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International Letters of Chemistry, Physics and Astronomy
ILCPA Volume 60

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Synthesis, Biological Evaluation and Docking Studies of some Novel (E)-(4-(2-(Benzo[d]Thiazol-2-yl)Hydrazono)Methyl-2,6-Diphenylpiperidin-1-yl)(Phenyl)Methanone Derivatives

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A series of biologically active some novel (E)-(4-(2-(benzo [d] thiazol-2-yl) hydrazono)-3-methyl-2,6-diphenylpiperidin-1-yl)(phenyl) methanone derivatives (14-19) were synthesized and characterized by IR, 1H NMR, 13C NMR and HSQC spectral analysis. Molecular docking studies were also carried out for compounds 14-19 using the crystal structure of Ribonucleotide Reductase to disclose the binding mode and orientation of target molecule into the active site of respective receptors. The synthesized compounds were also screened for their antimicrobial activity against selected panel strains Antimicrobial studies revealed that the synthesized compound 14 exhibited noticeable activity against B.cerus whereas compounds17 and 18 displayed appreciable activity against K.pneumoniae. Bromo substituted phenyl group at C-2 and C-6 of piperidine ring showed excellent antibacterial activity against K.pneumoniae and B.cerus at MIC of 25μg/ml. The antifungal studies revealed that compounds 17, 18 and 19 exposed significant antifungal activity against the pathogenic strains used in this study. In particular compound 19 are showed excellent antifungal activity against C.albicans and A.niger.


International Letters of Chemistry, Physics and Astronomy (Volume 60)
D. Rajaraman et al., "Synthesis, Biological Evaluation and Docking Studies of some Novel (E)-(4-(2-(Benzo[d]Thiazol-2-yl)Hydrazono)Methyl-2,6-Diphenylpiperidin-1-yl)(Phenyl)Methanone Derivatives", International Letters of Chemistry, Physics and Astronomy, Vol. 60, pp. 35-46, 2015
Online since:
September 2015

R. Jeyaraman, S. Avila, Chemistry of 3- azabicyclo[3. 3. 1] nonanes. Chem. Rev, 81 (1981) 149.

K. Narayanan, M. Shanmugam, S. Jothivel, S. Kabilan, 1-allyl substituted 2, 6- diphenylpiperidin-4-ones and derivatives of oximes/ oxime ethers. Bioorg. Med. Chem. Lett. 22 (2012) 6602-6607.

G. Aridoss, S. Balasubramanian, P. Parthiban, S. Kabilan, Synthesis, stereochemistry and antimicrobial evaluation of some N-morpholinoacetyl-2, 6-diarylpiperidon-4-ones. European J. Med. Chem. 42 (2007) 851-860.

R. V. Perumal, M. Adiraj, P. Shanmugapandiyan, Synthesis, analgesic and anti- inflammatory evaluation of substituted 4-piperidines. Indian Drugs. 38 (2001) 156-159.

H. I. El-Subbagh, S. M. Abu-Zaid, M. A. Mahran, F. A. Badria, A. M. Alofaid, Synthesis and biological evaluation of certain α, β unsaturated ketones and their corresponding fused pyridines as antiviral and cytotoxic agents. J Med. Chem. 43 (2000).

A. A. Watson, G. W. J. Fleet, N. Asano, R. J. Molyneux, Polyhydroxylated alkaloids-natural occurance and therapeutic application. Photochemistry. 56 (2001) 265.

N. Rameshkumar, A. Veena, R. Ilavarasan, M. Adiraj, P. Shanmugapandiyan, S. Sridhar, Synthesis of 6-fluoro-1, 4-dihydro-4-oxo-quinoline-3-carboxlic acid derivatives as potential antimicrobial agents. European. Med. Chem. 26 (2003) 188.

R. V. Perumal, M. Adiraj, P. Shanmugapandiyan, Synthesis, analgesic and anti- inflammatory evaluation of substituted 4-piperidines. Indian Drugs. 38 (2001) 156-159.

H. M. Eisa, A. S. Tantaway, M. M. El-Kerdawy, Synthesis of certain 2-aminoadamantane derivatives as potential antimicrobial agents. Pharmazie Mar, 46 (1991) 182-184.

A. Gursoy, N. Terzioglu, G. Otuk, synthesis of some new hydrazide-hydrazones. Eur J Med Chem. 32 (1997) 753-757.

S. Rollas, N. N. Gulerman, H. Erdeniz. Synthesis and antimicrobial activity of some new hydrazones of 4-fluorotenzoic acid hydrazide and 3-acetyl-2, 5-discubstituted-1, 3, 4 oxadiazolines. J Farmaco. 57 (2002) 171-174.

P. Vicini, F. Zani, P. Cozzini, I. Doytchinova, Hydrazones of 1, 2-benzisothiazole hydrazides: synthesis, antimicrobial activity and QSAR investigations. Eur J Med Chem. 37 (2002) 553564.

C. Sankar, K. Pandiyarajan, Synthesis and anti-tuberlar and antimicrobial activities of some 2r, 4c- diaryl-3-azabicyclo[3. 3. 1] nonan-9-one N-isonicoylhydrazone derivatives. Eur J Med Chem. 45 (2010) 5480-5485.

Neeraj Kumar.; Lalit Singh Chauhan.; Nipun Dashora.; Chandra Shekhar Sharma. Anticonvulant potential of Hydrazone derivatives: A Review. Sch. Acad. J. Pharm, 3 (2014) 366-373.

O. I. El-sabbagh, H. M. Rady, Synthesis of new acridines and hydrazones derived from cyclic β-diketone from cytotoxic and antiviral evaluation. Eur J Med Chem. 44 (2009) 3680-3686.

R. Kalsi, K. Pande, T. N. Bhalla, J. P. Bartwall G. P. Gupta, S.S. Parmar, Anti-inflammatory activity of quinazolinoformazans. J Pharm Sci. 79 (1990) 317-320.

W.H. Lewis, Ribonucleotide reductase from wild type and hydroxyurea-resistant chinese hamster ovary cells. Cell Physiol. 87 (1978) 97.

P. Reichard, From RNA to DNA, why so many ribonucleotide reductases. Science, 260 (1993) 1773-1777.

J. A. Wright, A. K. Chan, B. K. Choy, R. A. Hurta, G. A. McClarty, A. Y. Tagger, Regulation and drug resistance mechanisms of mammalian ribonucleotide reductase, and the significance to DNA synthesis. Biochem Cell Biol. 68 (1990) 1364-71.

H. Eklund, U. Uhlin, M. Farnegardh, D. T Logan. P. Nordlund, Structure and function of the radical enzyme ribonucleotide reductase. Prog Biophys Mol Biol. 77 (2001) 177-268.

J. M. Cocking, Gene for M1 subunit of ribonucleotide reductase is amplified in hydroxyurearesistant hamster cells. Somat cell mol Genet. 13 (1987) 221.

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