Design, synthesis, molecular docking, antimicrobial, and antioxidant activities of new phenylsulfamoyl carboxylic acids of pharmacological interest

AbstractsThe research explores the facile synthesis of some new phenylsulfamoyl carboxylic acids, their molecular docking, antimicrobial, and antioxidant activities. The procedure involved the mild reaction of amino acids with benzenesulfonyl chloride in a medium of aqueous base. The compounds were characterized using FTIR,1H-NMR,13C-NMR, and an elemental analysis. They were tested for their antimicrobial activities against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, Salmonella typhi, Candida albicans, and Aspergillus niger microorganisms. The antioxidant activity of the compounds were measured in vitro by the inhibition of generated stable 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical. The molecular docking was carried out properly and five different disease conditions were studied, namely: trypanosomiasis, malaria, bacterial, fungal infections, and oxidative stress. From the results, compounds4c,4d,4e, and4g possess more excellent in vitro antibacterial and antifungal activities than the standard drug Ofloxacin used. Compound4e displayed the most excellent antioxidant activity. Compound4g showed significant 2D interaction with amino acid residue of urate oxidase fromAspergillus flavus complexed with uracil. Interestingly, compounds4a,4c,4d,4e, and4g exhibited excellent antibacterial, antifungal, antioxidant, antitrypanosome, and antimalaria activities comparable to the corresponding standard drugs such as Penicillin, Ketoconazole;...
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research

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This study evaluates the effects of different gum extraction methods on the mucoadhesive strengths of Abelmoschus esculentus (AE) and Irvingia gabonensis (IG) gums and the release of vaccine antigen in vaccine-gum formulations. AE and IG gums were extracted employing previously documented methods with acetone or sodium chloride (NaCl) and either oven-dried or freeze-dried. Gum extracts were analyzed for mucoadhesive strengths using a modified rotational cylinder method on animal mucosa. The time taken to detach from the mucosa was taken as the Peak Adhesion Time (PAT). The gum extracts were charged with Peste des petits ru...
Source: Journal of Immunoassay and Immunochemistry - Category: Biochemistry Tags: J Immunoassay Immunochem Source Type: research
In this study, an efficient pattern-join based algorithm is proposed to discover network motif in biological networks. The performance of the proposed algorithm is evaluated on the transcription regulatory network of Escherichia coli and the protein interaction network of Saccharomyces cerevisiae. The running time of the proposed algorithm outperforms most of the existing algorithms to discover large motifs.
Source: IET Systems Biology - Category: Biology Source Type: research
In humans, oxidative stress is involved in the development of diabetes, cancer, hypertension, Alzheimers' disease, and heart failure. One of the mechanisms in the cellular defence against oxidative stress is the activation of the Nrf2-antioxidant response element (ARE) signalling pathway. Computation of activity, efficacy, and potency score of ARE signalling pathway and to propose a multi-level prediction scheme for the same is the main aim of the study as it contributes in a big amount to the improvement of oxidative stress in humans. Applying the process of knowledge discovery from data, required knowledge is gathered an...
Source: IET Systems Biology - Category: Biology Source Type: research
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Source: American Journal of Translational Research - Category: Research Tags: Am J Transl Res Source Type: research
Authors: Wang LY, Yang PY, Chen YJ, Wu HD, Huang YH, Hsieh CH Abstract Because radiotherapy (RT) can induce diaphragm dysfunction, this study investigated the protective effect of inspiratory muscle training (IMT) on RT-induced diaphragm damage in patients with esophageal cancer during concurrent chemoradiotherapy (CCRT) in a preclinical setting, and an animal model was designed to confirm and explore the underlying mechanism. Six subjects who underwent CCRT were randomly enrolled in the control or concurrent-IMT group (n=3 per group). The training intensity was set to 30% maximal effort. The diaphragmatic function...
Source: American Journal of Translational Research - Category: Research Tags: Am J Transl Res Source Type: research
This study tested the hypothesis that early administration with cold water (CW)-assisted adipose-derived mesenchymal stem cell (ADMSC)-derived exosome (Exo) therapy was superior to either one on protecting the heart against ischemia-reperfusion (IR) (i.e., by ligation of 50 minutes and relieved by day 5 prior to euthanizing the animals) injury. Adult-male SD rats (n=30) were equally categorized into groups 1 (sham-operated control), 2 (IR), 3 (IR + CW), 4 (IR + Exo) and 5 (IR + CW-Exo). The left ventricular ejection fraction (LVEF) was highest in group 1, lowest in group 2, and significantly higher in group 5 than in group...
Source: American Journal of Translational Research - Category: Research Tags: Am J Transl Res Source Type: research
Abstract Giardia duodenalis is a cosmopolitan zoonotic protozoan parasite causing giardiasis, one of the most common diarrhoeal diseases in human and animals. Beyond its public health relevance, Giardia represents a valuable and fascinating model microorganism. The deep-branching phylogenetic position of Giardia, its simple life cycle and its minimalistic genomic and cellular organization provide a unique opportunity to define basal and "ancestral" eukaryotic functions. The eukaryotic 14-3-3 protein family represents a distinct example of phosphoserine/phosphothreonine-binding proteins. The extended netw...
Source: Advances in Parasitology - Category: Parasitology Authors: Tags: Adv Parasitol Source Type: research
Abstract A total of eight Giardia species are accepted. These include: Giardia duodenalis (syn. Giardia intestinalis and Giardia lamblia), which infects humans and animals, Giardia agilis, Giardia ardeae, Giardia psittaci, Giardia muris, Giardia microti, Giardia peramelis and G. cricetidarum, which infect non-human hosts including amphibians, birds, rodents and marsupials. Giardia duodenalis is a species complex consisting of eight assemblages (A-H), with assemblages A and B the dominant assemblages in humans. Molecular studies to date on the zoonotic potential of Giardia in animals are problematic and are hampere...
Source: Advances in Parasitology - Category: Parasitology Authors: Tags: Adv Parasitol Source Type: research
Abstract Infection with Giardia produces a wide range of clinical outcomes. Acutely infected patients may have no overt symptoms or suffer from severe cramps, diarrhea, nausea and even urticaria. Recently, post-infectious irritable bowel syndrome and chronic fatigue syndrome have been identified as long-term sequelae of giardiasis. Frequently, recurrent and chronic Giardia infection is considered a major contributor to stunting in children from low and middle income countries. Perhaps the most unusual outcome of infection with Giardia is the apparent reduced risk of developing moderate-to-severe diarrhea due to ot...
Source: Advances in Parasitology - Category: Parasitology Authors: Tags: Adv Parasitol Source Type: research
acute;a R Abstract During the course of giardiasis in humans and experimental models, G. duodenalis trophozoites express and secrete several proteins (ESPs) affecting structural, cellular and soluble components of the host intestinal milieu. These include the toxin-like molecules CRP136 and ESP58 that induce intestinal hyper-peristalsis. After the completion of the Giardia genome database and using up-to date transcriptomic and proteomic approaches, secreted 'virulence factors' have also been identified and experimentally characterized. This repertoire includes arginine deiminase (ADI) that competes for arginine, ...
Source: Advances in Parasitology - Category: Parasitology Authors: Tags: Adv Parasitol Source Type: research
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