Recent Study on Synthesis of Novel Series of Quinolino [3,2-f][1,2,4] triazolo [3,4-b][1,3,4] Thiadiazepines Derivatives Incorporated with 3-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl) Moiety as Potent Antimicrobial Agent | Chapter 11 | Current Perspectives on Chemical Sciences Vol. 4

A Quinolino novel series[3,2-f] [1,2,4] The [3,4-b] Triazolo [1,3,4] The Thiadiazepine (7a-i) derivatives incorporated with 3-(5--i) (benzofuran-2-yl) -1-phenyl-1H-3-yl pyrazol) Moiety was synthesised by a 5-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)) one-point cyclo-condensation reaction. -4-amino-4H-1,2,4-triazole-3-thiol (4) in the presence of K2CO3 in DMF with 2-chloro-quinoline-3-carbaldehyde derivatives (6a-i). Characterization of 3-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)-substituted quinolino [3,2-f] newly synthesised compounds [1,2,4] triazolo[3,4-b] triazolo Elemental analysis and spectral studies such as FT-IR, 1H NMR and 13C NMR, further assisted by Mass Spectra, have been performed with[1,3,4]thiadiazepines. Both synthesised compounds were tested in vitro against the pathogenic microorganism bacterial strains, S. aureus E.coli, P.vulgaris, S.typhi at different concentrations for their antimicrobial activities. In comparison with Chloramphenicol, the bioassay outcome suggested strong to moderate activity against these microbial strains. Through cyclocondensation of 5-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)-4-amino-4H-1,2,4-triazole-3-thiol with 2-chloro-quinoline-3-carbaldehyde derivatives in DMF as a solvent, 1,3,4-thiadiazepine derivatives have been synthesised by economic, better yield and safer methods. Physical, analytical and spectral data established their purity and confirmation. The antimicrobial screening of compounds 7a-f was investigated and it was found that these compounds had excellent to moderate activity against selected strains of bacteria.

Author (s) Details

Dr. M. Idrees
Department of Chemistry, Government Institute of Science, Nagpur (M.S.), 440001, India.

Dr. S. Kola
Department of Chemistry, Government Science College, Gadchiroli (M.S.), 442 605, India.

Dr. N. J. Siddiqui
Department of Chemistry, Government Institute of Science, Nagpur (M.S.), 440001, India.

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Synthesis and Structural Features of Indanone, Tetralone and Naphthone Derivatives: Selective Fluorination and Condensation Products | Chapter 2 | Current Perspectives on Chemical Sciences Vol. 2

 The present study seeks to investigate the synthesis and structural characteristics of derivatives of Indanone, Tetralone and Naphthone. Via Claisen condensations, arylhydrazine condensations, BakerVenkataraman rearrangements, Claisen-Schmidt reactions, selective fluorinations and trifluoroacetylations in yields ranging from 22-92 percent, indanone, tetralone and naphthone derivatives and fused-ring heterocycles were prepared. Regiochemistry and stereochemistry observed in these products and their usefulness as scaffolds for the preparation of heterocyclic derivatives are of particular interest. Unusual changes such as a novel one-pot, dual trifluoroacetylation, trifluoroacetylnaphthone synthesis via deacetylation and an exchange of the acetyltrifluoroacetyl group are also noted. Using crystallographic methods, solid-state structural features exhibited by these compounds were investigated. In addition , this study will concentrate on the selective introduction of fluorine and fluorine-containing groups into these heterocyclic materials. In the near future , we expect these results to be announced.

Author(s) Details

Paul D. Boyle
Department of Chemistry, Western University, 1151 Richmond St., London, Ontario, N6A 5B7, Canada.

David Breaud
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Matthew Churley
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Patrick Coppock, Jr.
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Elvia Encarnacion-Thomas
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Chloe Fernandes
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Augustus W. Fountain
Department of Chemistry and Biochemistry, University of South Carolina, 631 Sumter Street Columbia, SC 29208, USA.

Cristina Gomez
Department of Chemistry and Life Science, United States Military Academy, 646 Swift Road, West Point, NY 10996, USA.

Alejandro Guzman
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

James L. Jackson
US Army Corps of Engineers, 101 West Oglethorpe Avenue, Savannah, GA 31401, USA.

Linh Lam
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Ajay Mallia
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Samantha Moseley
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Sang H. Park
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

William F. Pearman
Department of Chemistry and Life Science, United States Military Academy, 646 Swift Road, West Point, NY 10996, USA.

Robert D. Schmidt
Department of Chemistry, North Carolina State University, P.O. Box 8204, Raleigh, NC 27695, USA.

Joseph C. Sloop
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Roger D. Sommer
Molecular Education, Technology, and Research Innovation Center, North Carolina State University, 2620 Yarbrough Dr., Raleigh, NC 27695, USA.

Stephanie Stalker
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Jonathan Weyand
Department of Chemistry and Life Science, United States Military Academy, 646 Swift Road, West Point, NY 10996, USA.

Karla Wilmott
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

Jonathan Yi
School of Science and Technology, Georgia Gwinnett College, 1000 University Center Lane, Lawrenceville, GA 30043, USA.

 

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