Synthesis and pharmacokinetic study of new thiazole derivatives containing pyrazole moiety

• Authors: Dipti L. Namera , Umed C. Bhoya , Anamik K. Shah
• Languages of publication: EN

Abstracts

EN

For developed new eco-friendly synthetic route for the synthesis of organic compounds, here in, we have synthesized new series of thiazole derivatives 7(a-h) under microwave irradiation method using less amount of methanol as solvent and less hazardous K2CO3 as catalyst. Then after for the pharmacokinetic study, we can calculate Lipinski rules of five data using swiss ADME software, molecule 7f was fitted in ‘rules of five’ (Ro5) other compounds are showed violence in log P(o/w). The structures of all synthesized compounds are well characterized by Mass, 1H NMR, 13C NMR.

Keywords

EN

Microwave irradiation; Pharmacokinetic; Pyrazole; Thiazole; eco-friendly

Discipline

• CHEMISTRY: CHEMISTRY

• Publisher: Scientific Publishing House „DARWIN”
• Journal: World Scientific News
• Year: 2019
• Volume: 132
• Pages: 277-284

Contributors

author

Dipti L. Namera

• National Facility for Drug Discovery Centre, Department of Chemistry, Saurashtra University, Rajkot - 360005, Gujarat, India

author

Umed C. Bhoya

• National Facility for Drug Discovery Centre, Department of Chemistry, Saurashtra University, Rajkot - 360005, Gujarat, India

author

Anamik K. Shah

• National Facility for Drug Discovery Centre, Department of Chemistry, Saurashtra University, Rajkot - 360005, Gujarat, India

References

• [1] Borisenko, V. E.; Koll, A; Kolmakov, E. E.; Rjasnyi, A. G. J. Mol. Struct. 2006, 101
• [2] (a) Bhargava, P.N.; Lakhan, R.; Tripathi, K., J. Ind. Chem. Soc. 1982, 59, 773
• (b) Maulard, T.; Lagorce, J. F.; Thomos, J. C.; Raby, C.; J. Pharm. Pharmacol. 1993, 731.
• [3] Milne, G. W. A.; Handbook of Antineoplastic Agents, Gower; Ashgate, Ed., London, UK, 2000.
• [4] Maj, J.; Rog, Z.; Skuza, G.; Kolodziejezyk, K.; J. Neural. Transm. 1997, 525
• [5] De Souza, M. V. N.; De Almeida, M. V., Quim. Nova. 2003, 366
• [6] Markus, B.; Salome von, G.; Christoph, B.; Werner, J. P., Curr. Drug. Tar., 2004, 1
• [7] Knadler, M. P.; Bergstrom, R. F.; Callaghan, J. T; Rubin, A.; Drug Metab. Dispos. 1986, 175
• [8] Breslow, R., J. Am. Chem. Soc. 1958, 3719
• [9] (a) Alamino, R. J.; U. S. Patent, 1977, 4012409
• (b) Bhargava, P. N.; Lakhan, R.; Tripathi, K; J. Ind. Chem. Soc., 1982, 59, 773
• (c) Maulard, T, Lagorce, J. F. Thomos, J. C; Raby, C.; J. Pharm. Pharmacol., 1993, 45, 731
• (d) Tsuruoka, A.; Kaku, Y. Y.; Kakinumato, H.; Tsukada, I.; Yanagishawa, M.; Naito, T.; J. Chem. Pharm. Bull. 1997, 45, 1169
• [10] Badaweya; Sayed, A.M.; Ashmawey; Ibrahim, M., J. Med. Chem 33, 1998, 349-361
• [11] Mohamed, A. A.; Gamal, E. A.; Abuo-Rahmaa, Hassan, A. A., Eur. J. Med. Chem. 2009, 44, 3480
• [12] Derelanko, M.J.; Hollinger, M.A.; 2002. Acute, subacute and chronic toxicology. Hand Book of Toxicology, second ed. CRC Press, New York, 69.
• [13] Vera, L.M.; Silvaa, J.; Elguerob Artur, M.S.; Silvaa, Eur. J. Med. Chem. 2018, 156, 394.
• [14] Pratap Kumar Patra, Chniranjan Patra, Subasini Pattnaik; International Journal of Pharmacy and Pharmaceutical Sciences, 2014, 6, 1.
• [15] Al-Ghamdi, H.M., Oriental journal of chemistry 2019, 35, 391
• [16] Dipankar Bardalai; Panneerselvam, P., Int. Res J Pharm. App Sci. 2012; 2,1
• [17] Hantzsch, A. R.; Weber, H. J.; Berichte, 1887, 20, 3118; 21, 938; Ann. Chem. 1888, 249, 1, 27.
• [18] Ayinde, W. B.; Gitari & Amidou Samie, W. M.; Green Chemistry Letters and Reviews, 2019, 12, 225-234,
• [19] Kavadia, K.M.; Kapadiya, K. M.; Manvar, P.; Munshi, K.P.; Khunt, R.C., Chemistry & Biology Interface, 2014, 4, 111
• [20] Barsoum, F.F.; Girgis, A.S.; Eur. J. Med. Chem. 2009, 44, 2172

• Document Type: short_communication