2. Academic Validation
  3. Design synthesis and evaluation of novel aldose reductase inhibitors: The case of indolyl-sulfonyl-phenols

Design synthesis and evaluation of novel aldose reductase inhibitors: The case of indolyl-sulfonyl-phenols

  • Bioorg Med Chem. 2020 Aug 1;28(15):115575. doi: 10.1016/j.bmc.2020.115575.
Konstantinos Koutsopoulos 1,  Vasiliki Lavrentaki 2,  Ioakeim Antoniou 2,  Antonios Kousaxidis 2,  Matina Lefkopoulou 2,  Anna Tsantili-Kakoulidou 3,  Lucia Kovacikova 4,  Milan Stefek 4,  Ioannis Nicolaou 5
Affiliations

Affiliations

  • 1 Pharmaceutical Department, 251 General Air Force Hospital, 11525 Athens, Greece.
  • 2 Department of Pharmaceutical Chemistry, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54214 Thessaloniki, Greece.
  • 3 Department of Pharmaceutical Chemistry, School of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis, 15771 Athens, Greece.
  • 4 Institute of Experimental Pharmacology and Toxicology, Slovak Academy of Sciences, Dubravska Cesta 9, 841 04 Bratislava, Slovakia.
  • 5 Department of Pharmaceutical Chemistry, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54214 Thessaloniki, Greece. Electronic address: inikolao@pharm.auth.gr.
PMID: 32631572 DOI: 10.1016/j.bmc.2020.115575
Abstract

Therapeutic interventions with Aldose Reductase inhibitors appear to be a promising approach to major pathological conditions (i.e. neuropathy/angiopathy related to chronic hyperglycemia, chronic inflammation and Cancer). Until now, the most potent Aldose Reductase inhibitors have been carboxylic acid derivatives, which poorly permeate biological membranes. In this work, continuing our previous works, we promote the bioisosteric replacement of the carboxylic acid moiety to make equally potent yet more druggable inhibitors.

Keywords

Aldose reductase; Bioisosterism; Indolyl–sulfonyl–phenols; Inflammatory pathologies; Long-term diabetic complications.

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