Pyrazole: A potent drug candidate with various Pharmacological activities

Authors

  • Anandi Kapri I.T.S College of Pharmacy, Ghaziabad, Muradnagar, India
  • Garima Raj I.T.S College of Pharmacy, Ghaziabad, Muradnagar, India
  • Nitin Gupta Mankind Research Centre, Gurgaon, India

DOI:

https://doi.org/10.21276/IJRDPL.2278-0238.2018.7(2).2941-2948

Keywords:

Pyrazole, Heterocyclic and Biological activity

Abstract

Aromatic organic heterocycle containing pyrimidine scaffolds. Pyrazole possess, a five-membered hetero aromatic ring with two nitrogen atoms. Presence of this nucleus in these Pyrazole skeletons comprise various ranges of pharmacological activities viz. analgesic, antipyretic, anticancer, antiviral, anti-Inflammatory, antioxidants, antimicrobial, anti-diabetic, anticonvulsant &antiarrhythmic. Pyrazole is a multipurpose lead compound which is developed by chemical architecture for effective molecules which are mostly biologically active. Several synthetic routes are accorded for the development of pyrazole containing reactions to afford a novel molecule.

Downloads

Download data is not yet available.

References

Gupta V, Kumar M,Gupta RR. heterocyclic chemistry springer-verlag berlin Heidelberg 1stIndian reprintvol 1: 1-2.

Barsoum FF, Girgis AS. Facile synthesis of bis(4,5-dihydro-1H-pyrazole-1-carboxamides) and theirthio-analogues of potential PGE2 inhibitory properties Eur J Med Chem2009; 44:2172-2177.

Delaunay T, Genix P, Es-Sayed M, Vors J, Monteiro N, Balme GA. Modular Sydnone Cycloaddition/ Suzuki-Miyaur Cross-Coupling Strategy to Unsymmetrical 3,5-Bis(hetero)aromatic Pyrazoles organic latter2010; 12: 3328-3331.

Shoman ME, Abdel-Aziz M, Aly OM, Farag HH, Morsy MA. Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives Eur J Med Chem2009; 44: 3068-3076.

Balsamo A, Coletta I, Guglielmotti A, Landolfi C, Mancini F, Martinelli A, Milanese C, Minutolo F, Nencetti S, Orlandini E, Pinza M, Rapposelli S, Rossello A.Synthesis of heteroaromatic analogues of (2-aryl-1-cyclopentenyl-1- alkylidene)-(arylmethyloxy)amine COX-2 inhibitors: effects on the inhibitory activity of the replacement of the cyclopentene central core with pyrazole, thiophene or isoxazole ring Eur J Med Chem2003; 38:157-1684.

Chandra T, Garg N, Lata S, Saxena K K, Kumar A (2010). Synthesis of substituted acridinyl pyrazoline derivatives and their evaluation for anti-inflammatory activity Eur J Med Chem 45: 1772-17765.

Lv P, Li H, Sun J, Zhou Y, Zhu H. Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents Bioorg Med Chem2010; 18: 4606-46146.

Dai H, Li Y, Du D, Qin X, Zhang X,Yu H, Fang J. Synthesis and Biological Activities of Novel Pyrazole Oxime Derivatives Containing a 2-Chloro-5-thiazolyl Moiety J Agric Food Chem200; 856: 10805-108107.

Ju Y, Varma RS. Aqueous N-Heterocyclization of Primary Amines and Hydrazines with Dihalides: Microwave-Assisted SynthesIs of N-Azacycloalkanes, Isoindole, Pyrazole, Pyrazolidine, and Phthalazine Derivatives J Org Chem2; 00671: 135-141.

Bartroli J, Turmo E, Alguero´M, Boncompte E, Vericat ML, Conte L, Ramis J, Merlos M, Garcia-Rafanell J, Forn J. New Azole Antifungals. 2 Synthesis and Antifungal Activity of Heterocyclecarboxamide Derivatives of 3-Amino-2-aryl-1-azolyl-2-butanol J Med. Chem1998; 41: 1855-1868.

Bekhit AA, Ashour HMA, Abdel Ghany YS, Bekhit ADA, Baraka A. Synthesis and biological evaluation of some thiazolyl and thiadiazolylderivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents. Eur J Med Chem2008; 43: 456-463.

Hall A, Billinton A, Brown SH, Clayton NM, Chowdhury A, Giblin GMP, Goldsmith P, Hayhow T G, Hurst D N, Kilford I R, Naylor A, Passingham Ba and Winyard L. Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy Bioorg Med Chem Lett2008; 18: 3392-3399.

Bandgar B P, Totre J V, Gawande S S, Khobragade C N, Warangkar S C, Kadam P D (2010). Synthesis of novel 3,5-diaryl pyrazole derivatives using combinatorial chemistry as inhibitors of tyrosinase as well as potent anticancer, anti-inflammatory agents Bioorg Med Chem 18: 6149-6155.

Burguete A, PontikE, Hadjipavlou-LitinaD, Villar R, Vicente E, SolanoB, Ancizu S, Perez-Silanes S, Aldana I, and Monge A. Synthesis and anti-inflammatory/antioxidant activities of some new ring substituted 3-phenyl-1-(1,4-di-N-oxidequinoxalin-2-yl)-2-propen-1-one derivatives and of their4,5-dihydro-(1H)-pyrazole analogues Bioorganic & Medicinal Chemistry Letters2007; 17: 6439-6443.

Abdel-Hafez EMN, Abuo-Rahma GEAA, Abdel-Aziz M, Radwan M F, Hassan H Farag. Design, synthesis and biological investigation of certain pyrazole-3-carboxylicacid derivatives as novel carriers for nitric oxide Bioorganic & Medicinal Chemistry2009; 17: 3829-3837.

Bekhit AA, Fahmy HTY, Rostom SAF, Bekhit AE-DA. Synthesis and Biological Evaluation of Some Thiazolylpyrazole Derivatives as Dual Anti-inflammatory Antimicrobial Agents Eur J Med Chem2010; xx: xx

Milano J, Rossato MF, Oliveira SM, Drewes C, Machado P, Beck P, Zanatta N,Martins M P, Mello CF, Rubin MA, Ferreira J, BonacorsoHelio G. Antinociceptive action of 4-methyl-5-trifluoromethyl-5-hydroxy-4, 5-dihydro-1H-pyrazole methyl ester in models of inflammatory pain in mice Life Sciences2008; 83: 739-746.

Gokhan-KelekciN, YabanogluS, KupeliE, Salg?n U, Ozgen O, Ucar G, Yesilada E, Kendi E, Yesiladaf A, and Bilgina AA. A new therapeutic approach in Alzheimer disease: Some novel pyrazole derivatives as dual MAO-B inhibitors and anti-inflammatory analgesics Bioorg Med Chem2007; 15: 5775-5786.

Barsoum FF, Girgis AS. Facile synthesis of bis (4, 5-dihydro-1H-pyrazole-1-arboxamides) and their thio-analogues of potential PGE2 inhibitory properties Eur J Med Chem2009; 44: 2172-2177.

Chandra T, Garg N, Lata S, Saxena KK, Kumar A. Synthesis of substituted acridinylpyrazoline derivatives and their evaluation for anti-inflammatory activity EurJ MedChem2010; 45: 1772-1776.

Christodoulou M S, LiekensS, Kasiotis K M, Haroutounian SA. Novel pyrazole derivatives: Synthesis and evaluation of anti-angiogenic activity Bioorg Med Chem2010; 18: 4338-4350.

Xia Y, Dong Z-W, Zhao B-X, Ge X, Meng Ning, Shinc D-S, and Miao J-Y. Synthesis and structure-activity relationships of novel 1-arylmethyl-3-aryl-1H-pyrazole-5-carbohydrazide derivatives as potential agents against A549 lung cancer cells Bioorg Med Chem2007; 15: 6893-6899.

Zheng L, Wub L, Zhao B, Dong W, Miao J. Synthesis of novel substituted pyrazole-5-carbohydrazide hydrazine derivatives and discovery of a potent apoptosis inducer in A549 lung cancer cells Bioorg Med Chem2009; 17: 1957 1962.

Insuasty Braulio, Tigreros A, Orozco F, Quiroga J, Abonia R, Nogueras M, Sanchez A,Cobo J Synthesis of novel pyrazolic analogues of chalcones and their 3-aryl-4-(3-aryl-4, 5-dihydro-1H-pyrazol-5-yl)-1-phenyl-1H-pyrazol derivatives as potential antitumor agents.Bioorg Med Chem201018: 4965-4974.

Bonesi M, Loizzo M R, St; atti G A, Michel S, Tillequin F, Menichini F. The synthesis and Angiotensin Converting Enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives Bioorganic& Medicinal Chemistry Letters201020: 1990-1993.;

Lv P, Li H, Sun J, Zhou Y, Zhu H-L. Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents Bioorganic & Medicinal Chemistry 2010; 18: 4606-4614.

Bruno O, Brullo C, Bondavalli F, Schenone S, Spisani S, Falzarano MS, Varani K, Barocelli E, Ballabeni V, Giorgio C, Tognolini M. 1-Methyl and 1-(2-hydroxyalkyl)-5-(3- 1H-pyrazole-4-carboxylic acid ethyl esters as potent human neutrophil chemotaxis inhibitors Bioorg Med Chem2009; 17: 3379-3387.

Niculescu-Duvaz D, Niculescu-Duvaz I, Suijkerbuijk B M J M, Ménard D, Zambon A, Nourry A, Davies L, Manne H A, Friedlos F, Ogilvie L, Hedley D, Takle A K, Wilson D M, Pons J-F, Coulter T, Kirk R, Cantarino N, Whittaker S, Marais R, Springer C J. Novel tricyclic pyrazole BRAF inhibitors with imidazole or furancentral scaffolds Bioorg Med Chem2010; 18: 6934-6952.

Abdel-Aziz M, Abuo-RahmaG E-D A, Hassan A A. Synthesis of novel pyrazole derivativesand evaluation of their antidepressantand anticonvulsant activities Eur J Med Chem2009; 44: 3480-3487.

Gok S, Demet M, O¨zdemirA, Turan-Zitouni G. Evaluation of antidepressant-like effect of 2-pyrazoline derivatives Med Chem Res2010; 19: 94-101.

Can ÖD, Özkay ÜD, Kaplanclkl ZA, Öztürk Y. Effects of Some 1,3,5 Trisubstitued-2-pyrazoline Derivatives on depression and anxiety parameters of mice, Arch Pharm Res 200932: 1293-1299.

Published

2018-04-15

How to Cite

Kapri, A. ., Raj, G. ., & Gupta, N. . (2018). Pyrazole: A potent drug candidate with various Pharmacological activities. International Journal of Research and Development in Pharmacy & Life Sciences, 7(2), 2941 - 2948. https://doi.org/10.21276/IJRDPL.2278-0238.2018.7(2).2941-2948