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Synthesis, Characterization and Evaluation of 2-Amino 5 -Aryl 1,3,4 Thiadiazole Derivatives


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1 K.N.I.M.T. Faculty of Pharmacy, Sultanpur Uttar Pradesh-228001
     

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There are various biological activity of thiadiazole derivatives, I opted to synthesize derivatives having 1, 3, 4- thiadiazole nucleus and evaluate them for their antibacterial and anti-inflammatory activity. Various substituted 2 amino 5 aryl 1, 3, 4 thiadiazole derivatives were prepared by reacting various nitro and chloro substituted benzoic acid refluxing with thiosemicarbazide, bromine water ethanol and glacial acetic acid. Derivatives were characterized by FTIR, MASS and 1H NMR spectral data. All the compounds were evaluated for their in vitro antibacterial activity against two Gram negative strains (E. coli and P. aeruginosa) and two Gram-positive strains (Bacillus cereus and Staphylococcus aureus) and their minimum inhibitory concentration (MIC) were determined by disc diffusion method. Compounds were evaluated for their anti-inflammatory activity by carageneen method

Keywords

1, 3, 4 Thiadiazole, Antibacterial, Anti-inflammatory
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  • Sangapure S.S., Basawaraj R. Synthesis and biological activities of some 1,3,4-oxadiazoles, thiadiazoles, triazoles and related compounds possessing benzofuran moiety. Indian J. Pharm. Sci. 66(2): 2004; 221-225.
  • Cai-Jun Chen, Bao-An Song, Song Yang,Guang-Fang Xu, Pinaki S. Bhadury, Lin-HongJin, De-Yu Hu, Qian-Zhu Li, Fang Liu, Wei Xue, Ping Lu and Zhuo Chen; Synthesis andantifungal activities of 5-(3,4,5-trimethoxyphenyl)-2-sulfonyl-1,3,4- thiadiazole and 5- (3,4,5-trimethoxyphenyl)-2-sulfonyl-1,3,4- oxadiazole derivatives ;Bioorganic & Medicinal Chemistry 15 (2007) 3981–3989 .
  • A Gupta; P Mishra; SK Kashaw; V Kashaw;JP Stables; Synthesis of 3-aryl amino/amino-4-aryl-5-imino-D2-1,2,4-thiadiazoline and evaluated for anticonvulsant activity; European Journal of Medicinal Chemistry, 2008, 43, 749-754.
  • Schenone S, Bruno O, Ranise A, Bioorganic and Medicinal Chemistry 9,2001, 2149-2153.
  • Teranchian S., Tahmineh A., Mohammad R., Fazeli A.S. Bioorganic and Medicinal Chemistry Letter.17, 2007; 1023-1025.
  • Gazzar A E, Hegab M I, Bioorganic and Medicinal Chemistry Letters, 18,2008, , 4538-4543.
  • Sreenivasa A, Ghate Manjunath D, Indian Journal of Heterocyclic Chemistry, 11, 2002, 255-256
  • Sengupta, P., D. Deepak Kumar, C.V. Yeligar, K.Murugesh, D. Rajalingam, S. Jagadish and T.K.Maity, Evaluation of anticancer activity ofsome 1, 3, 4- oxadiazole derivatives. Indian J.Chem., 47 B,2008.: 460 - 462.
  • Rastogi, N., S. Rajendra, S. Shukla and R. Sethi,. Microwave mediated aminomethylation andantileishmanial activity of 2-{4'- (2",4"-Dichlorobenzyloxy)-phenyl}-1,3,4-oxadiazolin-5-thiones and 3-{4'-(2",4"-Dichlorobenzyloxy)-phenyl}-4-phenyl-1,2,4- triazolin-5- thiones. IndianJ. Heterocyclic Chem., 16: 2006 175- 181.
  • Xin-Ping, H., Z. Lin-Mei and Z. Zi-yi,.Synthesis and antibacterial activities of1,3,4-thiadiazole, 1,3,4-oxadiazole and 1,2,4-triazole derivatives of 5-methyl isooxazole.Indian J. Chem., 38B,1999: 1066 - 1069.
  • Barreiro E J, Varandas L S, Fraga C A, Letters in Drug Design and Discovery, 2,2005, , 62- 67.
  • Moreira A, Piuvezam M R, Journal of Ethnopharmacology 67,1999;, 171–177

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  • Synthesis, Characterization and Evaluation of 2-Amino 5 -Aryl 1,3,4 Thiadiazole Derivatives

Abstract Views: 318  |  PDF Views: 2

Authors

Arvind Kr. Singh
K.N.I.M.T. Faculty of Pharmacy, Sultanpur Uttar Pradesh-228001
Deepika Singh
K.N.I.M.T. Faculty of Pharmacy, Sultanpur Uttar Pradesh-228001

Abstract


There are various biological activity of thiadiazole derivatives, I opted to synthesize derivatives having 1, 3, 4- thiadiazole nucleus and evaluate them for their antibacterial and anti-inflammatory activity. Various substituted 2 amino 5 aryl 1, 3, 4 thiadiazole derivatives were prepared by reacting various nitro and chloro substituted benzoic acid refluxing with thiosemicarbazide, bromine water ethanol and glacial acetic acid. Derivatives were characterized by FTIR, MASS and 1H NMR spectral data. All the compounds were evaluated for their in vitro antibacterial activity against two Gram negative strains (E. coli and P. aeruginosa) and two Gram-positive strains (Bacillus cereus and Staphylococcus aureus) and their minimum inhibitory concentration (MIC) were determined by disc diffusion method. Compounds were evaluated for their anti-inflammatory activity by carageneen method

Keywords


1, 3, 4 Thiadiazole, Antibacterial, Anti-inflammatory

References