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1.
Mol Divers ; 27(2): 889-900, 2023 Apr.
Article in English | MEDLINE | ID: mdl-35781657

ABSTRACT

Individually, hydroxycoumarin and amino pyrimidine derivatives are of significant biological interest owing to their importance in drugs and pharmaceuticals. To access their combined biological impact into one molecule, we designed a novel, one-pot green approach for synthesizing trisubstituted methanes. A series of new heteroaryl-substituted methanes have been synthesized and subjected to in vitro antibacterial and antioxidant evaluation. Tests against clinical isolates of Escherichia coli (gram-negative) and Staphylococcus aureus showed potent activity of the derivatives 4a, 4b, 4d, 4e, 4f, 4l, and 5 against the former, and 4a, 4e, 4j, and 4l against the later one. Further, antioxidant assay for these TRSMs was also studied where 4a, 4b, 4f, 4j, and 4l exhibited the most promising results. These preliminary bioassay evaluations strongly suggest the promise and scope of these molecules in medical science. A one pot methodology for the synthesis of coumarin and uracil tethered trisubstituted methanes has been reported. The synthesized derivatives were further analyzed for their antibacterial and antioxidant properties to explore their medicinal applications. The salient features of this methodology are operational simplicity, short reaction time, good to moderate yields of the products, easy purification method. Biochemical assay of the synthesized TRSMs a reveals their utility in medicinal & pharma industry.


Subject(s)
Antioxidants , Methane , Antioxidants/chemistry , Anti-Bacterial Agents/chemistry , Catalysis , Microbial Sensitivity Tests
2.
Lett Appl Microbiol ; 76(1)2023 Jan 23.
Article in English | MEDLINE | ID: mdl-36688758

ABSTRACT

D-amino acids, the important components of the bacterial cell walls, are valuable molecular and genetic markers of bacterial-derived organic material in the environment. D-serine, a racemization product of L-serine is one such amino acid present in various prokaryotes and eukaryotes. It is a well-recognized regulator of various activities in the human nervous system. In plants, it has a role in the nitrogen cycle regulation and pollen tube growth. Serine enantiomers are present in different concentrations and few bacterial strains are reported to contribute to D-serine in the environment. During the present study, soil samples from different places in North India were collected and processed to isolate and screen the bacteria on M9 minimal media (Himedia) for D-serine synthesis. Thin-layer chromatography (TLC Silica gel 60 F 254 (20 × 20 cm, Merck, Darmstadt, Germany) and Mass spectroscopic analysis (Bruker MICROTOF II spectrometer) studies, etc were performed. D-serine-producing isolates were characterized as per standard procedures. Bacterial isolate A1C1 with maximum D-serine (0.919 ± 0.02 nM) synthesis under optimal growth conditions (37°C ± 0.5, 150 ± 0.5 RPM, and 7 ± 0.5 pH) was identified as Bacillus tequilensis based on 16sRNA sequencing. The isolate could be a valuable serine racemization tool for various industrial and environmental applications.


Subject(s)
Bacillus , Serine , Humans , Serine/analysis , Serine/chemistry , Serine/metabolism , Amino Acids/metabolism , Bacillus/metabolism , Chromatography, Thin Layer
3.
Can J Microbiol ; 67(2): 119-137, 2021 Feb.
Article in English | MEDLINE | ID: mdl-32783775

ABSTRACT

Antimicrobial resistance is one of the leading challenges in the human healthcare segment. Advances in antimicrobial resistance have triggered exploration of natural alternatives to stabilize its seriousness. Antimicrobial peptides are small, positively charged oligopeptides that are as potent as commercially available antibiotics against a wide spectrum of organisms, such as Gram-positive bacteria, Gram-negative bacteria, viruses, and fungal strains. In addition to their antibiotic capabilities, these peptides possess anticancer activity, activate the immune response, and regulate inflammation. Peptides have distinct modes of action and fall into various categories due to their amino acid composition. Although antimicrobial peptides specifically target the bacterial cytoplasmic membrane, they can also target the cell nucleus and protein synthesis. Owing to the increasing demand for novel treatments against the threat of antimicrobial resistance, naturally synthesized peptides are a beneficial development concept. Antimicrobial peptides are pervasive and can easily be modified using de-novo synthesis technology. Antimicrobial peptides can be isolated from natural resources such as humans, plants, bacteria, and fungi. This review gives a brief overview of antimicrobial peptides and their diastereomeric composition. Other current trends, the future scope of antimicrobial peptides, and the role of d-amino acids are also discussed, with a specific emphasis on the design and development of new drugs.


Subject(s)
Amino Acids/chemistry , Drug Resistance, Microbial/drug effects , Pore Forming Cytotoxic Proteins/chemistry , Pore Forming Cytotoxic Proteins/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Cell Membrane/drug effects , Cell Nucleus/drug effects , Drug Development , Pore Forming Cytotoxic Proteins/chemical synthesis , Protein Biosynthesis/drug effects , Stereoisomerism
4.
West J Emerg Med ; 22(4): 943-950, 2021 Jul 15.
Article in English | MEDLINE | ID: mdl-35354002

ABSTRACT

INTRODUCTION: Traumatic intracranial hemorrhages (TIH) have traditionally been managed in the intensive care unit (ICU) setting with neurosurgery consultation and repeat head CT (HCT) for each patient. Recent publications indicate patients with small TIH and normal neurological examinations who are not on anticoagulation do not require ICU-level care, repeat HCT, or neurosurgical consultation. It has been suggested that these patients can be safely discharged home after a short period of observation in emergency department observation units (EDOU) provided their symptoms do not progress. METHODS: This study is a retrospective cross-sectional evaluation of an EDOU protocol for minor traumatic brain injury (mTBI). It was conducted at a Level I trauma center. The protocol was developed by emergency medicine, neurosurgery and trauma surgery and modeled after the Brain Injury Guidelines (BIG). All patients were managed by attendings in the ED with discretionary neurosurgery and trauma surgery consultations. Patients were eligible for the mTBI protocol if they met BIG 1 or BIG 2 criteria (no intoxication, no anticoagulation, normal neurological examination, no or non-displaced skull fracture, subdural or intraparenchymal hematoma up to 7 millimeters, trace to localized subarachnoid hemorrhage), and had no other injuries or medical co-morbidities requiring admission. Protocol in the EDOU included routine neurological checks, symptom management, and repeat HCT for progression of symptoms. The EDOU group was compared with historical controls admitted with primary diagnosis of TIH over the 12 months prior to the initiation of the mTBI protocols. Primary outcome was reduction in EDOU length of stay (LOS) as compared to inpatient LOS. Secondary outcomes included rates of neurosurgical consultation, repeat HCT, conversion to inpatient admission, and need for emergent neurosurgical intervention. RESULTS: There were 169 patients placed on the mTBI protocol between September 1, 2016 and August 31, 2019. The control group consisted of 53 inpatients. Median LOS (interquartile range [IQR]) for EDOU patients was 24.8 (IQR: 18.8 - 29.9) hours compared with a median LOS for the comparison group of 60.2 (IQR: 45.1 - 85.0) hours (P < .001). In the EDOU group 47 (27.8%) patients got a repeat HCT compared with 40 (75.5%) inpatients, and 106 (62.7%) had a neurosurgical consultation compared with 53 (100%) inpatients. Subdural hematoma was the most common type of hemorrhage. It was found in 60 (35.5%) patients, and subarachnoid hemorrhage was found in 56 cases (33.1%). Eleven patients had multicompartment hemorrhage of various classifications. Twelve (7.1%) patients required hospital admission from the EDOU. None of the EDOU patients required emergent neurosurgical intervention. CONCLUSION: Patients with minor TIH can be managed in an EDOU using an mTBI protocol and discretionary neurosurgical consults and repeat HCT. This is associated with a significant reduction in length of stay.


Subject(s)
Brain Injuries, Traumatic , Intracranial Hemorrhage, Traumatic , Brain Injuries, Traumatic/therapy , Clinical Observation Units , Cross-Sectional Studies , Humans , Retrospective Studies
5.
Emerg Med Clin North Am ; 37(3): 431-444, 2019 Aug.
Article in English | MEDLINE | ID: mdl-31262413

ABSTRACT

Acute hypoxemic respiratory failure (AHRF) is a common challenge in emergency medicine. Patient outcomes depend on interventions performed during preintubation, intubation, and postintubation. The article presents recommendations for evidence-based practice to optimally manage patients with AHRF and the acute respiratory distress syndrome.


Subject(s)
Hypoxia/therapy , Respiration, Artificial , Respiratory Insufficiency/therapy , Algorithms , Emergency Medicine , Extracorporeal Membrane Oxygenation , Fluid Therapy , Glucocorticoids/therapeutic use , Humans , Hypoxia/complications , Hypoxia/epidemiology , Neuromuscular Blocking Agents/therapeutic use , Oxygen Inhalation Therapy , Prone Position , Respiratory Distress Syndrome/therapy , Respiratory Insufficiency/epidemiology , Respiratory Insufficiency/etiology , Tidal Volume , Vasodilator Agents/therapeutic use , Ventilator-Induced Lung Injury/prevention & control
7.
BMJ Case Rep ; 20132013 Jul 31.
Article in English | MEDLINE | ID: mdl-23904416

ABSTRACT

We present a case of a 78-year-old African-American man with a history of hypertension, and with no prior history of seizure. The patient presented with hypertensive urgency as well as stroke such as symptoms of confusion, seizure, postictal confusion, left hemianopsia and hyponatraemia. MRI findings were suggestive of posterior reversible encephalopathy syndrome (PRES). The patient was treated with appropriate medications with the resolution of his stroke-like symptoms. This case report discusses a patient with PRES, in the setting of hyponatraemia, and how prompt recognition may prevent permanent neurological sequela such as epilepsy.


Subject(s)
Hyponatremia/complications , Posterior Leukoencephalopathy Syndrome/complications , Aged , Humans , Male
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