13 research outputs found

    Knowledge and attitude towards antimicrobial self medication usage: a cross sectional study among medical and nursing students

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    Background: Antimicrobial drug resistance is a fast mounting universal crisis. Many factors like self medication, inappropriate use and unregulated sale of medicines and self medication have been attributed to this problem. The objective was to determine extend and causes of antimicrobial self medication and to compare the knowledge attitude of senior and junior medical/nursing students. Methods: We conducted a cross-sectional study on randomly selected 410 students from Baba Farid University of Health Sciences Faridkot, Punjab. A total sample of 220 medical students were enrolled from GGS Medical College, Faridkot (1st year students 50 and 170 above 1st year senior medical students ) and 190 nursing students were enrolled from University College of Nursing, Faridkot. Results: prevalence of antimicrobial self medication came out to be around 74%. The most common cause for seeking antimicrobial (self therapy) was upper respiratory tract infection. A statistical significant knowledge/attitude gap was found between senior and fresher medical/nursing students. Conclusions: High prevalence of antimicrobial self medication among medical/nursing students is a matter of concern and it should be discouraged at appropriate level to safeguard students from preventable adversary exposure.

    Deliberately losing control of C-H activation processes in the design of small molecule fragment arrays targeting peroxisomal metabolism

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    Combined photochemical arylation, “nuisance effect” (S N Ar) reaction sequences have been employed in the design of small arrays for immediate deployment in medium throughput X‐ray protein‐ligand structure determination. Reactions have been deliberately let “out of control,” in terms of selectivity; for example the ortho‐arylation of 2‐phenylpyridine gave five products resulting from mono‐, bis‐ arylations combined with S N Ar processes. As a result, a number of crystallographic hits against NUDT7, a key peroxisomal CoA ester hydrolase, have been identified

    7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists

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    High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat

    Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases

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    Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished NVP-QAV680, a highly selective compound with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development

    Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease

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    Mutations in the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) ion channel are established as the primary causative factor in the devastating lung disease cystic fibrosis (CF). More recently, cigarette smoke exposure has been shown to be associated with dysfunctional airway epithelial ion transport, suggesting a role for CFTR in the pathogenesis of Chronic Obstructive Pulmonary Disease (COPD). Here, the identification and characterization of a high throughput screening hit 6 as a potentiator of mutant human F508del and wild type CFTR channels is reported. The design, synthesis and biological evaluation of compounds 7 to 33 to establish structure activity relationships (SAR) of the scaffold are described, leading to the identification of clinical development compound icenticaftor (QBW251) 33, which has subsequently progressed to deliver two positive clinical proofs of concept in patients with CF and COPD and is now being further developed as a novel therapeutic approach for COPD patients
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