Discovery of 6,7-dihydro-3H-pyrano[4,3-c]isoxazol-3-ones as a new class of pathogen specific anti-leptospiral agents

Ilangovan, Andivelu; Sakthivel, P.; Sivasankari, Karikalacholan; Mercy, Charles Solomon Akino; Natarajaseenivasan, Kalimuthusamy

doi:10.1016/j.ejmech.2016.09.020

Cited by 11 publications

(4 citation statements)

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“…Of note, this compound also proved efficient to avoid renal colonization. Interestingly, in silico docking experiments suggested that this compound could bind to LipL32, expressed only in pathogenic strains [70], potentially explaining the lack of effect on saprophytic strains. However, further investigation is required to understand if binding to LipL32 can explain the toxicity of these drugs towards pathogenic leptospires.…”

Section: Antimicrobial Drugsmentioning

confidence: 99%

Recent findings related to immune responses against leptospirosis and novel strategies to prevent infection

Vernel-Pauillac

Werts

2018

Microbes and Infection

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What are the new approaches and emerging ideas to prevent leptospirosis, a neglected bacterial re-emerging zoonotic disease? How do Leptospira interrogans escape the host defenses? We aim here to review and discuss the most recent literature that provides some answers to these questions, in particular data related to a better understanding of adaptive and innate immunity towards leptospires, and design of vaccines. This is an opinion paper, not a comprehensive review. We will try to highlight the new strategies and technologies boosting the search for drugs and vaccines. We will also address the bottlenecks and difficulties impairing the search for efficient vaccines and the many gaps in our knowledge of immunity against leptospirosis. Finally, we aim to delineate how Leptospira spp. escape the innate immune responses of Toll-Like receptors (TLR) and Nod-Like receptors (NLR). The rational use of TLR and NLR agonists as adjuvants could be key to design future vaccines against pathogenic leptospires.

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Section: Antimicrobial Drugsmentioning

confidence: 99%

Recent findings related to immune responses against leptospirosis and novel strategies to prevent infection

Vernel-Pauillac

Werts

2018

Microbes and Infection

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“…Isoxazole and isoxazolone derivatives have also been reported to have potent antimicrobial properties against different Gram‐positive and Gram‐negative organisms ,. They also possess many other biological activities, some of which have recently been reported by Ilangovan et al and Panathur et al . Compounds bearing the isoxazole motif are reported to be Ca 2+ Channel blockers and other isoxazole‐incorporating compounds have been reported to be selective modulators of the multidrug resistant protein…”

Section: Introductionmentioning

confidence: 93%

2,4‐Disubstituted Phenylhydrazonopyrazolone and Isoxazolone Derivatives as Antibacterial Agents: Synthesis, Preliminary Biological Evaluation and Docking Studies

et al. 2018

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A series of new 2,4-disubstituted phenylhydrazonopyrazolone and isoxazolones have been synthesized and evaluated for antibacterial activity. These compounds incorporated the bioactive moieties 3-methyl isoxazolone and 3-methyl pyrazolone. Based on the preliminary results, evaluation of these new compounds as potential antimicrobial agents revelead that four of them which incorporate the isoxazolone moiety exhibited selective antimicrobial activity against Gram-positive bacteria with MICs for S. aureus in the 50-100 mgmL À1 range. Additionally, docking studies were performed in order to explore the possible binding poses in the MurB protein of S. aureus and the results were correlated to the antimicrobial results reported herein.

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“… Ilangovan et al (2017) described the synthesis of new pyrano derivatives and their efficacy against Leptospira interrogans serovar Autumnalis, indicating promising spirocidal activity. Furthermore, Ramalakshmishmi et al synthesized 4-aryl 3-chloro N-pyridine 2-yl 2-azetidinones and found them to exhibit significant inhibition against Leptospira intrerrogans serovar Icterohaemorrhagiae, underscoring their potential as therapeutic candidates ( Puratchikody, 2009 ).…”

Section: Newly Synthesized/natural Compounds Of Spirocidal Agentsmentioning

confidence: 99%

“…Additionally, Natarajan et al evaluated novel azetidinones bearing quinoxaline derivatives and reported high inhibitory activity against Leptospira, suggesting their candidacy for further investigation (Selvaraj et al, 2013). Ilangovan et al (2017) described the synthesis of new pyrano derivatives and their efficacy against Leptospira interrogans serovar Autumnalis, indicating promising spirocidal activity. Furthermore, Ramalakshmishmi et al synthesized 4-aryl 3-chloro N-pyridine 2-yl 2-azetidinones and found them to exhibit significant inhibition against Leptospira intrerrogans serovar Icterohaemorrhagiae, underscoring their potential as therapeutic candidates (Puratchikody, 2009).…”

Section: Newly Synthesized/natural Compounds Of Spirocidal Agentsmentioning

confidence: 99%

Current treatment options for leptospirosis: a mini-review

Petakh,

Behzadi,

Oksenych

et al. 2024

Front. Microbiol.

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Leptospirosis, one of the most common global zoonotic infections, significantly impacts global human health, infecting more than a million people and causing approximately 60,000 deaths annually. This mini-review explores effective treatment strategies for leptospirosis, considering its epidemiology, clinical manifestations, and current therapeutic approaches. Emphasis is placed on antibiotic therapy, including recommendations for mild and severe cases, as well as the role of probiotics in modulating the gut microbiota. Furthermore, novel treatment options, such as bacteriophages and newly synthesized/natural compounds, are discussed, and the findings are expected to provide insights into promising approaches for combating leptospirosis.

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Discovery of 6,7-dihydro-3H-pyrano[4,3-c]isoxazol-3-ones as a new class of pathogen specific anti-leptospiral agents

Cited by 11 publications

References 50 publications

Recent findings related to immune responses against leptospirosis and novel strategies to prevent infection

Recent findings related to immune responses against leptospirosis and novel strategies to prevent infection

2,4‐Disubstituted Phenylhydrazonopyrazolone and Isoxazolone Derivatives as Antibacterial Agents: Synthesis, Preliminary Biological Evaluation and Docking Studies

Current treatment options for leptospirosis: a mini-review

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