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  1. Jamshed S, Bhagavathula AS, Zeeshan Qadar SM, Alauddin U, Shamim S, Hasan S
    Hosp Pharm, 2020 Oct;55(5):292-305.
    PMID: 32999499 DOI: 10.1177/0018578719893378
    Background: Gastroesophageal reflux disease (GERD) is a common gastrointestinal disorder that results from regurgitation of acid from the stomach into the esophagus. Treatment available for GERD includes lifestyle changes, antacids, histamine-2 receptor antagonists (H2RAs), proton pump inhibitors (PPIs), and anti-reflux surgery. Aim: The aim of this review is to assess the cost-effectiveness of the use of PPIs in the long-term management of patients with GERD. Method: We searched in PubMed to identify related original articles with close consideration based on inclusion and exclusion criteria to choose the best studies for this narrative review. The first section compares the cost-effectiveness of PPIs with H2RAs in long-term heartburn management. The other sections shall only discuss the cost-effectiveness of PPIs in 5 different strategies, namely, continuous (step-up, step-down, and maintenance), on-demand, and intermittent therapies. Results: Of 55 articles published, 10 studies published from 2000 to 2015 were included. Overall, PPIs are more effective in relieving heartburn in comparison with ranitidine. The use of PPIs in managing heartburn in long-term consumption of nonsteroidal anti-inflammatory drug (NSAID) has higher cost compared with H2RA. However, if the decision-maker is willing to pay more than US$174 788.60 per extra quality-adjusted life year (QALY), then the optimal strategy is traditional NSAID (tNSAID) and PPIs. The probability of being cost-effective was also highest for NSAID and PPI co-therapy users. On-demand PPI treatment strategy showed dominant with an incremental cost-effectiveness ratio of US$2197 per QALY gained and was most effective and cost saving compared with all the other treatments. The average cost-effectiveness ratio was lower for rabeprazole therapy than for ranitidine therapy. Conclusion: Our review revealed that long-term treatment with PPIs is effective but costly. To achieve long-term cost-effective approach, we recommend on-demand approach to treat heartburn symptoms, but if the symptoms persist, treatment with continuous step-down therapy should be applied.
  2. Shamim S, Awan MJ, Mohd Zain A, Naseem U, Mohammed MA, Garcia-Zapirain B
    J Healthc Eng, 2022;2022:6566982.
    PMID: 35422980 DOI: 10.1155/2022/6566982
    The coronavirus (COVID-19) pandemic has had a terrible impact on human lives globally, with far-reaching consequences for the health and well-being of many people around the world. Statistically, 305.9 million people worldwide tested positive for COVID-19, and 5.48 million people died due to COVID-19 up to 10 January 2022. CT scans can be used as an alternative to time-consuming RT-PCR testing for COVID-19. This research work proposes a segmentation approach to identifying ground glass opacity or ROI in CT images developed by coronavirus, with a modified structure of the Unet model having been used to classify the region of interest at the pixel level. The problem with segmentation is that the GGO often appears indistinguishable from a healthy lung in the initial stages of COVID-19, and so, to cope with this, the increased set of weights in contracting and expanding the Unet path and an improved convolutional module is added in order to establish the connection between the encoder and decoder pipeline. This has a major capacity to segment the GGO in the case of COVID-19, with the proposed model being referred to as "convUnet." The experiment was performed on the Medseg1 dataset, and the addition of a set of weights at each layer of the model and modification in the connected module in Unet led to an improvement in overall segmentation results. The quantitative results obtained using accuracy, recall, precision, dice-coefficient, F1score, and IOU were 93.29%, 93.01%, 93.67%, 92.46%, 93.34%, 86.96%, respectively, which is better than that obtained using Unet and other state-of-the-art models. Therefore, this segmentation approach proved to be more accurate, fast, and reliable in helping doctors to diagnose COVID-19 quickly and efficiently.
  3. Rafique R, Khan KM, Arshia, Chigurupati S, Wadood A, Rehman AU, et al.
    Bioorg Chem, 2020 01;94:103410.
    PMID: 31732193 DOI: 10.1016/j.bioorg.2019.103410
    Over-expression of α-amylase enzyme causes hyperglycemia which lead to many physiological complications including oxidative stress, one of the most commonly associated problem with diabetes mellitus. Marketed α-amylase inhibitors such as acarbose, voglibose, and miglitol used to treat type-II diabetes mellitus, but also linked to several harmful effects. Therefore, it is essential to explore new and nontoxic antidiabetic agents with additional antioxidant properties. In this connection, a series of new N-sulfonohydrazide substituted indazoles 1-19 were synthesized by multistep reaction scheme and assessed for in vitro α-amylase inhibitory and radical (DPPH and ABTS) scavenging properties. All compounds were fully characterized by different spectroscopic techniques including 1H, 13C NMR, EI-MS, HREI-MS, ESI-MS, and HRESI-MS. Compounds showed promising α-amylase inhibitory activities (IC50 = 1.23 ± 0.06-4.5 ± 0.03 µM) as compared to the standard acarbose (IC50 1.20 ± 0.09 µM). In addition to that all derivatives were found good to moderate scavengers of DPPH (IC50 2.01 ± 0.13-5.3 ± 0.11) and ABTS (IC50 = 2.34 ± 0.07-5.5 ± 0.07 µM) radicals, in comparison with standard ascorbic acid having scavenging activities with IC50 = 1.99 ± 0.09 µM, and IC50 2.03 ± 0.11 µM for DPPH and ABTS radicals. In silico molecular docking study was conducted to rationalize the binding interaction of α-amylase enzyme with ligands. Compounds were observed as mixed type inhibitors in enzyme kinetic characterization.
  4. Yeye EO, Kanwal, Mohammed Khan K, Chigurupati S, Wadood A, Ur Rehman A, et al.
    Bioorg Med Chem, 2020 06 01;28(11):115467.
    PMID: 32327353 DOI: 10.1016/j.bmc.2020.115467
    Thirty-three 4-amino-1,2,4-triazole derivatives 1-33 were synthesized by reacting 4-amino-1,2,4-triazole with a variety of benzaldehydes. The synthetic molecules were characterized via1H NMR and EI-MS spectroscopic techniques and evaluated for their anti-hyperglycemic potential. Compounds 1-33 exhibited good to moderate in vitro α-amylase and α-glucosidase inhibitory activities in the range of IC50 values 2.01 ± 0.03-6.44 ± 0.16 and 2.09 ± 0.08-6.54 ± 0.10 µM as compared to the standard acarbose (IC50 = 1.92 ± 0.17 µM) and (IC50 = 1.99 ± 0.07 µM), respectively. The limited structure-activity relationship suggested that different substitutions on aryl part of the synthetic compounds are responsible for variable activity. Kinetic study predicted that compounds 1-33 followed mixed and non-competitive type of inhibitions against α-amylase and α-glucosidase enzymes, respectively. In silico studies revealed that both triazole and aryl ring along with different substitutions were playing an important role in the binding interactions of inhibitors within the enzyme pocket. The synthetic molecules were found to have dual inhibitory potential against both enzymes thus they may serve as lead candidates for the drug development and research in the future studies.
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