Synthesis and selective inhibitory activity against human COX-1 of novel 1-(4-substituted-thiazol-2-yl)-3,5-di(hetero)aryl-pyrazoline derivatives

Archiv der Pharmazie

Volumn 345, Issue 12, 2012, Pages 973-979

  Carradori, Simone ^a   Secci, Daniela ^a   Bolasco, Adriana ^a   De Monte, Celeste ^a   Yáñez, Matilde ^b  

^a SAPIENZA UNIVERSITY OF ROME   (Italy)

^b UNIVERSITY OF SANTIAGO DE COMPOSTELA   (Spain)

Author keywords

Cyclooxygenase; Microwave assisted synthesis; Pyrazoline; Selective hCOX 1 inhibitors; Thiazole

Indexed keywords

1 (4 SUBSTITUTED THIAZOL 2 YL) 3,5 DI(HETERO)ARYL PYRAZOLINE DERIVATIVE; CYCLOOXYGENASE 1 INHIBITOR; DICLOFENAC; INDOMETACIN; UNCLASSIFIED DRUG;

ANTIINFLAMMATORY ACTIVITY; ARTICLE; DRUG SYNTHESIS; HUMAN; IN VITRO STUDY; PRIORITY JOURNAL; SPECTROSCOPY;

BLOOD PLATELETS; CYCLOOXYGENASE 1; CYCLOOXYGENASE INHIBITORS; DRUG DISCOVERY; HUMANS; MICROSOMES; MOLECULAR STRUCTURE; PYRAZOLES; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

EID: 84870558988     PISSN: 03656233     EISSN: 15214184     Source Type: Journal    
DOI: 10.1002/ardp.201200249     Document Type: Article

References (17)

1. L. J. Marnett, Annu. Rev. Pharmacol. Toxicol. 2009, 49, 265-290.
2. Z. A. Radi, N. K. Khan, Exp. Toxicol. Pathol. 2006, 58, 163-173.
3. M. G. Perrone, A. Scilimati, L. Simone, P. Vitale, Curr. Med. Chem. 2010, 17, 3769-3805.
4. P. X. Franklin, A. D. Pillai, P. D. Rathod, S. Yerande, M. Nivsarkar, H. Padh, K. K. Vasu, V. Sudarsanam, Eur. J. Med. Chem. 2008, 43, 129-134.
5. M. V. R. Reddy, V. K. Billa, V. K. Pallela, M. R. Mallireddigari, R. Boominathan, J. L. Gabriel, E. P. Reddy, Bioorg. Med. Chem. 2008, 16, 3907-3916.
6. R. Fioravanti, A. Bolasco, F. Manna, F. Rossi, F. Orallo, F. Ortuso, S. Alcaro, R. Cirilli, Eur. J. Med. Chem. 2010, 45, 6135-6138.
7. M. A.-A. El-Sayed, N. I. Abdel-Aziz, A. A.-M. Abdel-Aziz, A. S. El-Azab, Y. A. Asiri, K. E. H. ElTahir, Bioorg. Med. Chem. 2011, 19, 3416-3424.
8. S. V. Bhandari, S. C. Dangre, K. G. Bothara, A. A. Patil, A. P. Sarkate, D. K. Lokwani, S. T. Gore, B. J. Deshmane, V. T. Raparti, C. V. Khachane, Eur. J. Med. Chem. 2009, 44, 4622-4636.
9. C. Cusan, G. Spalluto, M. Prato, M. Adams, A. Bodensieck, R. Bauer, A. Tubaro, P. Bernardi, T. Da Ros, Il Farmaco 2005, 60, 327-332.
10. G. Eren, S. Ünlü, M. T. Nuñez, L. Labeaga, F. Ledo, A. Entrena, E. Banoǧlu, G. Costantino, M. F. Şahin, Bioorg. Med. Chem. 2010, 18, 6367-6376.
11. A. A. Bekhit, H. T. Y. Fahmy, S. A. F. Rostom, A. E. A. Bekhit, Eur. J. Med. Chem. 2010, 45, 6027-6038.
12. D. Kakati, J. C. Sarma, Chem. Central J. 2011, 5, 8-13.
13. F. Chimenti, S. Carradori, D. Secci, A. Bolasco, B. Bizzarri, P. Chimenti, A. Granese, M. Yáñez, F. Orallo, Eur. J. Med. Chem. 2010, 45, 800-804.
14. S. Vilar, E. Quezada, L. Santana, E. Uriarte, M. Yáñez, N. Fraiz, C. Alcaide, E. Cano, F. Orallo, Bioorg. Med. Chem. Lett. 2006, 16, 257-261.
15. M. Yáñez, N. Fraiz, E. Cano, F. Orallo, Biochem. Biophys. Res. Commun. 2006, 344, 688-695.
16. M. M. Bradford, Anal. Biochem. 1976, 7, 248-254.
17. R. A. Copeland, J. M. Williams, J. Giannaras, S. Nurnberg, M. Covington, D. Pinto, S. Pick, J. M. Trzaskos, Proc. Natl. Acad. Sci. USA 1994, 91, 11202-11206.