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1, 2, 4- Triazole Derivatives and its Pharmacological Activities


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1 Kamla Nehru Institute of Management and Technology (Faculty of Pharmacy), Sultanpur UP-228001, India
     

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Triazole, a heterocyclic nucleus has attracted a wide attention of the medicinal chemist in search for the new therapeutic molecules. This review provides a brief summary of 1,2,4-triazole Derivatives and its Pharmacological activities and highlights some examples of 1,2,4-triazole-containing drug substances. Either as single heterocyclic derivatives or in fusion with the other cycles, these heterocycle is emerging as the most explored centre to obtain clinically significant compounds. The major activities exhibited by 1,2,4 derivatives include antibacterial, antifungal, antiviral, antidepressant, antimalarial, hypnotic, anticonvulsant and anti-inflammatory activities.

Keywords

1,2,4- Triazoles, Pharmacological Activities
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  • Neeraj Upmanyu, Sanjay Kumar, Murali-dhar, Kamal Shah and Praadep Mishra, “Synthesis And Anti –Microbial Evaluation of Some Novel 1,2,4 -Triazole Derivatives”, Acta Poloniae Pharmaceutical Drug Research,2011, Vol. 68 No. 2, 213- 221.
  • Mevlut Serdar Nurhan Gumrukcuoglu ,Sengul alpay Karaogluaraoglu, Neslihan Demirbas, “Synthesis of Some Novel 3,5-Diaryl-1,2,4-TriazoleDerivatives and Investigation of Their Antimicrobial Activities”, Turk J Chem,2007, 31, 315 – 326 .
  • Rajkumar Agrawal and S. S. Pancholi, “Synthesis, characterization and evaluation of antimicrobial activity of a series of 1,2,4-triazoles”, Der Pharma Chemica,2011, 3 (6), 32- 40.
  • Yasemin Unver, Esra Dugdu, Kemal Sancak, Mustafa ER, Sengul Alpay Karaoglu, “Synthesis and Antimicrobial and Antitumor Activity of Some New [1,2,4] Triazole-5-one Derivatives”, Turk J Chem , 2009, 33 , 135 – 147 .
  • Jolanta Kutkowska, Bozena Modzelewska-Banachiewicz, Grazyna Ziolkowska, Wojciech Rzeski, Teresa Urbanik- Sypniewska, Zofia Zwalska and Monika Prus ,“ Antimicrobial activity of 3,4-Disubstituted-1,2,4-Triazole Derivatives”, Acta Poloniae Pharmaceutical Drug Research, 2005,Vol. 62 No. 4, 303-306
  • Hacer Bayrak, Ahmet Demirbas, Hakan Bektas, Sengul Alpaj Karagolu, Neslihas Demirbas, “Synthesis and antimicrobial activities of some new 1,2,4-triazole derivatives”, Turk J Chem , 2010 , 34, 835 – 846.
  • Joanna Stefanska, Stefan Tyski, Jerzy, Kossakowski and Maria Dobosz et al, “Antimicrobial activity of 2,4 dihydro-[1,2,4] triazol-3-one Derivatives,” Polish J Microbiology 2008 ,Vol-57 No-2, 179-182 .
  • Syed Azhar Nizami, M. Gurumurthy, Swarup Jyoti Chattarjee, Debashisha Panda, “Evaluation of Antimicrobial Potency of Some Synthesized Thiazolidin-4-one substituted 1,2,4-triazoles”, Journal of Advanced Pharmaceutical Research. 2010, 1, 26-35.
  • Monazza Serwar, Tashfeen Akhtar, Shahid Hameed, and Khalid M. Khan, “Synthesis, urease inhibition and antimicrobial activities of some chiral 5-aryl-4-(1-phenylpropyl)-2H-1,2,4- triazole-3(4H)-thiones”, ARKIVOC 2009, (vii), 210-221.
  • Nitin Muthal, Jyoti Ahirwar, Dheeraj Ahriwar, Pankaj Masih, Tanaji Mahmdapure and T. Sivakumarm, “Synthesis, Antimicrobial and Anti-inflammatory Activity of Some 5- Substituted-3-pyridine-1, 2, 4-Triazoles”, International Journal of PharmTech Research,2010, Vol.2, No.4, 2450-2455.
  • Deniz Sahin, Hacer Bayrak, Ahmet Demirbas, Nelihan Demirbas, Sengul Alpaj Karagolu,“Design and synthesis of new 1,2,4-triazole derivatives containing morpholine moiety as antimicrobial agents,”, Turk J Chem ,2012, 36 , 411 – 426..
  • Shantaram Khanage, Popat Mohite, Ramdas Pandhare, Appala Raju, “Synthesis and pharmacological evaluation of isoxazole derivatives containing 1,2,4-triazole Moiety”, Marmara Pharm, 2012, J 16: 134-140.
  • Katica Colanceska-Ragenovic, Vesna Dimova, Vlado Kakurinov, Dora Gabor Molnar and Aleksandra Buzarovska, “Synthesis, Antibacterial and Antifungal Activity of 4-Substituted-5-Aryl- 1,2,4-Triazoles”, Molecules 2001, 6, 815- 824.
  • Freddy H. Havaldar and Abhay R. Patil, “Abhay R. Patil ,“Syntheses of 1, 2, 4 Triazole Derivatives and their Biological Activity”, E-Journal of Chemistry, Vol. 5, No.2, pp.347-354, April 2008,Vol. 5, No.2, 347-354 .
  • Rambabu Nunna, Ramachandran. D and Viral B. Modi, Kirti J. Goswami et al, “Synthesis, characterization and biological evaluation of 2,6 diphenyl-3-(4-(3-phenyl-[1,2,4]triazolo [3,4b][1,3,4]thione”, Der Pharma Chemica,2012,4 (2),639-643.
  • Navin B. Patel and Imran H. Khan, “Synthesis of 1,2,4-triazole derivatives containing benzothiazoles as pharmacologically active molecule” Journal of Enzyme Inhibition and Medicinal Chemistry, 2011; 26(4),527–534.
  • E.V.S. Subrahmanyam, B.C. Revanasiddappa, K. Ishwar Bhat, Jisha Prems, P.S.Surya, “Synthesis and biological evaluation of some new 1,2,4-triazolo-[3,4,-b]-1,3,4-thiadiazoles”, J. Chem. Pharm. Res., 2010, 2(5):323-326.
  • Raafat M. Shaker, The chemistry of mercapto- and thionesubstituted 1,2,4-triazoles and their utility in heterocyclic synthesis,” ARKIVOC, 2006 ,(ix), 59-112.
  • Nubia Boechat ,Luiz C.S. Pinheiro, Osvaldo A. Santos-Filho and Isabor C. Silva, “Design and Synthesis of New N-(5- Trifluoromethyl)-1H-1,2,4-triazol-3-yl Benzenesulfonamides as Possible Antimalarial Prototypes” Molecules 2011, 16, 8083- 8097 .
  • Shantaram G. Khanagea, b, Popat B. Mohite, Ramdas B. Pandhareb, S. Appala Raju,“Study of analgesic activity of novel 1,2, 4-triazole derivatives bearing pyrazole and tetrazole moiety”, Journal of Pharmacy Research 2011, 4(10), 3609-3611.
  • Sudeep K. Mandal, Dibyajyoti Saha, Vibhor K. Jain, Bindu Jain,“Synthesis and Antitubercular activity of some triazole derivatives of Propyl Gallate,” International Journal of Pharma Sciences and Research (IJPSR),2010, Vol.1 (11), 465-472.
  • Pradeep K Goyal, Anil Bhandari, AC Rana , CB Jain ,“Synthesis of Some 3- Substituted -4H-1, 2, 4-Triazole Derivatives With Potent Anti-Inflammatory Activity”, Asian Journal of Pharmaceutical and Clinical Research 2010, 3, Issue 3, 244-246.
  • Abdel-Rahman Farghalya, Abdel-Rahman Farghaly, Erik De Clercq, and Hussein El- Kashef, “Synthesis and antiviral activity of novel[1,2,4]triazolo[3,4-b][1,3,4] thiadiazoles, [1,2,4 ]triazolo[3,4-b][1,3,4] thiadiazines and [1,2,4]triazolo[3,4- b][1,3,4] thiadiazepines”, ARKIVOC 2006, (x), 137-151.
  • Asif Husain, Mohammad A. Naseer and Mohammad Sarafroz, “Synthesis and Anticonvulsant Activity of Some Novel Fused Heterocyclic1,2,4-Triazoo-[3,4-b]-1,3,4-Thiadiazole Derivatives”, Acta Poloniae Pharmaceutical n Drug Research, 2009, 66 No. 2, 135-140 .
  • Sudhir N. Sambrekar, Suhas A. Patil, “Synthesis of 3- Substituted-4-Amino-5-Mercapto-4(H)-1, 2, 4-Triazole And Screening for Anti-Convulsant Activity”, Apr–Jun 2011, 2 (2) 520-524.
  • Mahendra R. Shiradkar, Mangesh Ghodake, Kailash G. Bothara, Shashikant V. Bhandari, Ana Nikalje, C Kalyan Chakravarthy Akula, Nisheeth C. Desai, and Prashant J. Burange, “Synthesis and anticonvulsant activity of clubbed thiazolidinone–barbituric acid and thiazolidinone–triazole derivatives”, ARKIVOC 2007 (xiv), 58-74. .
  • Olcay Bekircan, Bahittin Kahveci, Murat Kucuk,“Synthesis and Anticancer Evaluation of Some New Unsymmetrical 3,5-Diaryl- 4H-1,2,4-Triazole Derivatives”, Turk J Chem, 2006 ,30 ,29 – 40.
  • Dhanya Sunil, Arun M Isloor and Prakash Shetty, “Synthesis, characterization and anticancer activity of 1,2,4-Triazolo[3,4-b]- 1,3,4-thiadiazoles on Hep G2 cell lines”, Der Pharma Chemica, 2009, 1(2): 19-26 .
  • Dooseop Kim , Liping Wang , Maria Beconi , George J. Eiermann , Michael H. Fisher , Huaibing He , Gerard J. Hickey , Jennifer E. Kowalchick , Barbara Leiting , Kathryn Lyons , Frank Marsilio , Margaret E. McCann , Reshma A. Patel , Aleksandr Petrov , Giovanna Scapin , Sangita B. Patel , Ranabir Sinha Roy , Joseph K. Wu , Matthew J. Wyvratt , Bei B. Zhang , Lan Zhu , Nancy A. Thornberry ,and Ann E. Weber,“(2R)-4-Oxo-4- [3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl) butan-2-amine:i A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes” J. Med. Chem., 2005, 48 (1), 41–151.
  • A. Cansiz, M. Koparir and A. Demirdag, “Synthesis of Some New 4, 5-Substituted-4H-1,2,4-triazole-3-thiol Derivatives,” Molecules 2004, 9, 204-212.

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  • 1, 2, 4- Triazole Derivatives and its Pharmacological Activities

Abstract Views: 647  |  PDF Views: 5

Authors

Vipul Singh
Kamla Nehru Institute of Management and Technology (Faculty of Pharmacy), Sultanpur UP-228001, India
Arvind Kumar Singh
Kamla Nehru Institute of Management and Technology (Faculty of Pharmacy), Sultanpur UP-228001, India
Rohit Tripathi
Kamla Nehru Institute of Management and Technology (Faculty of Pharmacy), Sultanpur UP-228001, India
Preeti Mishra
Kamla Nehru Institute of Management and Technology (Faculty of Pharmacy), Sultanpur UP-228001, India
Roopes Kumar Maurya
Kamla Nehru Institute of Management and Technology (Faculty of Pharmacy), Sultanpur UP-228001, India

Abstract


Triazole, a heterocyclic nucleus has attracted a wide attention of the medicinal chemist in search for the new therapeutic molecules. This review provides a brief summary of 1,2,4-triazole Derivatives and its Pharmacological activities and highlights some examples of 1,2,4-triazole-containing drug substances. Either as single heterocyclic derivatives or in fusion with the other cycles, these heterocycle is emerging as the most explored centre to obtain clinically significant compounds. The major activities exhibited by 1,2,4 derivatives include antibacterial, antifungal, antiviral, antidepressant, antimalarial, hypnotic, anticonvulsant and anti-inflammatory activities.

Keywords


1,2,4- Triazoles, Pharmacological Activities

References