Novel Penicillin Derivatives Against Selected Multiple-Drug Resistant Bacterial Strains: Design, Synthesis, Structural Analysis, in silico and in Vitro Studies.

INTRODUCTION: The rising numbers of multiple drug-resistant (MDR) pathogens and the consequent antibacterial therapy failure that resulted in severe medical conditions push to illustrate new molecules with extended activity against the resistant strains. In this manner, chemical derivatization of known antibiotics is proposed to save efforts in drug discovery, and penicillins serve as an ideal in this regard. METHOD: Seven synthesized 6-aminopenicillanic acid-imine derivatives (2a-g) were structure elucidated using FT-IR, 1H NMR, 13C NMR, and MS spectroscopy. In silico molecular docking and ADMET studies were made. The analyzed compounds obeyed Lipinski's rule of five and showed promising in vitro bactericidal potential when assayed against E. coli, E. cloacae, P. aeruginosa, S. aureus, and A. baumannii. MDR strains using disc diffusion and microplate dilution techniques. RESULT: The MIC values were 8 to 32 µg/mL with more potency than ampicillin, explained by better membrane penetration and more ligand-protein binding capacity. The 2g entity was active against E. coli. This study was designed to find new active penicillin derivatives against MDR pathogens. CONCLUSION: The products showed antibacterial activity against selected MDR species and good PHK, PHD properties, and low predicted toxicity, offering them as future candidates that require further preclinical assays.

A novel low-cost indigenous goggle design for oxygen delivery in oxygen supplemented accelerated corneal collagen cross-linking.

PURPOSE: Our study aims to describe a novel low-cost indigenous design of goggles for delivery of oxygen during oxygen supplemented accelerated corneal collagen cross-linking (CXL). METHODS: The goggles were prepared by modifying the safety goggles available in personal protective equipment (PPE) kit. The goggle has two side openings covered with plugs. One plug was removed to insert a tubing for oxygen delivery at a rate of 5 litres/minute. A 20-gauge intravenous cannula was introduced from superior aspect of the goggle for measuring oxygen saturation in periocular environment. RESULTS: The procedure could be successfully performed without any intraoperative difficulty with an oxygen concentration between 80-90% throughout procedure. The time to achieve maximum concentration after switching on oxygen supply was between 30-60 s. None of our patients complained of any discomfort due to goggles. There was no mechanical interference of the goggles with the UV delivery system and a focused UV light could be delivered. The opening in goggles allowed for uninterrupted alignment and centration of UV light at the corneal level. The effective cost of the goggles, canula and tubing amounted to 400INR (5.50USD). There was no distortion, kinking or slippage of the tubing allowing for uninterrupted oxygen flow. These goggles could be sterilized multiple times using plasma sterilization. CONCLUSION: The current modified cost-effective goggle design could be an effective alternative to the currently available oxygen delivery goggles, especially in a low resource setting.

The morphogenesis of granular and lattice corneal dystrophy - A mutation combination hypothesis.

Mutations in the BIGH3 gene encoding for keratoepithelin protein have been described in different corneal dystrophies viz. granular corneal dystrophy, lattice corneal dystrophy, and their different clinical subtypes. Even though linked to the BIGH3 gene, the role of BIGH3 gene in the pathogenesis of corneal lattice dystrophy and corneal granular dystrophy remains to be elucidated. We describe the probable functions of a mutated BIGH3 gene in disease pathogenesis, postulate the existence of other phenotype modifier mutations in these dystrophies, and how the coinheritance of these mutations in different combinations along with a normal/mutated BIGH3 gene can lead to the different morphologic patterns seen in these corneal dystrophies and their subtypes.

A pilot study to determine the occurrence of concomitant diseases and drug intake in patients on antituberculosis therapy.

INTRODUCTION: Altered pharmacokinetics of antituberculosis (anti-TB) drugs due to interaction with non-TB medications or concomitant diseases may lead to suboptimal plasma levels of the affected drugs and hence contribute to the emergence of drug resistance in mycobacteria. Yet, few studies have investigated the prevalence of concomitant drug intake or concurrent diseases in patients on anti-TB therapy (ATT). The objective of this study is to study the prevalence of concomitant diseases and intake of non-TB drugs in patients on ATT. METHODS: Adult patients who were undergoing treatment for TB at a directly observed treatment short-course (DOTS) center were interviewed to find out any concomitant drug intake and ailments they were suffering from. Data were also collected from the patients' treatment cards. RESULTS: A total of 105 patients were interviewed for the study over a period of 1 month. Among these, 66 (62.9%) patients reported having taken a non-ATT drug in the last 3 months, 61 (58.1%) of which were drugs that may affect the ATT. A comparable number of patients (61 [58.1%]) reported suffering from one or the other concurrent illnesses or symptoms while on DOTS, including one patient with AIDS and eight with diabetes mellitus. Fluoroquinolones had been prescribed to four patients while on DOTS. CONCLUSION: A large proportion of the patients with TB were found to be on non-TB concomitant medications including drugs with potential for interactions that are capable of affecting ATT outcomes. It is, therefore, important that the patients and prescribing physicians be aware of any possible drug interactions.

Allergic rhinitis, rhinoconjunctivitis, and eczema: prevalence and associated factors in children.

OBJECTIVE: We aim to describe the data collected from India during phase 3 of the International study of asthma and allergy in childhood (ISAAC) study. Prevalence, severity, and population characteristics associated with rhinitis, rhinoconjunctivitis, and eczema were assessed. METHODS: Children from two age groups (6-7 and 13-14 years) were included in the study as per the ISAAC protocol. The symptoms of allergy and associated features were assessed using a questionnaire. RESULTS: The prevalence of allergic rhinitis among the 6-7 years age group was 11.3%, while it was 24.4% in the 13-14 years age group. The prevalence of allergic rhinoconjunctivitis was 3.9% in the 6-7 years age group and 10.9% in the 13-14 years age group. The prevalence of eczema was 2.8% in the 6-7 years age group and 3.7% in the 13-14 years age group. The passage of trucks near home, parental smoking, use of paracetamol, use of antibiotics, cooking with firewood, and television watching were associated with allergic rhinitis, rhinoconjunctivitis, and eczema. Maternal smoking was the strongest of all the associated features for allergic rhinitis, rhinoconjunctivitis, and eczema, especially in the 6-7 years age group (odds ratio: 1.9, 95% CI: 1.5-2.4; odds ratio: 2.9, 95% CI, 2.2-3.9; and odds ratio: 3.5, 95% CI: 2.6-4.8, respectively). CONCLUSION: Allergic conditions like allergic rhinitis, rhinoconjunctivitis, and eczema are prevalent among Indian children and are associated with environmental tobacco smoke, paracetamol use, antibiotic use, television watching, and outdoor and indoor air pollution.

Prevalence and severity of asthma among Indian school children aged between 6 and 14 years: associations with parental smoking and traffic pollution.

OBJECTIVE: Phase three of the International Study of Asthma and Allergy in Children (ISAAC) was carried out at various sites in India. The prevalence of asthma symptoms in school children and the effect of environmental tobacco smoke and traffic pollution on the occurrence of asthma were analysed. METHODS: Two groups of school children, aged 6-7 yr and 13-14 yr, participated according to the ISAAC protocol. Schools were randomly selected and responses to the ISAAC questionnaire were recorded. RESULTS: The prevalence of asthma was 5.35% in the 6-7 yr age group and 6.05% in the 13-14 yr age group. The odds ratios (ORs) for the risk of asthma in children with exposure to mild, moderate and heavy traffic pollution compared with minimal traffic pollution were 1.63 (95% CI: 1.43, 1.85), 1.71 (95% CI: 1.49, 1.96) and 1.53 (95% CI: 1.31, 1.78), respectively, in the younger group. Similarly, in the older group, they were 1.19 (95% CI: 1.04, 1.36), 1.51 (95% CI: 1.31, 1.75) and 1.51 (95% CI: 1.29, 1.76). Asthma was associated with maternal smoking [6-7 yr group: OR = 2.72 (2.05, 3.6); 13-14 yr group: OR = 2.14 (1.72, 2.66)] and paternal smoking [6-7 yr group: OR = 1.9 (1.70, 2.11); 13-14 yr group: OR = 1.21 (1.09, 1.34)]. CONCLUSIONS: The prevalence of asthma was lower in the 6-7 than the 13-14 yr age group. Environmental tobacco smoke and traffic pollution were the factors most strongly associated with asthma in Indian children.