SYNTHESIS, MOLECULAR BIOINFORMATICS MODELLING, AND ANTIMICROBIAL EVALUATION OF SOME NOVEL OXADIAZOLE FLUOROQUINOLONE DERIVATIVES

Objective: The present study envisages a series of oxadiazole fluoroquinolone derivatives that were synthesized (D1–D12) with added derivatives such as phenyl, aminophenyl, amino hydroxyphenyl along with cyclopropyl, ethyl, piperazine, and imidazole. Methods: All of the newly produced molecules were characterized by infrared, 1H nuclear magnetic resonance, mass spectrometry, and elemental analysis technique and screened for docking stimulation to find out binding modes of synthesized derivatives with 3FV5, 5IMW, and 5ESE and evaluated for in vitro antimicrobial activity. Results: From this study, it was found that the compound D8 showed good antibacterial activity against Gram-positive (Staphylococcus aureus), compound D9 showed good antibacterial activity against Gram-negative (Escherichia coli), and compound D3 showed good antifungal activity against fungi (Saccharomyces cerevisiae) in comparison with standard drugs (Ciprofloxacin and fluconazole). The zone of inhibition and minimum inhibitory concentration studies was performed on synthesized compounds. Conclusion: The analogs of oxadiazole flouroquinolone are suggested to be potent inhibitors with sufficient scope for further exploration

Anti-Neutrophil Cytoplasmic Antibody-Associated Vasculitis: A Glimpse into The Future

Background: A class of uncommon IgG4-related systemic diseases known as vasculitis caused by antineutrophil cytosolic antibodies (ANCA) is distinguished by the enlargement of small to large blood vessels. Objective: This review article offers an in-depth analysis of the most recent developments in ANCA-associated vasculitis, covering a range of topics from pathophysiology and diagnostics to treatment and long-term results.   Methods: In this review we investigated the existing work on ANCA associated vasculitis by different sources such as Science Direct, Scopus, Pubmed, Web of Science, Google scholar and SciHub. Results: A number of diseases, including eosinophilic granulomatosis with polyangiitis (EGPA), microscopic polyangiitis (MPA), and granulomatosis with polyangiitis (GPA), can have significant morbidity and mortality if they are not appropriately diagnosed and treated. Understanding the pathophysiology, clinical presentation, and curative options for ANCA-associated vasculitis have advanced significantly during the past ten years. The development of specific immunosuppressive medications has been largely responsible for the remarkable evolution in recent years in the treatment of ANCA-associated vasculitis. Conclusion: This review article has provided a detailed examination of the therapy for AAV, alternatives available, including induction and maintenance regimens, as well as the accompanying advantages and disadvantages. Additionally, the growing importance of biologic drugs like rituximab was examined, emphasizing its potential as supplements or replacements for traditional medical treatments

Formulation and optimization of Retapamulin loaded PLGA nanoparticles for burn wounds

In the present study, PLGA nanoparticles (PLGA-NP) of retapamulin (RP) were prepared and optimized by studying the effect of various formulation and process variables for effective delivery at burn wound site. Drug loaded PLGA-NP were successfully prepared and characterized by TEM, XRD and DSC study. Formulation and process variables like surfactant concentration, drug concentration, polymer concentration etc. showed significant effect on the particle size, entrapment efficiency and drug loading. PLGA-NP exhibited prolonged drug release following Higuchi release kinetics (R2= 0.9907). In vitro study demonstrated systemic escape of drug from PLGA-NP which might eliminate side effects associated with topical exposure through conventional treatment. Further retention of activity of entrapped drug was confirmed by in vitro antimicrobial assay. Optimized PLGA nanoparticle of Retapamulin was incorporated into PVA-Chitosan hydrogel slurry and casted into film to prepare multiphase hydrogel.Thus, present optimized system can be effectively used for delivery of drug at burn wound site in especially compromised wounds.&nbsp

SYNTHESIS, CHARACTERIZATION, AND ANTIMICROBIAL EVALUATION OF 3,5-DISUBSTITUTED TRIAZOLES BEARING 5-CHLORO-2-METHYLINDOLE: SYNTHESIS OF NOVEL 1,2,4- TRIAZOLES

Objectives: Synthesis, characterization, and antimicrobial evaluation of some novel 1,2,4-triazole derivatives clubbed with indole. Methods: Procedure includes the synthesis of 1,2,4-triazole compounds by condensation reaction with ammonia. The synthesis was carried out in three steps with chlorophenylhydrazine hydrochloride as starting material with ethyl acetoacetate and hydrazine hydrate in the presence of ethanol to form hydrazide derivative. The hydrazide derivative then refluxed with ammonium acetate to get the desired compounds. Results: All the synthesized compounds were characterized and confirmed by Fourier-transform infrared spectroscopy, mass spectroscopy, and nuclear magnetic resonance spectroscopy. The new compounds (Va-f) synthesized were evaluated for antimicrobial activity. Conclusion: All the compounds Va-f screened for antimicrobial activity against selected strains of microorganisms. Compound Vb was found to be potent against Escherichia coli, Vc was found to be more active against Aspergillus niger