Drug screening of rhodanine derivatives for antibacterial activity

ABSTRACT

Introduction: Bacteriological infections are a major risk to human health. These include all hospital and public-acquired infections. In drug discovery, rhodanines are privileged heterocyclic frameworks. Their derivatives possess strong anti-bacterial activity and some of them have shown potent activity against multidrug-resistant pathogens, both under in vitro and in vivo conditions. To treat multi-drug resistant pathogens, the development of novel potent drugs, with superior anti-bacterial efficacy, is paramount. One avenue which shows promise is the design and development of novel rhodanines.

Areas covered: This review summarizes the status on rhodanine-based derivatives and their anti-bacterial activity, based on published research over the past six years. Furthermore, to facilitate the design of novel derivatives with improved functions, their structure–activity relationships are assessed with reference to their efficacy as anti-bacterial agents and their toxicity.

Expert opinion: The pharmacological activity of molecules bearing a rhodanine scaffold needs to be very critically assessed in spite of considerable information available from various biological evaluations. Although, some data on structure–activity relationship frameworks is available, information is not adequate to optimize the efficacy of rhodanine derivatives for different applications.

KEYWORDS:

• Rhodanine
• anti-bacterial activity
• multi drug-resistance
• structure–activity relationship
• drug discovery

Article highlights

• A significant activity of rhodanine based molecules.

• Anti-bacterial activity against multidrug-resistant pathogens, both under in vitro and in vivo conditions.

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Declaration of interest

The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Referee Disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This manuscript is supported by GITAM University, India & University of KwaZulu Natal, South Africa.