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  • 1.
    Parshad, Badri
    et al.
    Department of Chemical Engineering and Biotechnology, University of Cambridge, Cambridge, United Kingdom.
    Kumari, Meena
    Department of Chemistry, Government College for Women Badhra, Haryana, Ch. Dadri, India.
    Khatri, Vinod
    Department of Chemistry, T.D.L. Govt. College for Women, Murthal, Haryana, Sonipat, India.
    Rajeshwari, Rajeshwari
    Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen.
    Pan, Yuanwei
    Institut für Chemie und Biochemie, Freie Universität Berlin, Takustraße 3, Berlin, Germany.
    Sharma, Atul K.
    Department of Chemistry, University of Delhi, Delhi, India.
    Ahmed, Ishtiaq
    Department of Chemical Engineering and Biotechnology, University of Cambridge, Cambridge, United Kingdom.
    Enzymatic synthesis of glycerol, azido-glycerol and azido-triglycerol based amphiphilic copolymers and their relevance as nanocarriers: a review2021Ingår i: European Polymer Journal, ISSN 0014-3057, E-ISSN 1873-1945, Vol. 158, artikel-id 110690Artikel, forskningsöversikt (Refereegranskat)
    Abstract [en]

    Amphiphilic polymeric nanocarriers have attained immense attention for transporting drugs and other bioactive species to the living systems owing to their high loading capacity and efficient internalization. To avoid the side-effects of undesired interactions within the biological system, the use of biocompatible building blocks is most crucial in preparing polymeric amphiphiles. The excellent biocompatibility and multivalency of both glycerol and triglycerol make them suitable monomers to construct macromolecular skeletons. Besides these, easy availability and remarkable aqueous solubility further enlarge their use in synthetic chemistry and give ample possibilities for creating fascinating entities for practical applications. The conversion of glycerol into azido-glycerol and azido-triglycerol further helped in differential functionalization of their polymers with various hydrophobic and hydrophilic groups in different ratios thereby assisting in tuning the amphiphilicity of resulting functionalized polymers. Herein, we review the enzymatic synthesis of glycerol, azido-glycerol and azido-triglycerol based amphiphilic polymeric architectures as nanocarriers for various bio-active species. Enzymatically synthesized linear copolymers synthesized by selective esterification of primary hydroxyl groups of glycerol and its derivatives with suitable diacids/diesters are explored in this review.

  • 2.
    Vidal-Albalat, Andreu
    et al.
    Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen.
    Kindahl, Tomas
    Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen.
    Rajeshwari, Rajeshwari
    Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen.
    Lindgren, Cecilia
    Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen.
    Forsgren, Nina
    CBRN Defence and Security, Swedish Defence Research Agency, Umeå, Sweden.
    Kitur, Stanley
    Centre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya.
    Tengo, Laura Sela
    Centre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya.
    Ekström, Fredrik
    CBRN Defence and Security, Swedish Defence Research Agency, Umeå, Sweden.
    Kamau, Luna
    Centre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya.
    Linusson, Anna
    Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen.
    Structure-activity relationships reveal beneficial selectivity profiles of inhibitors targeting acetylcholinesterase of disease-transmitting mosquitoes2023Ingår i: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 66, nr 9, s. 6333-6353Artikel i tidskrift (Refereegranskat)
    Abstract [en]

    Insecticide resistance jeopardizes the prevention of infectious diseases such as malaria and dengue fever by vector control of disease-transmitting mosquitoes. Effective new insecticidal compounds with minimal adverse effects on humans and the environment are therefore urgently needed. Here, we explore noncovalent inhibitors of the well-validated insecticidal target acetylcholinesterase (AChE) based on a 4-thiazolidinone scaffold. The 4-thiazolidinones inhibit AChE1 from the mosquitoes Anopheles gambiae and Aedes aegypti at low micromolar concentrations. Their selectivity depends primarily on the substitution pattern of the phenyl ring; halogen substituents have complex effects. The compounds also feature a pendant aliphatic amine that was important for activity; little variation of this group is tolerated. Molecular docking studies suggested that the tight selectivity profiles of these compounds are due to competition between two binding sites. Three 4-thiazolidinones tested for in vivo insecticidal activity had similar effects on disease-transmitting mosquitoes despite a 10-fold difference in their in vitro activity.

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