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RSC Advances Mar 2024In this study, we designed and synthesized a number of novel 1,2,3-triazole-piperazin-benzo[][1,4]thiazine 1,1-dioxide derivatives and investigated their antibacterial...
In this study, we designed and synthesized a number of novel 1,2,3-triazole-piperazin-benzo[][1,4]thiazine 1,1-dioxide derivatives and investigated their antibacterial and hemolytic activity. When compared to the lead chemical, dicloxacillin, the majority of the compounds demonstrated acceptable activity. Among them, the most promising compounds 6e, 6g, 6i, 8d, and 8e exhibited excellent antibacterial activity against the methicillin-susceptible (MSSA), methicillin-resistant (MRSA), and vancomycin-resistant (VRSA) with MIC values of 1.56 ± 0.22 to 12.5 ± 1.75 μg mL, respectively, The percentage of hemolysis ranged from 21.3 μg mL to 33.8 μg mL. Out of the six compounds (6i, 6e, 6f, 6g, 8e, 8d) tested compound 8e and 8d displayed minimal or negligible hemolytic activity across all the tested concentrations 29.6% and 30.2% recorded at 100 μg mL concentration respectively. docking studies were performed to evaluate the molecular interactions of 6e, 6f, 6g, 6i, 8d, and 8e compounds with Human, Mouse and Bovine TLR4 proteins (PDB: 3FXI, 3VQ1, 3RG1) and observed that three of the compounds (6i, 8d, and 8i) had appreciable binding energies ranging from -8.5 to -9.0 Kcal mol. Finally, the pharmacokinetic profile was predicted for potent compounds 8d, 8e and 6i using SWISS/ADME, All compounds investigated in this study adhered to Lipinski's rule of five with slight deviation in molecular weight (8d and 8e).
PubMed: 38500620
DOI: 10.1039/d3ra07509e -
Antibiotics (Basel, Switzerland) Feb 2024First-line treatments for methicillin-susceptible (MSSA) bacteraemia are nafcillin, oxacillin, or cefazolin. Regional shortages of these antibiotics force clinicians to...
BACKGROUND
First-line treatments for methicillin-susceptible (MSSA) bacteraemia are nafcillin, oxacillin, or cefazolin. Regional shortages of these antibiotics force clinicians to use other options like dicloxacillin and cephalotin. This study aims to describe and compare the safety and efficacy of cephalotin and dicloxacillin for the treatment of MSSA bacteraemia.
METHODS
This retrospective study was conducted in a referral centre in Mexico City. We identified MSSA isolates in blood cultures from 1 January 2012 to 31 December 2022. Patients ≥ 18 years of age, with a first episode of MSSA bacteraemia, who received cephalotin or dicloxacillin as the definitive antibiotic treatment, were included. The primary outcome was in-hospital all-cause mortality.
RESULTS
We included 202 patients, of which 48% (97/202) received cephalotin as the definitive therapy and 52% (105/202) received dicloxacillin. In-hospital all-cause mortality was 20.7% (42/202). There were no differences in all-cause in-hospital mortality between patients receiving cephalotin or dicloxacillin (20% vs. 21%, = 0.43), nor in 30-day all-cause mortality (14% vs. 18%, = 0.57) or 90-day all-cause mortality (24% vs. 22%, = 0.82). No severe adverse reactions were associated with either antibiotic.
CONCLUSIONS
Cephalotin and dicloxacillin were equally effective for treating MSSA bacteraemia, and both showed an adequate safety profile.
PubMed: 38391562
DOI: 10.3390/antibiotics13020176 -
Case Reports in Dermatology 2023Fungal infections can be challenging to diagnose, but doctors of every specialty may encounter this issue. They can be mistaken for other common dermatoses such as...
Fungal infections can be challenging to diagnose, but doctors of every specialty may encounter this issue. They can be mistaken for other common dermatoses such as eczema or psoriasis and inadvertently be treated with topical corticosteroids or calcineurin inhibitors. This may lead to tinea incognita, a term used to describe a fungal infection with an altered clinical appearance, which may confuse the clinician even further. This case report presents a 54-year-old previously healthy man with a 4-month history of a painful and pruritic rash in the genitoinguinal region. The patient's general practitioner had unsuccessfully attempted to treat the rash with topical terbinafine, econazole-triamcinolone, and betamethasone-fusidic acid, in addition to peroral dicloxacillin capsules. On examination, there were multiple red-bluish nodules and pustules coalescing into infiltrating erythematous plaques on both thighs and in the pubic region. Fungal cultures were negative, but the clinical features together with the history of prolonged use of combined topical steroids and antifungals raised suspicion of a deep fungal infection. Histopathological skin examination revealed deep suppurative and granulomatous folliculitis with ruptured hair follicles which was consistent with a diagnosis of Majocchi's granuloma. Treatment with itraconazole capsules was initiated, and after a 16-week course of systemic antifungal therapy, the rash resolved. In conclusion, our case report presents a case of Majocchi's granuloma, which is a great mimicker, especially for non-dermatologists. It is therefore important that the diagnosis is considered as a differential diagnosis, even though a patient has previously been treated with a topical antifungal.
PubMed: 37899944
DOI: 10.1159/000533475 -
Tidsskrift For Den Norske Laegeforening... Oct 2023While standard blood tests are often sufficient for an anaemia workup, sometimes more invasive diagnostic testing is required to exclude rare conditions.
BACKGROUND
While standard blood tests are often sufficient for an anaemia workup, sometimes more invasive diagnostic testing is required to exclude rare conditions.
CASE PRESENTATION
A man in his forties contacted his general practitioner because of increasing functional dyspnoea. He had completed a course of dicloxacillin a few months previously for a skin abscess on his abdomen. Bloodwork revealed severe anaemia (haemoglobin 5.4 g/dL), which required transfusion. Subsequent testing excluded iron and vitamin deficiency anaemia, haemolysis and malignancy. Initial bone marrow biopsy was of suboptimal quality. However, repeat tissue sample supported a diagnosis of pure red cell aplasia. The patient improved with ciclosporin treatment, which was gradually tapered.
INTERPRETATION
Pure red cell aplasia should be considered in patients with new onset isolated anaemia with severe reticulocytopenia. Diagnosis depends on obtaining representative tissue from bone marrow biopsy. It is difficult to conclude for this patient whether the aetiology of his pure red cell aplasia was idiopathic or secondary to recent dicloxacillin use.
Topics: Humans; Male; Anemia; Bone Marrow; Dicloxacillin; Neoplasms; Red-Cell Aplasia, Pure; Adult
PubMed: 37874056
DOI: 10.4045/tidsskr.23.0022