Novel linezolid-based oxazolidinones as potent anticandidiasis and antitubercular agents

Faazil, Shaik; Malik, M. Shaheer; Ahmed, Saleh A.; Alsantali, Reem I.; Poornachandra, Y.; Alsharif, Meshari A.; Shaikh, Iqbal N.; Kamal, Ähmed

doi:10.1016/j.bioorg.2022.105869

Cited by 14 publications

(10 citation statements)

References 37 publications

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“…Faazil et al (2022) reported the rationally modified linezolid and furazolidone molecules 1 a‐e, 2 a‐j (Figure 1) while retaining the essential bioactive moieties oxazolidinone and nitrofuran of the parent drug. SAR analysis revealed that the test molecules 2 a‐j (Figure 1) showed better bioactivity as compared to the 1 a‐h (Figure 1).…”

Section: Commentarymentioning

confidence: 99%

“…Furthermore, the fungi-Mycobacterium coinfection has been sporadically reported, which further requires newer design of the antifungal and antitubercular drugs. Faazil et al (2022) reported the rationally modified linezolid and furazolidone molecules 1 a-e, 2 a-j (Figure 1) while retaining the essential bioactive moieties oxazolidinone and nitrofuran of the parent drug. SAR analysis revealed that the test molecules 2 a-j (Figure 1) showed better bioactivity as compared to the 1 a-h (Figure 1).…”

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confidence: 99%

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Hybridization of antimicrobial oxazolidinones with commercial drugs: A fight against the “superbugs”

Prasher

Sharma

2023

Drug Development Research

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Antimicrobial resistance caused by the emergence of antibiotic‐resistant microbes, termed as “superbugs,” poses a grave healthcare concern in the contemporary era. Though this phenomenon is natural, an incessant use of antibiotics due to their unregulated over‐the‐counter availability, and a lack of compliance with the legislation seem to be major contributing factors. This phenomenon has further complicated the treatment of common infectious diseases thereby leading to prolonged illness, disability, and even death. In addition, a sizeable impact on the healthcare cost is met due to a prolonged stay at the medical facilities to receive an intensive care. Overall, the gains of “Millennium Development Goals” and the accomplishment of Sustainable Development Goals are at risk due to the emerging antimicrobial resistance. Since an early identification and development of novel antibiotic classes that evade antimicrobial resistance appears improbable, the strategy of hybridization of the existing antibiotics with efficacious pharmacophores and drug molecules with a different mechanism of antimicrobial action can be a silver lining for the management of superbugs. In this regard, we aim to provide a perspective for the applicability of the hybridization of oxazolidinone class of antibiotics with other drugs for evading antimicrobial resistance.

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Section: Commentarymentioning

confidence: 99%

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confidence: 99%

Hybridization of antimicrobial oxazolidinones with commercial drugs: A fight against the “superbugs”

Prasher

Sharma

2023

Drug Development Research

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“…The crystal structure of AChE has revealed the shape and mechanism of action of the enzyme. [140][141][142][143][144][145][146][147][148][149][150] AChE is one of the most important enzymes in the serine hydrolase family, as it is engaged in the cleavage of ACh, exhausting ACh levels linked to memory and learning. 151 As a result, the cholinergic hypothesis for cognition problems implies that degeneration in ACh-containing neurons play a signicant role in the cognitive decline linked to old age.…”

Section: Cholinesterase Inhibition Mechanismmentioning

confidence: 99%

Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase

et al. 2022

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“…In fact, fungal infections are easier to treat than bacterial and other infections. But unfortunately, resistance to drugs complicates the treatment process . Studies have shown that ergosterol biosynthesis is crucial for the survival of fungi, and many antifungal drug targets have been found based on these studies …”

Section: Introductionmentioning

confidence: 99%

“…But unfortunately, resistance to drugs complicates the treatment process. 4 Studies have shown that ergosterol biosynthesis is crucial for the survival of fungi, and many antifungal drug targets have been found based on these studies. 5 As antifungal agents, azoles act through inhibition of fungal lanosterol 14-α-demethylases (CYP51), an enzyme required to catalyze the oxidative removal of 14-α-demethylases in sterol biosynthesis by fungi.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antifungal Activities, Molecular Docking and Molecular Dynamic Studies of Novel Quinoxaline-Triazole Compounds

Osmaniye,

Baltacı Bozkurt,

Levent

et al. 2023

ACS Omega

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Uncontrolled use of antifungal drugs affects the development of resistance to existing drugs. Azole antifungals constitute a large part of antifungal therapy. Therefore, there is a need for new azole antifungals. Within the scope of this study, 17 new triazole derivative compounds were synthesized. Structure determinations were clarified by spectroscopic analysis methods ( 1 H-NMR, 13 C-NMR, HRMS). In addition, structure matching was completed using two-dimensional NMR techniques, HSQC, HMBC and NOESY. The antifungal effects of the compounds were evaluated on Candida strains by means of in vitro method. Compound 5d showed activity against Candida glabrata with a MIC 90 = 2 μg/mL. Compound 5d showed activity against Candida krusei with a MIC 90 = 2 μg/mL. This activity value, which is higher than fluconazole, is promising. In addition, the biofilm inhibition percentages of the compounds were calculated. Molecular docking and molecular dynamics simulations performed with compound 5d are in harmony with activity studies.

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Novel linezolid-based oxazolidinones as potent anticandidiasis and antitubercular agents

Cited by 14 publications

References 37 publications

Hybridization of antimicrobial oxazolidinones with commercial drugs: A fight against the “superbugs”

Hybridization of antimicrobial oxazolidinones with commercial drugs: A fight against the “superbugs”

Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase

Synthesis, Antifungal Activities, Molecular Docking and Molecular Dynamic Studies of Novel Quinoxaline-Triazole Compounds

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