New -(2-phenyl-4-oxo-1,3-thiazolidin-3-yl)-1,2-benzothiazole-3-carboxamides and acetamides as antimicrobial agents.

Journal: MedChemComm
Published Date: Nov 3, 2017

Abstract

A series of 21 novel -[2-phenyl-4-oxo-1,3-thiazolidin-3-yl]-1,2-benzothiazole-3-carboxamides/acetamides () as well as a series of '-(halophenylmethylidene)-1,2-benzothiazole-3-acetohydrazides () have been synthesized and evaluated for their antimicrobial activity against eight bacterial and eight fungal species, among them plant, animal and human pathogens and food contaminating species. All compounds appeared to be potent and the best activity was exhibited by compound with MIC in the range of 10.7-21.4 μmol mL × 10 and MBC of 21.4-40.2 μmol mL × 10. The best antifungal activity was observed for compounds and . Elucidation of the relationship between the antimicrobial activity and molecular properties of the synthesized compounds was also performed. Synthetic intermediates were also tested with several exhibiting good antimicrobial activities. Docking studies for some compounds were performed.

Authors

  • Matteo Incerti
    Dipartimento di Scienze degli Alimenti e del Farmaco , Universita' degli Studi di Parma , Italy.
  • Paola Vicini
    Dipartimento di Scienze degli Alimenti e del Farmaco , Universita' degli Studi di Parma , Italy.
  • Athina Geronikaki
    Aristotle University , School of Pharmacy , Thessaloniki , 54124 , Greece . Email: geronik@pharm.auth.gr ; ; Tel: +30 2310 997616.
  • Phaedra Eleftheriou
    Department of Medical Laboratory Studies , School of Health and Medical Care , Alexander Technological Educational Institute of Thessaloniki , Greece.
  • Athanasios Tsagkadouras
    Department of Medical Laboratory Studies , School of Health and Medical Care , Alexander Technological Educational Institute of Thessaloniki , Greece.
  • Panagiotis Zoumpoulakis
    Institute of Biology , Medicinal Chemistry and Biotechnology , National Hellenic Research Foundation , 48 Vas. Constantinou Ave. , 11635 , Athens , Greece.
  • Charalmpos Fotakis
    Institute of Biology , Medicinal Chemistry and Biotechnology , National Hellenic Research Foundation , 48 Vas. Constantinou Ave. , 11635 , Athens , Greece.
  • Ana Ćirić
    Mycological Laboratory , Department of Plant Physiology , Institute for Biological Research , Siniša Stanković , University of Belgrade , Bulevar , Serbia.
  • Jasmina Glamočlija
    Mycological Laboratory , Department of Plant Physiology , Institute for Biological Research , Siniša Stanković , University of Belgrade , Bulevar , Serbia.
  • Marina Soković
    Mycological Laboratory , Department of Plant Physiology , Institute for Biological Research , Siniša Stanković , University of Belgrade , Bulevar , Serbia.

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