In-vitro inhibition studies on endogenous proteolysis of liver homogenate in presence of synthesized pyrazoles

International Journal of Pharmacy and Pharmaceutical Sciences

Volumn 5, Issue SUPPL 3, 2013, Pages 365-368

  Singh, Mamta ^a   Raghav, Neera ^a  

^a KURUKSHETRA UNIVERSITY   (India)

Author keywords

Cysteine proteases; Endogenous proteolysis; Inhibition studies; Substituted pyrazoles

Indexed keywords

1, 3, 5-TRIPHENYL PYRAZOLINE; 5 (4' BROMOPHENYL) 1,3 DIPHENYL 2 PYRAZOLE; 5 (4' CHLOROPHENYL) 1,3 DIPHENYL 2 PYRAZOLE; 5 (4' FLUOROPHENYL) 1,3 DIPHENYL 2 PYRAZOLE; 5 (4' METHOXY PHENYL) 1,3 DIPHENYL 2 PYRAZOLE; 5 (4' METHYLPHENYL) 1,3 DIPHENYL 2 PYRAZOLE; 5 (4' NITROPHENYL) 1,3 DIPHENYL 2 PYRAZOLE; CHALCONE DERIVATIVE; HYDRAZINE DERIVATIVE; PYRAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG STRUCTURE; DRUG SYNTHESIS; INFRARED SPECTROMETRY; LIVER HOMOGENATE; NONHUMAN; OXIDATION; PROTEIN ANALYSIS; PROTEIN DEGRADATION;

EID: 84882760826     PISSN: None     EISSN: 09751491     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. Sahu PK, Sahu PK, Gupta SK, Thavaselvamd D, Agarwal DD. Synthesis and evaluation of antimicrobial activity of 4H-pyrimido[2, 1-b] benzothiazole, pyrazole and benzylidene derivatives of curcumin, Eur J of Med Chem. 2012; 54: 366-378.
2. Menozzi G, Mosti L, Schenone P, Donnoli D, Schiariti F, Marmo E. 1-phenyl-1H-pyrazole derivatives with antiinflammatory, analgesic and antipiretic activities. Farmaco. 1990; 45(2): 167-86.
3. Abd-El Gawad NM, Hassan GS, Georgey HH. Design and synthesis of some pyrazole derivatives of expected anti-inflammatory and analgesic activities. Med Chem Res. 2012; 21: 983-994.
4. Prabhu VV, Kuruvilla CA, Guruvayoorappan C. Potentiating effect of 1, 2-diazole a plant alkaloid on carrageenan and formalin induced paw edema in experimental mice. Int J Pharm Pharm Sci. 2012; 4(3): 380-383.
5. Kees KL, Fitzgerald JJ Jr, Steiner KE, Mattes JF, Mihan B, Tosi T, Mondoro D, McCaleb ML. New potent antihyperglycemic agents in db/db mice: synthesis and structure-activity relationship studies of (4-substituted benzyl) (trifluoromethyl)pyrazoles and-pyrazolones. J Med Chem. 1996; 39(20): 3920-3928.
6. Aly HM, El-Gazzar MG. Novel pyrazole derivatives as anticancer and radiosensitizing agents. Arzneimittelforschung. 2012; 62(3): 105-12.
7. Musad EA, Mohamed R, Saeed BA, Vishwanath BS, Rai KML. Synthesis and evaluation of antioxidant and antibacterial activities of new substituted bis(1, 3, 4-oxadiazoles), 3, 5-bis(substituted) pyrazoles and isoxazoles Bio & Med Chem Letters. 2011; 21: 3536-3540.
8. Ahasan NB, Islam MR. Cytotoxicity study of pyrazole derivatives. Bangladesh J Pharmacol. 2007; 2: 81-87.
9. Abdel-Aziz M, Abuo-Rahma GA, Hassan AA. Synthesis of novel pyrazole derivatives and evaluation of their antidepressant and anticonvulsant activities. Eur. J. Med. Chem. 2009; 44: 3480-3487.
10. Insuasty B, Tigreros A, Orozco F, Quiroga J, Abonia R, Nogueras M et al. Synthesis of novel pyrazolic analogues of chalcones and their 3-aryl-4-(3-aryl-4, 5-dihydro-1H-pyrazol-5-yl)-1-phenyl-1H-pyrazole derivatives as potential antitumor agents. Bioorg & Med Chem. 2010; 18: 4965-4974.
11. Faidallah HM, Khan K, Asiri AM. Synthesis and biological evaluation of new3-trifluoromethylpyrazolesulfonyl-urea and thiourea derivatives as antidiabetic and antimicrobial agentsJournal of Fluorine Chemistry. 2011; 132: 131-137.
12. Kumar S, Kumar G, Kapoor M, Surolia A. Synthesis and Evaluation of Substituted Pyrazoles: Potential Antimalarials Targeting the Enoyl-ACP Reductase of Plasmodium Falciparum. Synthetic Commun. 2006; 36: 215-226.
13. Sung HH, Wagner KM, Morisseau C, Liu JY, Dong H, Wecksler AT et al. Synthesis and StructureActivity Relationship Studies ofUrea-Containing Pyrazoles as Dual Inhibitors of Cyclooxygenase-2 and Soluble Epoxide Hydrolase. J. Med. Chem. 2011; 54(8): 3037-3050.
14. Szabo G, Varga B, Payer-Lengyel D, Szemzo A, Erdelyi P, Vukics K et al. Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists. J. Med. Chem. 2009; 52: 4329.
15. Yamamoto S, Tomita N, Suzuki Y, Suzaki T, Kaku T, Hara T et al. Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists Bioorg Med Chem. 2012; 20(7): 2338-2352.
16. Newhouse B., Hansen JD, Grina J, Welch M, Topalov G, Littman N et al. Non-oxime pyrazole based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2011; 21(11): 3488-3492.
17. Kantevari S, Addla D, Bagul PK, Sridhar B, Banerjee SK. Synthesis and evaluation of novel 2-butyl-4-chloro-1-methylimidazole embedded chalcones and pyrazoles as angiotensin converting enzyme (ACE) inhibitors. Bioorg & Med Chem. 2011; 19: 4772-4781.
18. Gorja DR, Kumar KS, Kandale A, Meda CLT, Parsa KVL, Mukkanti K. Design and synthesis of 4-alkynyl pyrazoles as inhibitors of PDE4: A practical access via Pd/C-Cu catalysis. Bio & Med Chem. Lett. 2012; 22: 2480-2487.
19. Xiaocong MY, Andrei WK, Minghua S, Shendong Y, Danielle L A, Michael D et al Discovery of a novel [3. 2. 1] benzo fused bicyclic sulfonamidepyrazoles as potent, selective and efficacious γ-secretase inhibitors. Bioorg & Med Chem Lett. 2013; 23: 996-1000.
20. Nepali K, Singh G, Turan A, Agarwal A, Sapra S, Kumar R. A rational approach for the design and synthesis of 1-acetyl-3, 5-diaryl-4, 5-dihydro(1H)pyrazoles as a new class of potential non-purine xanthine oxidase inhibitors. Bioorg & Med Chem. 2011; 19: 1950-1958.
21. Gomez L, Hack MD, Wu J, Wiener JJ, Venkatesan H, Santillán A Jr et al. Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: synthesis and preliminary SAR analysis. Bioorg Med Chem Lett. 2007; 17(10): 2723-2727.
22. Wiener JJ, Wickboldt AT Jr, Wiener DK, Lee-Dutra A, Edwards JP, Karlsson L et al. Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions. Bioorg Med Chem Lett. 2010; 20(7): 2375-2378.
23. Chimenti F, Bolasco A, Manna F, Secci D, Chimenti P, Befani O et al. Synthesis and Selective Inhibitory Activity of 1-Acetyl-3, 5-diphenyl-4, 5-dihydro-(1H)-pyrazole Derivatives against Monoamine Oxidase. J Med Chem. 2004; 47: 2071-207.
24. Barrett AJ, Rawlings ND, Woessner JF. The Handbook of Proteolytic Enzymes, 2nd ed. Academic Press 2003.
25. Singh M, Raghav N. In-Vitro inhibition Studies on Endogenous proteolysis of Liver Homogenate in Presence of Synthesized Pyrazolines. Int J Pharm Pharm Sci. 2013; 5(1): 80-86.
26. Bradford MM. A rapid and sensitive method for the quantitation of microgram quantities of proteins utilizing the principle of protein-dye binding. Anal. Biochem. 1976; 72: 248-254
27. Stoschek CM. Quantitation of Protein. Methods Enzymol. 1990; 182: 50-68.
28. Chapman HA, Riese RJ, Shi GP. Emerging roles for cysteine proteases in human biology. Annu Rev Physiol 1997; 59: 63-88.
29. Rzychon M, Chimiel D, Stec-Niemczyk J. Modes of inhibition of cysteine proteases. Acta Biochim Polonica. 2004; 51(4): 861-873.
30. Otto H H, Schirmeister T. Cysteine proteases and their inhibitors. Chem Rev 1997; 97: 133-171.
31. Janoff A, Carp. H. Proteases, antiproteases, and oxidants: pathways of tissue injury during inflammation. Monogr Pathol. 1982; 23: 62-82.
32. Baricos W H, Shah S V. Proteolytic enzymes as mediators of glomerular injury. Kidney Int. 1991; 40: 161-173.
33. Chung S, Kawai K. Protease activities in gastric cancer tissues. Clin Chim Acta. 1990; 189: 205-210.
34. Katunuma N, Kominami E. Abnormal expression of lysosomal cysteine proteinases in muscle wasting diseses. Rev Physiol Biochem Pharmacol 1987; 108: 1-20.
35. Kos J, Werle B, Lah T, Brunner N. Cysteine proteinases and their inhibitors in extracellular fluids: markers for diagnosis and prognosis in cancer. Int J Biol Markers 2000; 15: 84-89.
36. Frohlich E. Proteases in cutaneous malignant melanoma: relevance as biomarker and therapeutic target. Cell Mol Life Sci. 2010; 67: 3947.
37. Raghav N, Kaur R, Singh M, Suman, Priyanka. Effect of semicarbazones on endogenous protein hydrolysis in liver homogenate. Asian J Chem 2010; 22(9): 7097-7101.
38. Kaur R, Singh M, Jangra S, Raghav N. Proteolytic Studies in Liver Homogenate in Presence of Substituted Thiosemicarbazones. Int J chem Sci. 2012; 10(3): 1698-1704.
39. Raghav N, Singh M, Kaur R, Suman, Priyanka. Proteolytic Studies in Liver Homogenate in Presence of Substituted Aryl Hydrazones. Asian J Chem. 2011; 23(3): 1409-1410.
40. Raghav N, Singh M, Kaur R, Suman, Priyanka. Proteolytic studies in liver homogenate in presence of phenylhydrazone. Int J Pharm Tech. 2010; 2(3): 743-749.