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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 31, 2016 - Issue sup1
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Short Communication

Isoform-selective inhibitory profile of 2-imidazoline-substituted benzene sulfonamides against a panel of human carbonic anhydrases

Claudiu T. SupuranNeurofarba Department, Universita Degli Studi Di Firenze, Florence, Italy, Correspondence[email protected] [email protected]
,
Stanislav KalininThe Ushinsky Yaroslavl State Pedagogical University, Yaroslavl, Russian Federation,
,
Muhammet TançNeurofarba Department, Universita Degli Studi Di Firenze, Florence, Italy,
,
Pakornwit SarnpitakEskitis Institute for Drug Discovery, Griffith University, Brisbane, Queensland, Australia, and
,
Prashant MujumdarEskitis Institute for Drug Discovery, Griffith University, Brisbane, Queensland, Australia, and
,
Sally-Ann PoulsenEskitis Institute for Drug Discovery, Griffith University, Brisbane, Queensland, Australia, and
&
Mikhail KrasavinInstitutes of Chemistry and Translational Biomedicine, Saint Petersburg State University, Saint Petersburg, Russian FederationCorrespondence[email protected] [email protected]
 show all
Pages 197-202 | Received 24 Mar 2016, Accepted 11 Apr 2016, Published online: 10 May 2016

Figures & data

Figure 1. Structures of benzenesulfonamide CAIs containing hydrophobic ureido tails (1–3), the “dual-tail” compounds (4–6) and the design rationale for 2-imidazoline-substituted compounds 7.

Figure 1. Structures of benzenesulfonamide CAIs containing hydrophobic ureido tails (1–3), the “dual-tail” compounds (4–6) and the design rationale for 2-imidazoline-substituted compounds 7.

Scheme 1. Synthesis of 2-imidazoline-substituted benzene sulfonamides 5a–o.

Scheme 1. Synthesis of 2-imidazoline-substituted benzene sulfonamides 5a–o.

Scheme 2. Microwave-assisted synthesis of 5m.

Scheme 2. Microwave-assisted synthesis of 5m.

Table 1. Inhibitory activity data for compound 5a–o obtained against hCA I, II, IV and VII.

Figure 2. Spatial alignment of compound 5a (green) with its ureido analog 3 (red).

Figure 2. Spatial alignment of compound 5a (green) with its ureido analog 3 (red).
Supplemental material

IENZ_1178248_Supplementary_Material.pdf

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Related Research Data

Isoform-selective inhibitory profile of 2-imidazoline-substituted benzene sulfonamides against a panel of human carbonic anhydrases
Source: Figshare
Isoform-selective inhibitory profile of 2-imidazoline-substituted benzene sulfonamides against a panel of human carbonic anhydrases
Source: Figshare

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