A REVIEW ON THE VARIOUS BIOLOGICAL ACTIVITIES OF THIADIAZOLE

Authors

  • Dinesh Mehta M. M College of pharmacy, M. M. U, Mullana, 133207, India.
  • Poonam Taya M. M College of pharmacy, M. M. U, Mullana, 133207, India.
  • Neetu R.K.S.D College of Pharmacy, Kaithal

Keywords:

Thiadiazole, Anti-inflammatory, Antimicrobial, Antihelminthics, Anticancer, Antibacterial and antiviral

Abstract

Thiadiazole and their derivatives have been studied colossally because of their wide range of biological activity. They are found to be effectual as antibacterial, antimalarial, antiviral, antiinflammatory, anticancer and antianthelminthic agents. Distinct biological activities, such as antibacterial, anti-inflammatory, and antiviral have been consort with 1, 3, 4-thiadiazole derivatives. The substituted 1, 3, 4 Thiadiazole nucleus is particularly ubiquitous, and found in some marketed drugs such as acetazolamide, Methazolamide and antibacterial such as Sulphamethazole, antibiotic like Cefazoline. The synthesis of 1, 3, 4 Thiadiazole derivatives has allured widespread attention due to their diverse biological activities, including antimicrobial, anti-inflammatory, analgesic, and antianthelmintic. These reviews focused on various biological activities consorted with thiadiazole nucleus.

 

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Author Biography

Neetu, R.K.S.D College of Pharmacy, Kaithal

Assistant professor in Department Of Chemistry,R.K.S. D College of Pharmacy, Kaithal, India.

References

Singh AK, Parthsarthy R, Kshitiz J, Mishra G. Synthesis, characterization and antibacterial activity of 1, 3, 4-thiadiazole derivatives. IJSID 2011;3:353-61.

Siddiqui N, Ahuja P, Ahsan W, Pandeya SN, Alam SM. Thiadiazoles: Progress report on biological activities. J Chem Pharm Res 2009;1:19-30.

Jalhan S, Jindal A, Gupta A, Hemraj. Synthesis, biological activities and chemistry of thiadiazole derivatives and schiff bases. Asian J Pharm Clin Res 2012;3:199-208.

Foroughifar N, Mobinikhaledi A, Ebrahimi S, Moghanian H, Bodaghi Fard MA, et al. Synthesis of a new class of azathia crown macrocycles containing two1, 3, 4-thiadiazole rings as subunits. Tetrahedron Lett 2009;50:836–9.

Bhat RA, Tazeem Amir A, Choi I, Athar F. 3-(1, 3, 4-Thiadiazole-2-yl) quinoline derivatives: Synthesis, characterization and anti-microbial activity. Eur J Med 2011;46:3158-66.

Chapleo BC, Myers M, Myers PL, Saville JF, Smith ACB, Stillings MR, et al. Substituted 1, 3, 4-Thiadiazoles with anticonvulsant activity Hydrazines. J Med Chem 1986;29:2273-80.

Jung KY, Kim SK, Gao ZG, Gross AS, Melman N, Jacobsonb KA, et al. Structure–activity relationships of thiazole and thiadiazolederivatives as potent and selective human adenosine A3 receptor antagonists. Bioorg Med Chem 2004;12:613–23.

Shen HL, Yu Li, H Shang HX, Tian S, Lai YS, Liu LJ. Synthesis and cytotoxic evaluation of new colchicine derivatives bearing 1, 3, 4-thiadiazole moieties. Chin Chem Lett 2013;24:299–302.

Juszczak M, Matysiak J, Szeliga M, Zarowski P, Niewiadomy N, Albrecht J, et al. 2-Amino-1, 3, 4-thiadiazole derivative (FABT) inhibits the extracellular signal-regulated kinase pathway and induces cell cycle arrest in human non-small lung carcinoma cells. Bioorg Med Chem Lett 2012;22:5466–9.

Kumar AK, Kumar VG, Renuka N. Thiadiazoles: molecules of diverse applications-a review. Int J Chem Tech Res 2013;5:239-48.

Mahendrasinh MR, Patel HV, Lata MR, Patel NK. Synthesis and biological evaluation of some new 1, 3, 4-thiadiazole derivatives for their antimicrobial activities. IJPCBS 2013;3:814-9.

Kamal M, Shakya AK, Jawid T. 1, 3, 4-Thiadiazole as Antimicrobial agent: a review. IJBR 2011;1:41â€61.

Bak B, Nygaard L, Pedersen EJ, Anderson RJ. A mathematical contribution to structure-activity studies. Mol Spectra 1996;19:283.

Paul F, Jasont B, Mark H, jean MJF. Synthesis, antibacterial and antifungal activities of triazine derivatives. J Am Chem Soc 2003;125:13165.

Yang SJ, Lee SH, Kwak HJ, Gong YD. Regioselective Synthesis of 2Â°ï€ Amino-Substituted 1, 3, 4-Oxadiazoleand 1, 3, 4-Thiadiazole Derivatives via Reagent-Based Cyclization of Thiosemicarbazide Intermediate. J Org Chem 2013;78:438−44.

Katritzky R, Logowski R. Synthesis and antifungal activity of some 2-aryl-3-hydroxymethylbenzo[b]thiophenes. Int J Chem Tech Res 1963;2:27.

Mahendrasinh MR, Patel HV, Lata M, Patel NK. Synthesis, Characterization and Antimicrobial Evaluation of some 5-(substituted)-2-amino-Thiadiazoles. Int J Res Chem Environ 2013;3:9-15.

Srivastava SK, Vermaand S, Srivastava SD. Synthesis, characterization and biological activity of 1, 3-thiazolidin-4-one derivatives of 2-mercapto-5-methyl-1, 3, 4-thiadiazole. J Chem Pharm Res 2010;5:270-6.

Turner S, Myers M, Gadie B, Hale SA, Horsley A, Nelson AJ, et al. Antihypertensive thiadiazoles-vasodilator activity of Some2-Aryl-5-guanidino-1, 3, 4-t hiadiazoles. J Med Chem 1988;31:906-13.

Chapleo BC, Myers PL, Smith CBA, Tulloch IF, Walter DS. Substituted 1, 3, 4-thiadiazoles with anticonvulsant activity. J Med Chem 1987;30:951-4.

Rushda P, Ahmad S, Mishra R, Alam S. Potential review on thiadiazoles. Int J Chem Tech Res 2006;6:2917-23.

Kucukguzel G, Satılmıs G, Nichols DB, Talele TT, Gurukumar KR, Basu NK, et al. 2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase. Eur J Med Chem 2013;69:931-41.

Misra U, Hitkari A, Saxena AK, Gurtu S, Shanker K. Biologically active indolylmethyl-1, 3, 4-oxadiazoles, 1, 3, 4-thiadiazoles, 1, 3, 4-triazoles and 1, 2, 4-triazines. Eur J Med Chem 1996;31(7-8):629-34.

Rollas S, Kokyan S, Kaymakioglu KB, Turan SO, Akbuga J. Synthesis and evaluation of cytotoxic activities of some substituted isoxazolone derivatives. Eur J Med Chem 2011;15:94-9.

Gilani SJ, Khan SA, Siddiqui N. Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted 1, 2, 4-triazolo-[3, 4-b]-1, 3, 4-thiadiazole and 1, 3, 4 oxadiazole derivatives of isoniazid. Bioorg Med Chem Lett 2010;20:4762–5.

Yang SJ, Lee SH, Kwak HJ, Gong YD. Regioselective synthesis of 2amino-substituted 1, 3, 4-oxadiazole and 1, 3, 4-thiadiazole derivatives via reagent-based cyclization of thiosemicarbazide intermediate. J Org Chem 2013;78:438−44.

Maddila S Gorle, Sampath C, Lavanya P. Synthesis and anti-inflammatory activity of some new 1, 3, 4-thiadiazoles containing pyrazole and pyrrole nucleus. J Saudi Chem Soc 2012;3:16-25.

Amir M, Kumar H, Javed SA. Condensed bridgehead nitrogen heterocyclic system: Synthesis and pharmacological activities of 1, 2, 4-triazolo-[3, 4-b]-1, 3, 4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid. Eur J Med Chem 2008;43:2056-66.

Radwan MAA, Ragab EA, Sabrya NM, Shenawy El SM. Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents, Bioorg Med Chem 2007;15:3832–41.

Dawood KM, Gawad HA, Rageb EA, Ellitheyc M, Mohamed HA. Synthesis, anticonvulsant, and anti-inflammatory evaluation of some new benzotriazole and benzofuran-based heterocycles. Bioorg Med Chem 2006;14:3672–80.

Schenone S, Brullo C, Bruno O, Bondavalli F, Ranise A, Filippelli W, et al. New 1, 3, 4-thiadiazole derivatives endowed with analgesic and anti-inflammatory activities. Bioorg Med Chem 2012;14:1698–705.

Kuldipsinh P, Barot KS, Manjunath DG. Design, synthesis and antimicrobial activities of some novel 1, 3, 4-thiadiazole, 1, 2, 4-triazole-5-thione and 1, 3-thiazolan-4-one derivatives of benzimidazole. J Saudi Chem Soc 2013;6:1725-34.

Plech T, Wujec M, Kosikowska U, Barbara K. Studies on the synthesis and antibacterial activity of 3, 6-disubstituted 1, 2, 4-triazolo[3, 4-b]1, 3, 4-thiadiazoles. Eur J Med Chem 2012;47:580-4.

Kaur A, Kumar R, Kalidhar U. Synthesis, spectral studies and biological activity of some novel biphenyl imidazo[2, 1-b][1, 3, 4]thiadiazole derivatives. RJPBCS 2012;2:1085-6.

Mahendrasinh MR, Patel H, raj LM, Patel NK. Synthesis and biological evaluation of some new 1, 3, 4-thiadiazole derivatives for their antimicrobial activities. IJPCBS 2013;3:814-9.

Singh AK, Parthsarthy RK, shitiz J, Mishra M. Synthesis, Characterization and antibacterial activity of 1. 3. 4-thiadiazole derivatives. IJSID 2011;3:353-61.

Bhat AR, Tazeem Azam A, Choi I, Athar F. 3-(1, 3, 4-Thiadiazole-2-yl)quinoline derivatives: Synthesis, characterizationand anti-microbial activity. Eur J Med Chem 2011;46:3158-66.

Swamy SN, Basappa BS, Prabhuswamy B, Doreswamy BH, Prasad JS, Rangappa S. Synthesis of pharmaceutically important condensed heterocyclic 4, 6-disubstituted-1, 2, 4-triazolo-1, 3, 4-thiadiazole derivatives as antimicrobials. Eur J Med Chem 2006;41:531–8.

Talath S, Gadad AK. Synthesis, antibacterial and antitubercular activities of some 7-[4-(5-amino-[1, 3, 4]thiadiazole-2-sulfonyl)-piperazin-1-yl] fluoroquinolonic derivatives. Eur J Med Chem 2006;41:918–24.

Zhao HC, Shi YP, Liu YM, Li CW, Xua LN, Wang P, et al. Synthesis and antitumor-evaluation of 1, 3-selenazole-containing 1, 3, 4-thiadiazole derivatives. Bioorg Med Chem Lett 2013;23:6577–9.

Mohammadhosseini N, Parastoo SA, Aryapour H, Afshar F, Edraki N, Siavoshi F, et al. Synthesis and biological evaluation of novelbenzyl piperazine derivatives of 5-(5-nitroaryl)-1, 3, 4-thiadiazoles as Anti-Helicobacter pylori agents. J Pharm Sci 2013;21:66-73.

Omaima M, Abdelhafez KM, Ali AH, Mohamed M, Batran ARZ. Synthesis of new 7‑Oxycoumarin derivatives as potent and selective monoamine oxidase inhibitors. J Med Chem 2012;55:10424−36.

Cara L, Carrion MD, Entrena A, Gallo AM, Espinosa A, Lopez A, et al. 1, 3, 4-Thiadiazole derivatives as selective inhibitors of iNOS versus nNOS: Synthesis and structure-activity dependence. Eur J Med Chem 2012;50:129-39.

Song XJ, Dong XSY. Microwave-assisted synthesis of some novel fluorinated pyrazolo[3, 4-d]pyrimidine derivatives containing 1, 3, 4-thiadiazole as potential antitumor agents. Chin Chem Lett 2012;22:1036–8.

Gullar RK, Metin B, Arslan BS, Gokce AK. Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1, 3, 4-thiadiazole-2-sulfonamide. Eur J Med Chem 2010;45:4769-73.

Ibrahim DA. Synthesis and biological evaluation of 3, 6-disubstituted [1, 2, 4]triazolo[3, 4-b][1, 3, 4]thiadiazole derivatives as a novel class of potential anti-tumor agents. Eur J Med Chem 2009;44:2776–81.

Yusuf M, Khan RA, Ahmed B. Synthesis and anti-depressant activity of 5-amino-1, 3 4-thiadiazole-2-thiol imines and thiobenzyl derivatives. Bioorg Med Chem 2008;16:8029–34.

Terzioglu N, Gursoy A. Synthesis and anticancer evaluation of some new hydrazine derivatives of 2, 6-dimethylimidazo [2, 1-b]-[1, 3, 4] thiadiazole-5-carbohydrazide. Eur J Med Chem 2003;38:781-6.

Stephen T, Myers M, Gadie B, Stafford AH, Horsley A, Nelson AJ, et al. Antihypertensive Thiadiazoles. 2. ' Vasodilator Activity of Some 2-Aryl-5-guanidino-1, 3, 4-t hiadiazoles J Med Chem 1988;31:906-13.

Published

01-04-2015

How to Cite

Mehta, D., P. Taya, and Neetu. “A REVIEW ON THE VARIOUS BIOLOGICAL ACTIVITIES OF THIADIAZOLE”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 7, no. 4, Apr. 2015, pp. 39-47, https://journals.innovareacademics.in/index.php/ijpps/article/view/3126.

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Section

Review Article(s)