Karpagam, S (2014) Design, Synthesis and Characterization of N-Phenylpyrazoline and 3,4- Dihydropyrimidine from Chalcone Derivatives and study their Biological Activities. Masters thesis, College of Pharmacy, Madurai Medical College, Madurai.
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Abstract
Medicinal Chemistry is a Science Which includes all branches of Chemistry and biology. The discipline of Medicinal chemistry is devoted to the discovery and development of new agents for treating diseases. Most of this activity is directed to new natural or synthetic organic compounds. Inorganic compounds continue to be important in therapy. The molecules were designed by the software tools and the lead molecules of chalcone were synthesized by “ CLAISEN-SCHMIDT REACTION” followed by phenyl hydrazine and urea treatment forms N-phenylpyrazoline and 3,4-dihydropyrimidine respectively. The formation of molecules was confirmed by TLC. The structure of synthesized compounds were confirmed by FT-IR, 1HNMR, MASS Spectroscopy. The IR data’s showed relavant peaks for C=C, C=N, C=O groups. The 1HNMR also showed relavant proton peaks for all synthesized compounds. The MASS spectrum confirm the molecular ion peak of all synthesized compounds. The In-vitro anti-oxidant property for all the compounds showed positive results. The compounds K1, K3 & K6, K8 showed more potent activity. These four compounds shows Nphenylpyrazoline and 3,4-dihydropyrimidine with P-dimethyl amino benzaldehyde, Pchlorobenzaldehyde substitution at fifth and sixth position respectively. Hence the compounds may be evaluated for Anti-tuberculosis activity. The In-vitro anti-diabetic activity of all the compounds was evaluated and compared with standard. The compounds such as K1, K2 & K6, K7 showed more potent activity. Hence N-phenylpyrazoline and 3,4-dihydropyrimidine with P-Chloro baenzaldehyde, Trimethoxy benzaldehyde substitution at fifth and sixth position respectively showed better activity. The In-vitro anti-inflammatory activity of all the compounds was evaluated and compared with standard. All the compounds showed significant activity. The compounds such as K1, K3 & K6, K8 exhibited more potent activity. Based on In-vitro antioxidant activity the compounds K1, K3, K6, K8 were selected and evaluated for Anti-tuberculosis activity. The compounds K3 exhibit potent activity against Mycobacterium tuberculosis. Hence N-phenylpyrazoline with phenyl substitution at third position and P-dimehtyl amino benzaldehyde substitution at fifth position showed better activity. In Future, the compounds K1, K2, K6, K7 can be studied for In-vivo anti-diabetic activity as it exhibited significant In-vivo anti-diabetic activity.
| Item Type: | Thesis (Masters) |
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| Uncontrolled Keywords: | Design; Synthesis; Characterization; N-Phenylpyrazoline; Dihydropyrimidine; Chalcone Derivatives; Biological Activities |
| Subjects: | PHARMACY > Pharmaceutical Chemistry |
| Depositing User: | Ravindran C |
| Date Deposited: | 12 Jul 2017 05:45 |
| Last Modified: | 13 Oct 2017 00:15 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/1501 |
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