EDEMA REDUCING PROSPECTIVE OF MURRAYANINE BASED CHALCONE COMPOUND AS EMERGING NSAID AGENT
Abstract
In this study substituted murrayanine based chalcone compound (E)-3-(5-chloro-2-hydroxy-4-methylphenyl)-1-(1-methoxy-9H-carbazol-3-yl)prop-2-en-1-one has been synthesized by conventional method and screened for in vivo anti-inflammatory activity in Swiss albino rats employing the carrageenan-induced paw edema method. The synthesized compound was characterized by spectroscopic techniques (FT-IR; 1H-NMR; and Mass) and elemental analyses. The compound displayed % edema reduction of 24.91%, 34.49%, and 51.31%, respectively in the carrageenan-induced paw edema method over the 3 hrs duration. The molecule presented a fairly significant activity owing to inhibition of the inflammatory mediators like cyclooxygenase-1/2 (COX-1/2) and lipoxygenase (LOX) through the various electron-donating and electron-withdrawing substituents present in the B-ring of the chalcone scaffold. The activity was not analogous with that of the standard drug indomethacin which exhibited 74.59% in the third hr which indicated that still much improvement is needed for the development of better anti-inflammatory candidates. The study will undoubtedly motivate the researchers working on pharmacologically active low-molecular-weight ligands in the better and rational development of the molecules.References
Joseph TM, Mahapatra DK. 5-Lipoxygenase and Phospholipase A2 inhibitory potentials of alcoholic extract of Cyperus rotundus: In vitro and in silico study. Res Rev J Pharmacol 2018;8(2):1-5.
Mahapatra DK, Thote LT, Dhabarde DM. The emerging anti-inflammatory potentials of some novel Schiff’s base derivatives of 3,4-dioxymethylene acetophenone. J Appl Pharm Sci Res 2018;1(3):1-4.
Mahapatra DK, Dadure KM, Haldar AGM. Exploring the anti-inflammatory potentials of N-((5-(((1,3-dioxoisoindolin-2-yl)methyl)amino)-1,3,4-thiadiazol-2-yl)methyl)benzamide. Drug Discov 2018;12:42-45.
Joseph TM, Sharanya CS, Mahapatra DK, Suresh KI, Sabu A, Haridas M. In vitro Assessment of Selected Benzoic Acid Derivatives as Anti-inflammatory Compounds. J Sci Indus Res 2018;77(6):330-336.
Shivhare RS, Mahapatra DK, Nair RR, Deshmukh SN. Schiff’s base derivatives of murrayanine demonstrated enhanced anti-oxidant activity than its parent moiety. Indian J Pharm Edu Res 2016;50(4):9-15.
Mahapatra DK, Bharti SK. Drug Design. New Delhi: Tara Publications Private Limited, 2016.
Mahapatra DK, Ugale VG, Shivhare RS. Murrayanine-1,3,4-Oxadiazole-Uracil Hybrid: The Emerging Anti-inflammatory Candidate. Int J Pharm Sci Res 2018;9(8):99-102.
Mahapatra DK, Shivhare RS, Ugale VG. Anti-inflammatory potentials of some novel Murrayanine containing 1,3,4-Oxadiazole derivatives. Asian J Pharm Technol 2018;8(1):47-51.
Mahapatra DK, Shivhare RS. 3′,4′-Methylenedioxy Moiety Containing Murrayanine Based Chalcone as Emerging Anti-inflammatory Agent. J Mod Chem Chem Technol 2018;9(1):12-16.
Mahapatra DK, Dadure KM, Shivhare RS. Edema Reducing Potentials of Some Emerging Schiff’s bases of Murrayanine. MOJ Bioorg Org Chem 2018;2(4):172-175.
Mahapatra DK, Dadure KM, Shivhare RS. Murrayanine-1,3,4-Thiadiazole-Uracil Hybrid as Emerging Anti-inflammatory Candidate. Madridge J Novel Drug Res 2018;2(1):75-78.
Mahapatra DK, Shivhare RS, Haldar AGM. Novel Schiff’s base containing Murrayanine–1,3,4-Thiadiazole Hybrids as potential anti-inflammatory agents. Asian J Chem Pharm Sci 2017;2(2):10-15.
Mahapatra DK, Dadure KM, Shivhare RS. Exploring the Site-Specific Influence of Hydroxyl group in Ring-B of Murrayanine-Chalcone on Edema Reducing Potential. MOJ Drug Design Devel Ther 2018;2(4):191-194.
Mahapatra DK, Shivhare RS, Kumar P. Murrayanine-chalcone transformed into novel pyrimidine compounds demonstrated promising anti-inflammatory activity. Asian J Pharm Res 2018;8(1):6-10.
Mahapatra DK, Bharti SK, Asati V. Anti-cancer Chalcones: Structural and molecular targets perspectives. Eur J Med Chem 2015;98:69-114.
Mahapatra DK, Bharti SK, Asati V. Chalcone scaffolds as anti-infective agents: Structural and molecular target perspectives. Eur J Med Chem 2015;101:496-524.
Mahapatra DK, Asati V, Bharti SK. Chalcones and their role in management of diabetes mellitus: Structural and pharmacological perspectives. Eur J Med Chem 2015;92:839-865.
Mahapatra DK, Bharti SK. Therapeutic Potential of chalcones as cardiovascular agents. Life Sci 2016;148:154-172.
Mahapatra DK, Bharti SK, Asati V. Chalcone Derivatives: Anti-inflammatory Potential and Molecular Targets Perspectives. Curr Top Med Chem 2017;17(28):3146-69.
Mahapatra DK, Shivhare RS. Anti-microbial Perspective of a Chalcone, (E)-1-(1-methoxy-9H-carbazol-3-yl)-3-(4-(methylsulfonyl)phenyl)prop-2-en-1-one: Fabrication of a Hybrid by Unification of a Natural Product with a Synthetic Component. Int J Agr Life Sci 2018;4(2):236-240.
Kanhed AA, Mehere AP, Pandey KR, Mahapatra DK. 4-(2-chloroacetamido) Benzoic Acid Derivatives as Local Anesthetic Agents: Design, Synthesis, and Characterization. UK J Pharm Biosci 2016;4(6):35-44.
Amdare MD, Jogdand KR, Kathane LL, Kuhite NG, Padole CD, Mahapatra DK. Synthesis of a potential anti-inflammatory pyrazole derivative from hippuric acid as the starting material. J Pharm Chem Biol Sci 2017;5(3):216-220.