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In search of new α-glucosidase inhibitors: Imidazolylpyrazole derivatives.
Chaudhry, Faryal; Naureen, Sadia; Huma, Rahila; Shaukat, Ayesha; Al-Rashida, Mariya; Asif, Nadia; Ashraf, Mohammad; Munawar, Munawar Ali; Khan, Misbahul Ain.
Afiliação
  • Chaudhry F; Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan; Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan.
  • Naureen S; Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan.
  • Huma R; Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan.
  • Shaukat A; Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
  • Al-Rashida M; Department of Chemistry, Forman Christian College (A Chartered University), Ferozepur Road, Lahore 54600, Pakistan.
  • Asif N; Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan.
  • Ashraf M; Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
  • Munawar MA; Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan. Electronic address: mamunawar.chem@pu.edu.pk.
  • Khan MA; Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan; Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
Bioorg Chem ; 71: 102-109, 2017 04.
Article em En | MEDLINE | ID: mdl-28160945
ABSTRACT
Under three different reaction conditions (conventional heating, microwave irradiations and amino acid catalysis), a series of imidazolylpyrazoles (2a-2k) were synthesized in good to excellent yields from a mixture of three precursors aryl(hetaryl)pyrazole-4-carbaldehydes (1a-1k), benzil and ammonium acetate. α-Glucosidase inhibition assay revealed a new class of highly potent agents wherein each compound displayed significant inhibitory potentials (in terms of percentage inhibition and relative IC50 values) as compared to that of the reference drug (Acarbose). Moreover, molecular modelling of most potent compounds 2h, 2j and 2k also helped in understanding the structure and activity relationship.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Saccharomyces cerevisiae / Alfa-Glucosidases / Inibidores de Glicosídeo Hidrolases Limite: Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Paquistão

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Saccharomyces cerevisiae / Alfa-Glucosidases / Inibidores de Glicosídeo Hidrolases Limite: Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Paquistão