nitrogen and benzonitrile.



         Zamani K, Faghihi K. Sangi MR and Zolgharnin J2., synthesized 3,5-
    Disubstituted-1,2,4-triazole from 1-(4-methyl phenyl)-4-(isomeric

    pyridoyl) thionemicarbazide.

   XU ,Liang-Zhong, Jian, Fang-Fang Shi, Jian-Gang Sun, Ping-ping,

    Jiao     kui3.,    synthesized    2,2-Dimethyl-4-S       (N,N-dimethyl

    dithiocarbamate)-5-(1,2,4-triazol-1-yl)-propione and 2,2-Dimethyl-4-

    S(N,N-diethyldithiocarbamate)-5-(1,2,4-triazol-1-yl)-3-propane     from

    2,2-dimethyl-4-bromo-5-(1,2,4-triazol-1-yl)propione and tested for

    their biological activity.The results of the biological test showed that

    the two compounds have fungistasis and plant growth regulating

    activities.

   Liang- Zhongx, Shu-Shen zhang, Shu-yanNiu, Yong-Qi Qin, Xue-Mei

    li and Kuijiao4., synthesis thirteen new triazoles containing 1, 3-

    dioxolane were synthesized and evaluated for fungicidal and plant

    growth regulant activities all of these compounds possess some

    fungicidal and plant growth regulant activities.

   Bekircan O, Kahveci B, Kucuk M5., synthesized un- symmetrical 3,5-

    Diaryl-4H-1,2,4-Triazole derivative from the treatment of 4-Amino-

    4H-1,2,4-Triazoles with certain aldehyde and tested for anticancer

    activities on 3 human tumour cell lines (breast cancer, non-small cell

    lung cancer and CNS cancer) and some 4-derivative showed anti-

    tumour activity.

   Khalil    N   S.A.M6   .,synthesized   6-aryl-2H-(1,2,4)triazolo   (3,4-

    b)(1,3,4)thiadiazole-3-thiones from 4-amino-4H-(1,2,4)triazole-3,5-
    dithiol by its cyclization with the appropriate carboxylic acid or acid

    chloride in refluxing phosphoryl chloride. Arabinosidation of parent

    compound with 2,3,4-tri-O-acetyl -β-L-arabinopyrosyl bromide yield

    the   N-   and    S-   -L-arabinopyranosyl(1,2,4)     trizolo   (3,4-b)

    (1,3,4)thiadiazoles and made anti-microbial screening of two selected

    regioisomeric compounds against aspergillus fumigatus, pencillium

    italium, syncephalastrum race mosum, candida albicans, s. aureus,

    pseudomonas aeruginosa B. subtilis and E.coli are compared.

   Yun Ding, Yun Yan Zhang, Jiong zhang, Yao-quan chen7 .,reported

    synthesis of two types of ribonucleoside anologueswith thiosubstituted

    five-membered heterocyclic base and tested for biological activity.

   Udupi RH and Bhatt AR8 ., carried out the synthesis of 4-(n-pyridyl

    carboxamido)-5-mercapto-3-substituted-1,2,4-triaxzoles and scrrened

    for their anti-tubercular activity. All the compounds were active

    against Mycobacterium tuberculosis at 100µg but not as much as

    standard Streptomycin, which was active even at 10µg, thereby

    suggesting a scope for further modification in the molecule.
6.3 Main objective of the study :

The present work is an attempt to

      Synthesize new Triazole derivatives of pharmacological interest

      Characterization of synthesized compounds

      Screening of derivatives for their biological activities.

Materials & methods



7.1 Source of the data :



       The Preliminary data required for the experimental study was obtained

       from

       1. Library of Govt.college of pharmacy. Bangalore.

       2. JRD TATA memorial Library IISc. Bangalore.

       3. Chemical Abstracts.

       4. Journals and e-journals.

       5. Library and information centre, Rajiv Gandhi University of health

           Science, Bangalore.

       6. Internet Sources.

       7. http://www.rguhs.ac.in/HelinetHome/




7.2 Method of collection of data:
       Data pertaining to the present study will be obtained by

     Department of Pharmaceutical Chemistry laboratory, Govt.college of

  pharmacy. Bangalore.




7.3 Does the study require any investigations or interventions to be

   conducted on patients or other humans or animals? If so, please

   describe in brief.

                                     yes




7.4 Has ethical clearance been obtained from your institute in case 7.3?



                                   applied.
List of reference

    1. Kallury KMRR, Surendranath TG, Srinivasan VR., synthesis of some

       new substituted 1,2,4-triazole and 1,3,4-thiadiazole and their

       derivatives. Turk J Chem 2003; 27: 119-125

    2. Zamani K, Faghihi K, Sangi MR, Java., synthesis of some new

       substituted   1,2,4-Triazoles   and    1,3,4-Thiadiazoles   and   their

       derivatives. Turk J Chem 2003;119-125.

    3. XU, Liang-Zhong, JIAN, Fang-Fang Shi, Jian-Gang Sun, Ping-Ping,et-

       al., Synthesis, structure and biological activities of noval triazoles

       copounds containing N,N-Dialkyldithiocarbamate moiety. Chinese

       jounal of chemistry 2004;22;698-701.

    4. Liang-Zhongx, Shu-Shen Zhang, Shu-YanNiu, Yong-Qi Qin, Xue-mei

       li, Kuijiao., Synthesis and biological activities of novel triazole

       compounds containing 1,3-dioxolane rings. Molecules 2004; 9: 913-

       921.

    5. Bekircan O, kahveci B, Kucuk M., Synthesis and anticancer evaluation

       of some new unsymmetrical 3,5-diaryl-4H-1,2,4-triazole derivatives.

       Turk J Chem 2006; 30:29-40.

    6. Nasser S.A.M. khalil., synthesized N- and S--L-arabinopyranosyl

       (1,2,4) triazolo (3,4-b)(1,3,4)thiadiazoles.Eeuropean J of Medicinal

       chemistry. 2007;42:1193-1199.

    7. Ding Y, Zhang YY, Zhang J, Yao-quan chen., Synthesis and
   anticancer activity of ribonucleoside analogues containing thio-

   substituted five-membered heterocuylclic base. Bioorganic and

   medicinal chemistry letters 1997;7(13): 1607-1610.

8. Udupi RH, Bhatt AR. Synthesis of 4-(n-pyridyl carboxamide)-5-

   mercapto-3-substituted-1,2,4-triazoles for possible anti-tubercular

   activity., Indian J Heterocyclic Chem 1996;6:41-44.
9.    Signature of the Candidate:


10.   Remarks of the Guide:


11.   Name and Designation of:                M.S. NIRANJAN
                                             Professor & Head,
      11.1 Guide:                    Dept.of Pharmaceutical Chemistry,
                                        Govt. College of Pharmacy,
                                            Bangalore - 560 027.


      11.2 Signature:


      11.3 Co-guide:                       NOT APPLICABLE.




      11.4 Signature:


      11.5 Head of the Department:            M.S. NIRANJAN
                                             Professor & Head,
                                     Dept.of Pharmaceutical Chemistry,
                                        Govt. College of Pharmacy,
                                            Bangalore - 560 027.


      11.6 Signature:
12   12.1 Remarks of the chairman and Principal:


     12.2 Signature:                DR.SHASHIDHARA
                                    PRINCIPAL,
                                    GOVT. COLLEGE OF PHARMACY,
                                    BANGALORE –5600 27.

								
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