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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