BIOMAT Database Logo BIOMAT Database Logo

Synthesis and biological evaluation of N-(aryl)-2-thiophen-2-ylacetamides series as a new class of antitubercular agents. 2007

Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Instituto de Pesquisas Clínica Evandro Chagas-IPEC, Av. Brasil, 4365 Manguinhos Rio de Janeiro, RJ, Brazil.

The present article describes a series of 21 N-(aryl)-2-thiophen-2-ylacetamides, which were synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis, and the activity expressed as the minimum inhibitory concentration (MIC) in mug/mL. The compounds 2, 3, 7, 8, 11, 12, 15, 16, and 20 exhibited activity between 25 and 100 microg/mL and could be a good start point to find new lead compounds in the fight against multidrug resistant tuberculosis.

UI MeSH Term Description Entries
D008264 Macrophages The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.) Bone Marrow-Derived Macrophages,Monocyte-Derived Macrophages,Macrophage,Macrophages, Monocyte-Derived,Bone Marrow Derived Macrophages,Bone Marrow-Derived Macrophage,Macrophage, Bone Marrow-Derived,Macrophage, Monocyte-Derived,Macrophages, Bone Marrow-Derived,Macrophages, Monocyte Derived,Monocyte Derived Macrophages,Monocyte-Derived Macrophage
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D000081 Acetamides Derivatives of acetamide that are used as solvents, as mild irritants, and in organic synthesis.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000995 Antitubercular Agents Drugs used in the treatment of tuberculosis. They are divided into two main classes: "first-line" agents, those with the greatest efficacy and acceptable degrees of toxicity used successfully in the great majority of cases; and "second-line" drugs used in drug-resistant cases or those in which some other patient-related condition has compromised the effectiveness of primary therapy. Anti-Tuberculosis Agent,Anti-Tuberculosis Agents,Anti-Tuberculosis Drug,Anti-Tuberculosis Drugs,Antitubercular Agent,Antitubercular Drug,Tuberculostatic Agent,Tuberculostatic Agents,Antitubercular Drugs,Agent, Anti-Tuberculosis,Agent, Antitubercular,Agent, Tuberculostatic,Anti Tuberculosis Agent,Anti Tuberculosis Agents,Anti Tuberculosis Drug,Anti Tuberculosis Drugs,Drug, Anti-Tuberculosis,Drug, Antitubercular
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D013876 Thiophenes A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur. Thiophene
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus

Related Publications

Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Synthesis and biological evaluation of some novel N-aryl-1,4-dihydropyridines as potential antitubercular agents.
September 2011, Bioorganic & medicinal chemistry letters,
Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents.
August 2018, MedChemComm,
Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Synthesis and biological evaluation of a novel series of aryl S,N-ketene acetals as antileishmanial agents.
July 2013, Bioorganic & medicinal chemistry letters,
Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Synthesis of 2-methoxy-3-(thiophen-2-ylmethyl)quinoline containing amino carbinols as antitubercular agents.
June 2020, Bioorganic chemistry,
Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Synthesis and biological evaluation of 2-aminothiazole-thiazolidinone conjugates as potential antitubercular agents.
June 2018, Future medicinal chemistry,
Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Synthesis, Characterization, and Biological Evaluation of New Derivatives Targeting MbtI as Antitubercular Agents.
February 2021, Pharmaceuticals (Basel, Switzerland),
Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents.
January 2020, Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents,
Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Synthesis and biological evaluation of a new series of N-acyldiamines as potential antibacterial and antifungal agents.
October 2014, Bioorganic & medicinal chemistry letters,
Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents.
January 2022, Bioorganic & medicinal chemistry,
Maria Cristina Silva Lourenço, and Felipe Rodrigues Vicente, and Maria das Graças Muller de Oliveira Henriques, and André Luis Peixoto Candéa, and Raoni Schroeder Borges Gonçalves, and Thais Cristina M Nogueira, and Marcelle de Lima Ferreira, and Marcus Vinícius Nora de Souza
Novel 6-Phenylnicotinohydrazide Derivatives: Design, Synthesis and Biological Evaluation as a Novel Class of Antitubercular and Antimicrobial Agents.
January 2017, Biological & pharmaceutical bulletin,
Copied contents to your clipboard!