Synthesis and biological evaluation of new naphthalimide–thiourea derivatives as potent antimicrobial agents active against multidrug-resistant <i>Staphylococcus aureus</i> and <i>Mycobacterium tuberculosis</i>

Rana, Preeti; Parupalli, Ramulu; Akhir, Abdul; Saxena, Deepanshi; Maitra, Rahul; Imran, Mohmmad; Malik, Pradip; Mahammad Ghouse, Shaik; Joshi, Swanand Vinayak; Srikanth, Danaboina; Madhavi, Y. V.; Dasgupta, Arunava; Chopra, Sidharth; Nanduri, Srinivas

doi:10.1039/d4md00062e

RSC Med. Chem.

2024

DOI: 10.1039/d4md00062e

|View full text |Cite

Synthesis and biological evaluation of new naphthalimide–thiourea derivatives as potent antimicrobial agents active against multidrug-resistant Staphylococcus aureus and Mycobacterium tuberculosis

Preeti Rana,

Ramulu Parupalli,

Abdul Akhir

et al.

Abstract: Novel series of naphthalimide thiourea derivatives were synthesised and evaluated against bacterial pathogen panel and mycobacterial pathogen panel.

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2024

Publication Types

Select...

Article3

Relationship

Self Cite0

Independent3

Authors

Journals

Cited by 3 publications

References 37 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Pharmacological Evaluation of Bakuchiol From Psoralea corylifolia L. as Potent Antimicrobial Agent Against Staphylococcus aureus

Tripathi,

Roy,

Agnivesh

et al. 2024

Chemistry & Biodiversity

View full text Add to dashboard Cite

The surge in multi‐drug resistance in Staphylococcus aureus is the reason for pressing need to identify novel alternatives to combat antimicrobial resistance effectively. Bakuchiol is a bioactive prenylated phenolic meroterpene largely abundant in the seeds of Psoralea corylifolia. In this study, we present the biological assessment of bakuchiol derived from P. corylifolia as an antimicrobial agent. S. aureus, a significant opportunistic pathogen, attracts global concern for its biofilm formation and resilience against numerous antibiotics, escaping antibiotic pressure. The primary screening of bakuchiol as an antimicrobial agent against S. aureus delineated its potential as a strong bactericidal agent with a MIC and MBC of 2 μg/mL and 8 μg/mL respectively. Importantly, bakuchiol also exhibited low toxicity against HepG2 cells, showing a favorable selectivity index of 14.4. Furthermore, bakuchiol demonstrated comparable activity (MIC = 2 μg/ mL) against a lab‐generated ciprofloxacin‐resistant mutant of S. aureus. Bakuchiol could significantly inhibit the biofilm formation of S. aureus in a dose‐dependent manner with MBIC50 of 0.956 μg/mL. Bakuchiol effectively inhibited DNA gyrase supercoiling activity at a concentration eight times the MIC, establishing DNA gyrase inhibition as the mechanism of action for bakuchiol. Our findings suggest bakuchiol as potential therapeutic agent for S. aureus‐mediated nosocomial infections.

show abstract

Pharmacological Evaluation of Bakuchiol From Psoralea corylifolia L. as Potent Antimicrobial Agent Against Staphylococcus aureus

Tripathi,

Roy,

Agnivesh

et al. 2024

Chemistry & Biodiversity

View full text Add to dashboard Cite

show abstract

Development of naphthalimide hydrazide derivatives as potent antibacterial agents against carbapenem-resistant A. baumannii

Rana,

Maitra,

Saxena

et al. 2024

RSC Med. Chem.

View full text Add to dashboard Cite

show abstract

An Overview of Naphthylimide as Specific Scaffold for New Drug Discovery

Ruan,

Xie,

Wang

et al. 2024

Molecules

View full text Add to dashboard Cite

Naphthylimides play a pivotal role as aromatic heterocyclic compounds, serving as the foundational structures for numerous pharmacologically significant drugs. These drugs encompass antibacterial, antifungal, anticancer, antimalarial, antiviral, anti-inflammatory, antithrombotic, and antiprotozoal agents. The planar and heteroaromatic characteristics of naphthylimides grant them a strong ability to intercalate into DNA. This intercalation property renders naphthylimide derivatives highly valuable for various biological activities. The advantageous pharmacological activity and ease of synthesis associated with naphthylimides and their derivatives provide significant benefits in the design and development of new compounds within this class. Currently, only a few such molecules are undergoing preclinical and clinical evaluations. In this paper, we have compiled the literature on naphthylimides reported by researchers from 2006 to 2024. Our focus lies on exploring the pharmacological activities of their analogues from a drug development and discovery perspective, while examining their structure–activity relationship and mechanisms of action.

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Synthesis and biological evaluation of new naphthalimide–thiourea derivatives as potent antimicrobial agents active against multidrug-resistant Staphylococcus aureus and Mycobacterium tuberculosis

Abstract: Novel series of naphthalimide thiourea derivatives were synthesised and evaluated against bacterial pathogen panel and mycobacterial pathogen panel.

Cited by 3 publications

References 37 publications

Pharmacological Evaluation of Bakuchiol From Psoralea corylifolia L. as Potent Antimicrobial Agent Against Staphylococcus aureus

Pharmacological Evaluation of Bakuchiol From Psoralea corylifolia L. as Potent Antimicrobial Agent Against Staphylococcus aureus

Development of naphthalimide hydrazide derivatives as potent antibacterial agents against carbapenem-resistant A. baumannii

An Overview of Naphthylimide as Specific Scaffold for New Drug Discovery

Contact Info

Product

Resources

About