X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors

Jekaterina Ivanova; Janis Leitans; Muhammet Tanc; Andris Kazaks; Raivis Zalubovskis; Claudiu T. Supuran; Kaspars Tars

doi:10.1039/c5cc01854d

X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors

Jekaterina Ivanova
, Janis Leitans
, Muhammet Tanc
, Andris Kazaks
, Raivis Zalubovskis^*
, Claudiu T. Supuran
, Kaspars Tars

^*Corresponding author for this work

Department of Molecular Life Sciences, Microbiology and Biotechnology

Latvian Institute of Organic Synthesis
Latvian Biomedical Research and Study Centre
University of Florence

Research output: Contribution to journal › Article › peer-review

77 Citations (Scopus)

Abstract

1-N-Alkylated-6-sulfamoyl saccharin derivatives were prepared and assayed as carbonic anhydrase inhibitors (CAIs). During X-ray crystallographic experiments an unexpected hydrolysis of the isothiazole ring was evidenced which allowed us to prepare highly potent enzyme inhibitors with selectivity for some isoforms with medical applications.

Original language	English
Pages (from-to)	7108-7111
Number of pages	4
Journal	Chemical Communications
Volume	51
Issue number	33
DOIs	https://doi.org/10.1039/c5cc01854d https://doi.org/10.1039/C5CC01854D
Publication status	Published - 28 Apr 2015

OECD Field of Science

1.4 Chemical Sciences

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title = "X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors",

abstract = "1-N-Alkylated-6-sulfamoyl saccharin derivatives were prepared and assayed as carbonic anhydrase inhibitors (CAIs). During X-ray crystallographic experiments an unexpected hydrolysis of the isothiazole ring was evidenced which allowed us to prepare highly potent enzyme inhibitors with selectivity for some isoforms with medical applications.",

author = "Jekaterina Ivanova and Janis Leitans and Muhammet Tanc and Andris Kazaks and Raivis Zalubovskis and Supuran, \{Claudiu T.\} and Kaspars Tars",

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doi = "10.1039/c5cc01854d",

language = "English",

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T1 - X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors

AU - Ivanova, Jekaterina

AU - Leitans, Janis

AU - Tanc, Muhammet

AU - Kazaks, Andris

AU - Zalubovskis, Raivis

AU - Supuran, Claudiu T.

AU - Tars, Kaspars

PY - 2015/4/28

Y1 - 2015/4/28

N2 - 1-N-Alkylated-6-sulfamoyl saccharin derivatives were prepared and assayed as carbonic anhydrase inhibitors (CAIs). During X-ray crystallographic experiments an unexpected hydrolysis of the isothiazole ring was evidenced which allowed us to prepare highly potent enzyme inhibitors with selectivity for some isoforms with medical applications.

AB - 1-N-Alkylated-6-sulfamoyl saccharin derivatives were prepared and assayed as carbonic anhydrase inhibitors (CAIs). During X-ray crystallographic experiments an unexpected hydrolysis of the isothiazole ring was evidenced which allowed us to prepare highly potent enzyme inhibitors with selectivity for some isoforms with medical applications.

UR - https://www.scopus.com/pages/publications/84927761732

U2 - 10.1039/c5cc01854d

DO - 10.1039/c5cc01854d

M3 - Article

C2 - 25813715

AN - SCOPUS:84927761732

SN - 1359-7345

VL - 51

SP - 7108

EP - 7111

JO - Chemical Communications

JF - Chemical Communications

IS - 33

ER -

X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors

Abstract

OECD Field of Science

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