Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2017 Mar 9;22(3):434.
doi: 10.3390/molecules22030434.

N-Pyrrylarylsulfones with High Therapeutic Potential

Valeria Famiglini  1 , Sabrina Castellano  2 , Romano Silvestri  3
Affiliations
Review

N-Pyrrylarylsulfones with High Therapeutic Potential

Valeria Famiglini et al. Molecules. .

Abstract

This review illustrates the various studies made to investigate the activity of N-pyrrylarylsulfone containing compounds as potential antiviral, anticancer and SNC drugs. A number of synthetic approaches to obtain tetracyclic, tricyclic and non-cyclic compounds, and their biological activity with regard to structure-activity relationships (SARs) have been reviewed. The literature reviewed here may provide useful information on the potential of N-pyrrylarylsulfone pharmacophore as well as suggest concepts for the design and synthesis of new N-pyrrylarylsulfone based agents.

Keywords: heterocycle; polycyclic compound; sulfonamide; therapeutic agent.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Chart 1
Chart 1
Examples of sulfa and pyrrole containing drugs.
Scheme 1
Scheme 1
Synthesis of 14.
Scheme 2
Scheme 2
Synthesis of 21, and structure of 10-methyl-10-azaaptazepine (20).
Scheme 3
Scheme 3
Chemical transformation of 24.
Scheme 4
Scheme 4
Synthesis of 32.
Scheme 5
Scheme 5
Synthesis of 38 and 42.
Chart 2
Chart 2
Heterocyclic compounds structurally correlated to PBTD HIV-1 NNRTIs.
Chart 3
Chart 3
PBTDs as CML agents.
Scheme 6
Scheme 6
Synthesis of PAS 51–58.
Scheme 7
Scheme 7
Synthesis of PAS 60.
Chart 4
Chart 4
Structure of pyrryl heteroaryl sulfones 63–65.
Chart 5
Chart 5
Design of APAS derivatives.
Scheme 8
Scheme 8
Synthesis of APASs 69 and 70.
Scheme 9
Scheme 9
Smile rearrangement of 72 to 74.
Chart 6
Chart 6
Structure of indolylsulfones 78–86.
See this image and copyright information in PMC

References

    1. Gerald M.C. The Drug Book. Sterling Education; New York, NY, USA: 2013.
    1. Dogmagk G. Ein Beitrag zur Chemotherapie der bakteriellen Infektionen. Deutsch. Med. Wochenschr. 1935;61:250–253. doi: 10.1055/s-0028-1129486. - DOI
    1. Dogmagk G. Eine neue Klasse von Desinfectionsmitteln. Deutsch. Med. Wochenschr. 1935;61:829–832. doi: 10.1055/s-0028-1129654. - DOI
    1. Henry R.J. The mode of action of sulfonamides. Bacteriol. Rev. 1943;7:175–262. - PMC - PubMed
    1. Sulfamethoxazole DrugBank. [(accessed on 17 August 2016)]. Available online: http://www.drugbank.ca.

MeSH terms

LinkOut - more resources