Refine your search
Collections
Co-Authors
Year
A B C D E F G H I J K L M N O P Q R S T U V W X Y Z All
Kobzar, Natalya P.
- Search for Biologically Active Substances with Antimicrobial and Antifungal Action in the Series of 2.5-Disubstituted 1, 3, 4-Tiadiazoles
Abstract Views :141 |
PDF Views:0
Authors
Igor V. Sych
1,
Iryna V. Drapak
2,
Marharyta M. Suleiman
1,
Maryna V. Rakhimova
1,
Natalya P. Kobzar
1,
Irina A. Sych
1,
Lina O. Perekhoda
1
Affiliations
1 Department of Medicinal Chemistry, National University of Pharmacy, 53, Pushkinskaya St., Kharkiv, UA
2 Department of General, Bioinorganic, Physical and Colloidal Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska str. 69, Lviv, 79010, UA
1 Department of Medicinal Chemistry, National University of Pharmacy, 53, Pushkinskaya St., Kharkiv, UA
2 Department of General, Bioinorganic, Physical and Colloidal Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska str. 69, Lviv, 79010, UA
Source
Research Journal of Pharmacy and Technology, Vol 12, No 6 (2019), Pagination: 2871-2876Abstract
A range of derivatives of sulfonyl-substituted nitrogen-containing heterocyclic systems has been extended by synthesis of 2N (R)-5R1-1,3,4-thiadiazol-2-yl-arylsulfonamides and N-(diethylsulfamoyl)-N-(5-ethyl-1,3,4-thiadiazol-2-yl)benzamides. It was established that acylation of 5-ethylsulfanyl-1,3,4-thiadiazole-2-amine by heteryl-substituted acid chlorides allowed for obtaining not reported in the literature heterocyclic compounds, which structure contained two cycles of 1,3,4-thiadiazole. The structure and purity of the obtained compounds was confirmed by 1Н NMR-spectroscopy, elemental analysis, and thin-layer chromatography. Pharmacological studies on antimicrobial and antifungal activity have shown that all the compounds tested have sensitivity to both Gram-positive, and Gram-negative bacteria. In addition, the obtained substances have exhibited antifungal activity against Candida albicans. The studies have identified compound 4-butoxy-N-{5-[({[5- (ethylsulfanyl)-1,3,4-thiadiazol-2-yl] carbomoyl} methyl) sulfanyl] -1,3,4-thiadiazol-2-yl} benzamide with high antimicrobial activity further studies of which are promising.Keywords
Synthesis, 2.5-Disubstituted 1, 3, 4-Tiadiazoles, Antibacterial and Antifungal Activity.
References
- Padmavathi V, Reddy GS, Padmaja A, Kondaiah P, Shazia A. Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. Eur J Med Chem. 2011; 44: 2106–2112.
- Talath S, Gadad AK. Synthesis, antibacterial and antitubercular activities of some 7-[4-(5-amino-[1,3,4]thiadiazole-2-sulfonyl)-piperazin-1-yl] ßuoroquinolonic derivatives. Eur J Med Chem. 2006; 41: 918–924.
- Foroumadi A, Emami S, Hassanzadeh A, Rajaee M, Sokhanvar K, Moshap MH, Shapee A. Synthesis and antibacterial activity of N-(5-benzylthio-1,3,4-thiadiazol-2-yl) and N-(5-benzylsulfonyl-1,3,4-thiadiazol-2-yl)piperazinyl quinolone derivatives. Bioorg Med Chem Lett. 2005; 15: 4488–4492.
- Padmavathi V, Thriveni P, Reddy GS, Deepti D. Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. Eur J Med Chem. 2008; 43: 917–924.
- Chen C, Song B, Yang S, Xu G, Bhadury PS, Jin L, Hu D, Li Q, Liu F, Xue W, Lu P, Chen Z. Synthesis and antifungal activities of 5-(3,4,5-trimeth-oxyphenyl)-2-sulfonyl-1,3,4-thiadiazole and 5-(3,4,5-tri-methoxyphenyl)-2-sulfonyl-1,3,4-oxadiazole derivatives. Bioorg Med Chem. 2007; 15: 3981–3989.
- Padmavathi V, Reddy GD, Reddy SN, Mahesh K. Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl)methylthio) methylene)malononitriles. Eur J Med Chem. 2011; 46: 1367–1373.
- Khalaj A, Nakhjiri N, Negahbani AS, Samadizadeh M, Firoozpour L, Rajabalian S, Samadi N, Faramar-zi MA, Adibpour N, Shapee A, Foroumadi A. Discovery of a novel nitroimidazolyleoxazolidinone hybrid with potent anti Grampositive activity: synthesis and antibacterial evaluation. Eur J Med Chem. 2011; 46: 65–70.
- Sych IV, Perekhoda LO, Yeromina HO. Synthesis, physicochemical properties and prediction of the biological activity of new derivatives of 2-R1-N-(5-R-1,3,4-thiadiazol-2-yl)benzosulfonamides. Annals of Mechnikov Institute. 2015; 4: 75-81.
- Onkol T, Dogruer DS, Uzun L et all. Synthesis and antimicrobial activity of new 1,2,4-triazole and 1,3,4-thiadiazole derivatives. J Enzyme Inhib. Med Chem. 2008; 23: 277-284.
- Murugan V, Brijesh J, Geetha KM. Synthesis of 2-Imino-3-(5-Aryl-1, 3, 4-thiadiazol-2-yl)-5-arylidene-1, 3-thiazol-4-one as potent cns depressant and antimicrobial agents. Asian J. Research Chem. 2010; 3(3): P. 698-702.
- Anoop Singh, Acrana. Synthesis, spectral characterization and pharmacological screening of 1-methylene-4-(5-(4-(phenylamino)phenyl)-1,3,4-thiadiazol-2-yl) thiosemicarbazide derivatives. Research J. Pharm. and Tech. 2011; 4(2): P. 279-285.
- Sunakar P, Jagat KT. Thermodynamic, spectral and antimicrobial properties of inclusion complexes of 2-[benzylidenamino]-1,3,4-thiadiazino[6,5b]indole and 2-[furfurlidenamino]-1, 3, 4-thiadiazino [6,5b] indole: A Comparative Study. Research J. Pharm. and Tech. 2011; 4(11): P. 1693-1698.
- Vinita G, Sanchita S, Gupta Y.K. Synthesis and antimicrobial activities of Zn (II) complex of 2,5-diamino-1,3,4-thiadiazole. Research J. Science and Tech. 2013; 5(4): P. 462-465.
- Pradeep Kumar Y, Sreenivasulu M, Yasmeen R, Ramya Smruthiraj V, Swathi V. A review on 1,3,4-thiadiazoles. Asian J. Research Chem. 2013; 6(3): P. 272-277.
- Thriveni P, Hari Krishna M, Murali K, Sekhar T. Synthesis and biological evaluation of novel 1,3,4-thiadiazole heterocyclic derivatives as novel anti-microbial agents. Asian J. Research Chem. 2016; 9(3): P. 107-112.
- Shetha FA, Zainab HKA, Iman. MM. Synthesis, characterization of new 1,3,4-thiadiazole derivatives with studying their biological activity. Research J. Pharm. and Tech. 2018; 11(1): 284-293.
- Mustafa KS, Waseela AAR, Omar DAS, Sahar HM, Mustafa KM, Ansam NK. Ultrasonic synthesis and antimicrobial activity of some diazenyl-1,3,4-thiadizole derivatives. Research J. Pharm. and Tech. 2018; 11(3): 1089-1091.
- Karthic R, Andrews B, Subramani K. Microwave assisted synthesis and antifungal studies of 5-amino thiadiazole substituted pyrimidine compounds. Asian J. Research Chem. 2017; 10(2):119-123.
- Preety Mishra, Arvind Kumar Singh, Rohit Tripathi, Alok Giri. Review article on 2, 5-disubstituted-1,3,4-thiadiazole derivatives and its pharmacological activities. Asian J. Research Chem. 2015; 8(5): P. 362-368.