Synthesis and Antibacterial Activity of Hydroxy and Chloro-Substituted Chalcone Derivatives

Chalcones are a class of natural products reported with a wide range of biological activities. Among them antibacterial is much promising and many potent chalcones have been emerged as useful antibacterial agents. In view of this, we synthesized 15 chalcones (3a-3o) containing both hydroxyl and chlorine substituents and studied them by using spectroscopic methods. The compounds were tested for antibacterial efficacy against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Proteus vulgaris, among other harmful microorganisms. The compounds have moderate to high antibacterial activity, among them heteroaromatic ring containing compounds (3m, 3n, and 3o) elicited higher activity than the standard drug benzyl penicillin. The compound 3m having the pyridinyl compound displayed the maximum activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Proteus vulgaris, with zone of inhibition (in mm) values of 27.52±0.16, 28.85±0.11, 22.05±0.16, and 23.18±0.17, respectively. The synthesized compounds could be used as lead molecules in the development of novel antibacterial medicines.

Penicillins’ Solubility in Supercritical Carbon Dioxide: Modeling by Cubic Equations of States Revisited

Development of processes using green solvents as supercritical fluids (SCFs) depends on the accuracy of modeling and predicting phase equilibrium which is of considerable importance to exploit the use of SCF process at the level of pharmaceutical industries. Solid-Fluid equilibrium modeling is associated to many drawbacks when compressed gas-based models as cubic equations of states (cEoSs) are used. The unavailability of experimental values of solute’s sublimation pressure presents one of the major obstacles to the solubility modeling with this type of models, and thus, its estimation is essential and inevitable. This work is an attempt to address a question regarding “accurate estimated value” of sublimation pressure of two antibiotics Penicillin G (benzyl penicillin) and Penicillin V (phenoxymethyl penicillin). Toward that, first, cEoSs are provided as the thermodynamics modeling framework and fundamental approach. Second, a discussion and a review of some literature results are given. Third, results are invoked to present a criticism analysis that comes from the use of modified form of Peng-Robinson (PR) equation of states. Finally, considerable improvement of modeling results by using a new sublimation pressure is shown.

MRSA REMAINS A GREAT PRIORITY DUE TO THE TREMENDOUS MORTALITY --- A BIRD'S EYE VIEW

Methicillin-resistant Staphylococcus aureus (MRSA) is difcult to treat with methicillin, amoxicillin, penicillin, oxacillin, and other commonly used antibiotics because of its resistance. Staphylococcus organisms rapidly develop drug resistance as many as 50% of the domiciliary and 80% of the hospital strains are now penicillin resistant. Staphylococcus aureus also show multiple drug resistance. Therefore, Staphylococcal isolates should always be tested for antimicrobial sensitivity and chronic infection should be treated by more than one drug. Before 1960,when methicillin, is the rst penicillin's-resistant penicillin's, was brought into use, about 1%of the strains of the Staphylococcus aureus were "methicillin resistant" and by 1970 in Britain their proportion has risen to about 5%.These strains are tolerant of, low therapeutic concentrations of methicillin, cloxacillin, benzyl penicillin and ampicillin.They do not destroy methicillin and cloxacillin, but most of them are penicillinase-producing as well as being "methicillin resistant" and therefore inactivate benzyl penicillin and ampicillin. Its resistance is uncertain since infections may be cured with a high dose of methicillin.

Need for Intrapartum Antibiotic Prophylaxis in Women with Prior History of Group B Streptococcus Carriage

The incidence of early onset neonatal GBS(EOGBS) disease in the UK and Ireland is 0.57/1000 births. Intrapartum antibiotic prophylaxis (IAP) reduces the risk. Previous colonisation is associated with 50% carriage in the current pregnancy. In these women, RCOG recommends IAP with a history of neonatal infection, otherwise offering the option of screening at 35-37 weeks. In Ireland, there is no national consensus on IAP in prior GBS colonisation. Currently at University Hospital Waterford (UHW), all women with prior GBS colonisation receive IAP. Studies examining the use of point-of-care testing have shown reduction in the use of IAP and EOGBS rates. We aimed to examine the screening and IAP administration in maternal prior GBS colonisation and the incidence of GBS in this cohort in UHW. Data was collected retrospectively from laboratory, medical records and electronic patient manager systems. Women who received IAP between 1stJuly 2020 and 31stDecember 2020 were identified. Women who received IAP for current and prior GBS colonisation were included. Women who received IAP for preterm labour, preterm prelabour rupture of membranes and pyrexia in labour were excluded. Ninety-two women with current or prior GBS colonisation received IAP, of which only 15(16.30%) were current and 77(83.69%) were prior GBS colonisation. In women with prior GBS colonisation, 49(63.63%) were screened, 3/49(6.12%) were positive, 28 were not screened. Seventy-eight (84.78%) received benzyl-penicillin. Six (6.52%) received clindamycin. Twenty-two (23.91%) babies were admitted to the Neonatal Unit, however, only one cultured positive for gram-positive cocci. The incidence of EOGBS in this cohort is low. A risk-based approach or point-of-care testing should be considered to reduce unnecessary IAP administration.

Microbiological Pattern, Antimicrobial Resistance and Prevalence of MDR/XDR Organisms in Patients With Diabetic Foot Infection in an Indian Tertiary Care Hospital

Foot infections are the most prevalent problem in persons with diabetes. The burden of multidrug resistant (MDR) microorganisms in diabetic foot infections (DFIs) is rising day by day. Given that, the present study aims to determine the variety of microorganisms isolated from the diabetic foot ulcers (DFUs), and their antibiotic sensitivity pattern. This prospective observational study was conducted for 1 year at Bharati Hospital and Research Centre, Pune, India. Clinically infected patients with DFU admitted to the surgery ward were included in this study. The specimen for microbiological studies is obtained from the wound swabs, soft tissue, and bone tissue as a part of routine clinical care. All demographic, clinical data, microbial culture results were collected, and evaluated for each case. Antimicrobial susceptibility testing to different agents was carried out using the VITEK-2® machine. A total of 110 microorganisms were isolated from 76 specimens, with an average of 1.4 organisms per lesion. Staphylococcus aureus (n = 27, 24.5%) and Escherichia coli (n = 17, 15.4%) were the most prevalent Gram-positive and Gram-negative organisms isolated, respectively. MDR organisms constituted up to 52 (47.2%), while 6 (5.4%) of the samples were extensively drug resistant (XDR). Methicillin-resistant S aureus (MRSA) accounted for up to 19 (70.3%) of the S aureus isolates, likewise extended-spectrum beta-lactamase producing microorganisms constituted 16 (14.5%) of total isolates in this study. Oxacillin and benzyl penicillin exhibited least susceptibility against Gram-positive bacteria, among Gram-negative organisms; cefuroxime, ceftriaxone, and ciprofloxacin were least sensitive. As most of the S aureus isolate in our study was MRSA, empirical antimicrobial therapy may include coverage for MRSA in a patient with risk factors associated with this pathogen. A crucial observation is the presence of XDR strains of Proteus mirabilis in DFIs, which is resistant to almost all the antimicrobials, tested. Appropriate antimicrobial selection may reduce the morbidity and the emergence of MDR organisms in DFIs.

Benzylpenicillin-producing Trichophyton erinacei and methicillin resistant Staphylococcus aureus carrying the mecC gene on European hedgehogs – A pilot-study

Background A high carriage rate of methicillin-resistant Staphylococcus aureus with the mecC gene (mecC-MRSA) has been described among Wild European hedgehogs (Europeaus erineaus). Due to this frequent occurrence, it has been suggested that hedgehogs could be a natural reservoir for mecC-MRSA. However, the reason why hedgehogs carry mecC-MRSA remains unknown, but it has been hypothesized that mecC-MRSA could have evolved on the skin of hedgehogs due to the co-occurrence with antibiotic producing dermatophytes. The aim of this pilot-study was therefore to investigate if hedgehogs in Sweden carry Trichophyton spp. and to provide evidence that these dermatophytes are able to produce penicillin or similar substances. In addition, the study aimed to identify if dermatophytes co-occurred with mecC-MRSA. Methods Samples were collected from hedgehogs (Europeaus erineaus) that were euthanized or died of natural causes. All samples were screened for dermatophytes and mecC-MRSA using selective cultivation methods. Suspected isolates were characterized using PCR-based methods, genome sequencing and bioinformatic analyses. Identification of penicillin was performed by ultra-high-performance liquid chromatography-tandem mass spectrometry. Results In total 23 hedgehogs were investigated, and it was shown that two carried Trichophyton erinacei producing benzyl-penicillin, and that these hedgehogs also carried mecC-MRSA. The study also showed that 60% of the hedgehogs carried mecC-MRSA. Conclusion The pilot-study demonstrated that Trichophyton erinacei, isolated from Swedish hedgehogs, can produce benzylpenicillin and that these benzylpenicillin-producing T. erinacei co-occurred with mecC-MRSA. The study also reconfirmed the high occurrence of mecC-MRSA among hedgehogs.

Congenital Syphilis Coinfection in a Preterm Infant with Early Onset Sepsis due to Enterobacter cloacae

Introduction. Syphilis is a tropical disease, caused by a spirochete Treponema pallidum, which can be transmitted transplacentally from untreated mothers to the fetus during any stages of pregnancy. Clinical manifestations of early congenital syphilis are variable and nonspecific. The diagnosis is based on the serology status of the mother, newborn clinical symptoms, and comparative serology titer between mother and newborn. Case Presentation. A late preterm female infant, appropriate for gestational age, was treated for severe early onset sepsis due to Enterobacter cloacae since day 2 of life. The coinfection with Treponema pallidum was suspected and confirmed at day 4 with clinical signs and a fourfold increase of rapid plasma reagin (RPR) compared to mother’s serology. Combined with meropenem and amikacin, Benzyl-Penicillin was used for 10 days, thereby resulting in a significant clinical and laboratory improvement. The girl was discharged at day 18 and brought for regular follow-ups for both growth milestone and syphilis serology. RPR decreased fourfold at the age of 1 month. Conclusion. Syphilis should not be overlooked. The vertical transmission is preventable by an on-time treatment of the infected mother, triggered by a proper antenatal screening at the right time. Congenital syphilis should be ruled out in any challenging neonatal sepsis. The diagnosis tools and treatments are easily accessible and inexpensive in our economical settings.

Factors Associated with Streptococcus pneumoniae Nasopharyngeal Carriage and Antimicrobial Susceptibility among Children Under the Age of 5 Years in the Southwestern Colombia

Objective This work aims to evaluate the factors associated with Streptococcus pneumoniae nasopharyngeal colonization and antimicrobial susceptibility among pediatric outpatients in southwestern Colombia, 2019. Methods A cross-sectional study was performed using survey-based interviews and the collection of nasopharyngeal-swab specimens for microbiological characterization and antimicrobial susceptibility testing. Logistic regression analyses were performed for factors associated with nasopharyngeal carriage. Results A total of 452 children under the age of 5 years were examined in which 41.8% carried S. pneumoniae. Higher pneumococcal carriage frequencies were observed among participants aged <2 years and in individuals belonging to indigenous communities, which were lacking established pneumococcal-conjugated vaccine-10 immunization schemes. Additionally, children attending childcare institutions were also highly colonized by pneumococci. S. pneumoniae showed 57.7% nonsusceptibility to benzyl-penicillin (meningitis-cut); 45.5% intermediate-sensitivity to benzyl-penicillin (oral-cut) and 21.7% to cefotaxime; and resistance to erythromycin (40.7%), tetracycline (36.0%), trimethoprim/sulfamethoxazole (24.9%), clindamycin (24.3%), and ceftriaxone (27.0%). Conclusion The 41.8% of participants carrying S. pneumoniae show a scenario with the presence of multidrug and extensively drug-resistant strains, which constitutes important reservoirs of bacterial transmission by children aged <5 years in Colombia, leading to an onset of pneumococcal diseases. Hence, there is an urgent need to expand conjugate pneumococcal immunization in the community and ensure compliance with established immunization schedules.

Antibiotic Prescription Rationality And Associated In-Patient Treatment Outcomes In Children Under-Five With Severe Pneumonia At Bwizibwera Health Center IV, Mbarara District, South-Western Uganda

Background: Pneumonia is a major cause of morbidity and mortality in children under five. Antibiotic treatment must be started immediately in children with pneumonia. The irrational use of antibiotics may increase morbidity and mortality in children with pneumonia. Pneumonia accounted for approximately 16 % of the 5.6 million under-five deaths word wide in 2016. In Uganda, it kills approximately 2,400 children per year. Early diagnosis and appropriate case management with rational use of antibiotics remain the most effective intervention to reduce pneumonia-related mortality. This study aimed at determining antibiotic prescription rationality and associated in-patient treatment outcomes in children aged 2-59 months with severe community-acquired pneumonia at Bwizibwera Health Centre IV from 1st May 2018 to 30th April 2019. Methods: We conducted a retrospective cohort design; data were collected from in-patient records of all children aged 2-59 months with severe community-acquired pneumonia who met the eligibility criteria for a period of one year. Data abstraction template was used for data collection. Health care records of children aged 2-59 months who had other co-morbidities and were on medication that could influence or impact on in-patient treatment outcomes from 1st May 2018 to 30th April 2019 were excluded. Data was entered and analyzed using Epi-info v 7.2 and STATA v 13.0 respectively, Descriptive statistics were reported and Chi-square test was used to compare the proportions.Results: Of the total records of children retrieved and screened (N = 847), 229 prescription records of children fulfilled inclusion criteria, 57 (24.9 %) had rational prescriptions with good outcomes and 172 (75.1 %) had irrational prescriptions with 10 (4.4 %) having unfavorable outcomes. The majority (73.7 %) of those who received rational prescription were on treatment with a combination of benzyl penicillin plus gentamycin while (26.3 %) were on ampicillin plus gentamycin. The majority (32.4 %) of patients with good treatment outcomes were aged 6 – 11 months. This age category also doubled as the group that experienced the highest percentage (40.0 %) of unfavorable outcomes.Conclusion: The majority of children 172 (75.1%) had received irrational antibiotic prescriptions. There were no statistically significant associations between patient characteristics and treatment outcomes.

STUDY TO ANALYZE THE DRUG SENSITIVITY PROFILE OF THE PATIENTS SUFFERING FROM SORE THROAT: AN OBSERVATIONAL STUDY.

Aim: to analyze the drug sensitivity profile of the patients suffering from sore throat. Materials and Methods: The present prospective observational study was conducted in the Department of ENT, Sri Krishna Medical College and Hospital, Muzaffarpur, Bihar. Among 200 patients of either gender and of any age group attended the OPD of the ENT presented with the complaint of sore throat, throat pain, throat irritation, throat itching and foreign body sensation were recruited. A thorough ENT examination is done including ear examination, throat examination, and nasal examination. Throat swab samples collected through a sterile culture sensitivity tube and sent to microbiological lab and culture sensitivity reports collected from the patients during follow up visits. Results: majority of the patients were male 58.5% and rest 41.5% were female. Gram negative organisms are detected in (70.5%), Gram positive organisms detected (21.0%), and no organism detected (8.5%) of the swab samples. Conclusion: gram positive organisms were resistant to benzyl penicillin or ampicillin, clindamycin, ciprofloxacin or levofloxacin and sensitive to tetracycline, gentamicin, linezolid. Gram negative organisms were resistant to ampicillin, amoxyclav and sensitive to pipracillin or tazobactum, cefoperazone, amikacin, gentamicin, imipenem, cefepime, ciprofloxacin. Keywords: couture, throat swab, gram positive, gram negative, throat infection