Pharmacological screening of some newly synthesized triazoles for H1 receptor antagonist activity
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The present work deals with the pharmacological screening of some newly synthesized triazoles. A series of 1,2,4-triazoles have been synthesized using benzoic acid or 4-chloro benzoic acid as the starting materials. The synthesized compounds were characterized by physical and spectral analysis viz., Fourier transform infrared spectroscopy, 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, Gas Chromatography-Mass Spectrometry and elemental analysis Carbon, Hydrogen and Nitrogen analysis in order to confirm the structure. Acute toxicity studies were carried out in accordance with the Organization for Economic Co-operation and Development guideline 425. The compounds were not found to be lethal even at a dose level of 2000 mg/kg. Pharmacological evaluation was done following three intact animal experiments and one experiment on the isolated tissue. Results of the study indicated that the compound 7bi and 7bj protected up to 60% against histamine-induced dyspnea. Antihistaminic nature of the test compounds 7bi, 7bj, 7ai, and 7bk were also confirmed by the loss of catalepsy after the administration of clonidine (1%, s.c.). During experiments on isolated tissue, suppression of dose-response curve of histamine indicates a noteworthy denouement in favor of the said effect.
KeywordsTriazoles Amines Antihistaminic H1 antagonist
The authors are thankful to the GLA University administration for providing research facilities for the present work. The authors wish to thank SAIF-CIL Panjab University, Chandigarh for spectral studies.
Compliance with ethical standards
Conflict of interest
The authors declare that they have no competing interests.
- Asif M (2014) A mini review on antimalarial activities of biologically active substituted triazoles derivatives. Int J Adv Res Chem Sci 1:22–28Google Scholar
- Bekircan O, Kahveci B, Kucuk M (2006) Synthesis and anticancer evaluation of some new unsymmetrical 3,5-diaryl-4H-1,2,4-triazole derivatives. Turk J Chem 30:29–40Google Scholar
- DeRuiter J (2001) Histamine H1-receptor antagonists: antihistaminic agents. Princ Drug Action 2:1–20Google Scholar
- Ghochikyan TV, Samvelyan MA, Galstyan AS, Grigoryan SV (2016) Synthesis of some s-derivatives of 1,2,4-triazoles. Chem Biol 2:8–12Google Scholar
- Godhani DR, Jogel AA, Sanghani AM, Mehta JP (2015) Synthesis and biological screening of 1,2,4-triazole derivatives. Indian J Chem 54B:556–564Google Scholar
- Hou YP, Sun J, Pang ZH, Lv PC, Li DD, Yan L, Zhang HJ, Zheng EX, Zhao J, Zhu HL (2011) Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors. Bioorg Med Chem 19:5948–5954CrossRefPubMedGoogle Scholar
- Jadhav S, Rai M, Durrani A, Bembalkar SR (2010) Synthesis and characterization of substituted 1,2,4-triazole and its derivatives. Asian J Chem 26:725–728Google Scholar
- Pattan S, Gadhave P, Tambe V, Dengale S, Thakur D, Hiremath SV, Shete RV, Deotarse P (2012) Synthesis and evaluation of some novel 1,2,4-triazole derivatives for antimicrobial, antitubercular and anti-inflammatory activities. Indian J Chem 51B:297–301Google Scholar
- Romagnoli R, Baraldi PG, Lopez OC, Cara CL, Carrion MD, Brancale A, Hamel E, Chen L, Bortolozzi R, Basso G, Viola G (2010) Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues. J Med Chem 53:4248–4258CrossRefPubMedPubMedCentralGoogle Scholar
- Shaker RM (2006) The chemistry of mercapto- and thione- substituted 1,2,4-triazoles and their utility in heterocyclic synthesis. Arkivoc 9:59–112Google Scholar
- Upmanyu N, Kumar S, Kharya MD, Shah K, Mishra P (2011c) Synthesis and anti-microbial evaluation of some novel 1,2,4-triazole derivatives. Acta Pol Pharm – Drug Res 68:213–221Google Scholar
- Zamani K, Faghihi K (2003) Synthesis of some new substituted 1,2,4-triazole and 1,3,4-thiadiazole and their derivatives. Turk J Chem 27:119–125Google Scholar