http://13.232.72.61:8080/jspui/handle/123456789/6242 2026-04-04T03:02:07Z http://13.232.72.61:8080/jspui/handle/123456789/6647 Title: Synthesis of Some Substitutal Pyrazoles and Evaluation of their Biological activities Authors: Mohammd T K, Shahin; Das, Amit Kumar Abstract: Synthesis of Some Substitutal Pyrazoles and Evaluation of their Biological activities Description: Dissertation 2011-05-01T00:00:00Z http://13.232.72.61:8080/jspui/handle/123456789/6584 Title: Synthesis and Pharmacological Evaluation of Coumarin Derivatives Authors: Thomas, Vidhya; Giles, D Abstract: Coumarins are a class of compounds with benzopyrone ring system and constitute the core structure of a number of pharmacologically and biologically active compounds notably Warfarin. In the present work we synthesized new Coumarin derivatives with various substitutions and tested their biological potentials like their anti inflammatory, analgesic, antiulcer and antimicrobial activities. Title compound, Schiff base was synthesized with various aldehydes from thiazolyl hydrazine derivatives of 4-hydroxy-3-(3-oxo-1-phenylbutyl)-2H-chromen-2-one obtained by condensation and cyclization from brominated 4-hydroxy-3-(3-oxo-1-phenylbutyl)- 2H-chromen-2-one with thiosemicarbazide. The compounds were characterized by physical and spectral datas, Molecular docking, QSPR studies and pharmacological evaluation were carried out for all synthesized derivatives. The synthesized compounds possessing electron withdrawing group (-NO2) in phenyl ring exhibited good pharmacological activities when compared to that of other. The derivatives 4(b), 4(j) and 4(g) showed good anti-inflammatory activity by binding mostly with Thr 206, Ser 455 and His 386 amino acids in the protein sequence. The nitro substituted derivative 4(a) showed significant analgesic activity. Derivatives 4(a), 4(b) and 4(j) showed significant antibacterial activity and derivatives 4(a) and 4(c) showed significant antifungal activity. The docking results were compared with the pharmacological activity of the synthesized compounds. Docking results and observed pharmacological activity results were in accordance with each other. Description: Dissertation 2011-05-01T00:00:00Z http://13.232.72.61:8080/jspui/handle/123456789/6583 Title: Synthesis, Antiinflammatory and Anti-microbial Evaluation Of Thiazolidinedione Derivatives Authors: Naranbhai, Ahir Shveta; Das, Amit Kumar Abstract: A series of Schiff bases, 4(a-j) were synthesized from N-carbamoyl-4-[(1E,3E)-3-(2,4- dioxo-1,3-thiazolidin-5-ylidene)prop-1-en-1-yl]]benzenesulfonamide by condensation with different substituted aromatic aldehydes. The N-carbamoyl-4-[(1E,3E)-3-(2,4-dioxo- 1,3-thiazolidin-5-ylidene)prop-1-en-1-yl]]benzenesulfonamide was prepared from a chalcone, 5E-5-[(2E)-3-phenylprop-2-en-1-ylidene]-1,3-thiazolidine-2,4-dione via sulfonylation followed by amidation. The chalcone was obtained by Claisen Schmidt condensation of cinnamaldehyde with 1,3-thiazolidin-2,4-dione. The structures of new synthesized compounds were confirmed by IR, 1H NMR and Mass spectral data. Synthesized derivatives were evaluated for their anti inflammatory, antibacterial and antifungal activities. The synthesized compounds 4(a), 4(c) and 4(j) were found to possess significant anti inflammatory, antibacterial and antifungal activities. The docking studies were carried out in 2OYE, 1CX2, 1CQE, 1CVU and 1DCX receptors. The compound possessing nitro and methoxy group as substituent in phenyl ring exhibited good pharmacological activities than other synthesized derivatives. Description: Dissertation 2011-05-01T00:00:00Z http://13.232.72.61:8080/jspui/handle/123456789/6582 Title: Synthesis and Pharmacological Evaluation of Some Pyrazole Derivatives for Anti-Inflammatory and Analgesic Activity Authors: Raju M, Sajani; Das, Amit Kumar Abstract: 3-methyl-1-phenyl-4,5-dihydro-1H-pyrazol-5-one obtained from phenyl hydrazine and ethyl acetoacetate was acetylated and then subjected to Claisen-Schmidt condensation with 4-hydroxy benzaldehyde to get a chalcone. This chalcone was cyclized with the help of hydroxylamine hydrochloride to form an isoxazole derivatives which were further condensed with various substituted aromatic aldehydes to obtain titled compounds (4aD1-4aD15). The structures of new synthesized compounds were confirmed by IR, 1H NMR and Mass spectral data. Synthesized derivatives were evaluated for their anti-inflammatory and analgesic activity. The compound 4aD3, 4aD8, 4aD9, 4aD10 and 4aD14 was found to have comparable anti-inflammatory activity with that of standard drug indomethacin. The compound 4aD3,4aD8, 4aD9, 4aD10 and 4aD11 was found to have comparable analgesic activity with that of standard drug tramadol. QSPR and Molecular Docking studies of the synthesized compounds were carried out to compare the physical property with biological activity. The compounds which have good pharmacological activity have good QSPR values which are in accordance with the observed anti-inflammatory activity. Docking studies were carried in COX I and COXII receptors. Most of the hydrogen bonds formed in docking studies are with the help of hetero atoms present in the parent nuclei pyrazole and isoxazole. This indicates the involvement of pyrazole and isoxazole nucleus in docking with COX 2 receptor and anti-inflammatory activity. Description: Dissertation 2011-05-01T00:00:00Z