Indian Journal of Chemistry: Sec B- Organic Chemistry including Medicinal Chemistry

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Published by: NISCAIR (CSIR)

Subjects: Chemistry

Indian Journal of Chemistry (Section B) is published by the National Institute of Science Communication and Information Resources (NISCAIR)-CSIR, New Delhi. This journal publishes articles in Organic and Medicinal Chemistry. It includes full length papers, notes and communications and short reviews. The monthly issues covers articles in organic reaction mechanism, theoretical organic chemistry, structure-activity relationships, medicinal chemistry, synthesis of chiral compounds, bio-organic chemistry, enzymes in organic synthesis, reagents in organic synthesis, heterocyclic compounds, phytochemistry (natural products), amino acids, peptides and proteins, spectroscopy in characterization of organic compounds, chemoenzymatic and enantioselective synthesis of organic compounds, synthesis of fullerenes, metal-catalyzed asymmetric reactions, bioactive plant products and combinatorial chemistry.

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Editor,
Dr. P Paravatharajan
email: prema@niscair.res.in


ISSN No. :    0376-4699
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Synthesis, characterization and antimicrobial activity of ethyl 2-(3-formyl-4-((4-hydroxy-2-oxo-2H-chromen-3-yl)-alkoxy-)phenyl)-4-methylthiazole-5-carboxylate derivatives
Title: Synthesis, characterization and antimicrobial activity of ethyl 2-(3-formyl-4-((4-hydroxy-2-oxo-2H-chromen-3-yl)-alkoxy-)phenyl)-4-methylthiazole-5-carboxylate derivatives

Authors: Malik, G M; Naik, Chirag G

Abstract: During the present study, a number of substituted thiazole derivatives have been synthesized by the reaction of 4-hydrox-ybezene-1-carbothiomide and ethyl-2-chloro acetoacetate to give ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate. The latter reacts with PPA, HMTA and acetic acid to yield ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate. These compounds further react with di-bromo alkane and 4-hydroxy coumarin to give the final thiazole derivatives. These are characterized by elemental analysis, IR and 1H NMR spectra, and have been screened for their antimicrobial activity and found to have significant effect against the tested microorganisms. Some of the synthesized thiazole derivatives are found to exhibit promising activity.

Page(s): 1005-1010

Synthesis and characterization of N-substituted 2-hydroxypyrrolidine/ piperidine derivatives using cerium chloride as catalyst
Title: Synthesis and characterization of N-substituted 2-hydroxypyrrolidine/ piperidine derivatives using cerium chloride as catalyst

Authors: Suresh, M; Khader, K K Abdul; Chandrasekaran, T; Padusha, M Syed Ali

Abstract: 2-Hydroxypyrrolidine/piperidine derivatives have gained great interest in synthetic organic research because of their wide range of biological activities. A series of pyrrolidine derivatives have been synthesized using heterocyclic amines 5a-h and 2,3-dihydro-furan 2a. Further, a series of piperidine derivatives have been synthesized using 5a-h and 3,4-dihydro-2H-pyran 2b. Both 2a and 2b react with 5a-h via C-N cross-coupling reaction and result in the products 6a-p. Acetonitrile and cerium chloride heptahydrate have been used as solvent and catalyst respectively. The chemical structures of the newly synthesized compounds have been elucidated by spectral analysis (viz., 1H and 13C NMR and mass spectra) and analytical techniques. In the present study various solvents and catalyst have been employed. Among them CeCl3.7H2O and acetonitrile are found to be effective in these transformations, which lead to complete conversion to the coupled products.

Page(s): 999-1004

Quinoline alkaloids – Synthesis, molecular docking studies of atanine, 2-isopropylfuro [2,3-b] quinolines and 3,4-dihydro-2,2-dimethyl-2H-pyrano [2,3-b]quinolines
Title: Quinoline alkaloids – Synthesis, molecular docking studies of atanine, 2-isopropylfuro [2,3-b] quinolines and 3,4-dihydro-2,2-dimethyl-2H-pyrano [2,3-b]quinolines

Authors: Satheeshkumar, R; Kavitha, C.; Muthusankar, A; Shanmughavel, P; Prasad, K J Rajendra

Abstract: A simple and efficient route to synthesis of 3-prenyl-2-quinolinones, 2-isopropyl-furo[2,3-b]quinolines and 3,4-dihydro- 2,2-dimethyl-2H-pyrano[2,3-b]quinolines has been developed. 3(1'-Carboxy-3-methylbut-1'-enyl)-2-quinolinones have been decarboxylated using ethanolamine followed by Prevost’s reaction with HgO/I2/AcOH and AgOAc/I2/AcOH to yield 2-isopropyl-furo[2,3-b] quinolines and which on cyclization using a few drops of conc.H2SO4 in ethanol give 3,4-dihydro-2,2-dimethyl-2H-pyrano[2,3-b]quinolines. All the synthesized compounds have been structurally well characterized by spectral studies. The intermediates, 3-prenyl-2-quinolinones, were isolated and characterized. Subsequently the molecular docking studies for the first time have been carried out for all the synthesized compounds using the protein kinase Epidermal Growth Factor Receptor (EGFR) inhibitors.

Page(s): 988-998

Synthesis and biological screening of novel pyrazole and isoxazole derivatives
Title: Synthesis and biological screening of novel pyrazole and isoxazole derivatives

Authors: Raundal, Hemant N; Jadhav, Rahul P; Patil, Amar A; Bobade, Vivek D

Abstract: Novel 1,5-disubstituted pyrazole and isoxazole derivatives like, aryl 5-(3-fluoro-4-methoxyphenyl)-1H-pyrazole-3-carboxylic acid 8a-e, [(aryl)-piperazin-1-yl]-[5-(3-fluoro-4-methoxyphenyl)-isoxazol-3-yl]-methanone 9a-e, aryl 5-(3-fluoro- 4-methoxyphenyl)-1H-pyrazole-3-carboxylic acid 10a-e have been synthesized and characterized using IR, 1H NMR, 13C NMR and mass spectral analysis. All the synthesized compounds have been screened for their antibacterial activity against S. aureus, E. coli, B. subtilis, P. aeruginosa, S. pyogenes, K. terrigena and K. pneumoniae and antifungal activity against T. viride, A. flavus, A. brasillansis, and C. albicans. Interestingly all the synthesized compounds exhibit good antibacterial and antifungal activity.

Page(s): 979-987

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