Displaying publications 1 - 20 of 82 in total

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  1. The chemical relationships of the sulphonamide group of drugs
    Caldwell AF
    Journal of the Malaya Branch of the British Medical Association, 1939;3:46-51.
    Matched MeSH terms: Sulfonamides
  2. Fast crystal growth of amorphous nimesulide: implication of surface effects
    Shi Q, Wang Y, Xu J, Liu Z, Chin CY
    Acta Crystallogr B Struct Sci Cryst Eng Mater, 2022 Feb 01;78(Pt 1):33-39.
    PMID: 35129118 DOI: 10.1107/S2052520621012749
    Understanding crystallization behaviors is of utmost importance for developing robust amorphous pharmaceutical solids. Herein, the crystal growth behaviors of amorphous anti-inflammatory drug nimesulide (NIME) are systemically investigated in the glassy and supercooled liquid state as a function of temperature. A sudden over-tenfold increase is observed in the bulk crystal growth of NIME on cooling below its glass transition temperature (Tg). This fast growth behavior is known as a glass-to-crystal (GC) mode and has been reported in some molecular glasses. Fast surface crystal growth of NIME can persist up to Tg + 57°C with a weak jump in its growth rates at 30-40°C. In addition, surface crystal growth and GC growth of NIME exhibit an almost identical temperature dependence, supporting the view that GC growth is indeed a surface-facilitated process. Moreover, the bubble-induced fast crystal growth of NIME is observed in the interior of its supercooled liquid with approximately the same growth kinetics as surface crystal growth. These findings are relevant for a full understanding of the surface-related crystallization behaviors and physical stability of amorphous pharmaceutical formulations.
    Matched MeSH terms: Sulfonamides*
  3. Green synthesis, characterization, and biochemical impacts of new bioactive isoxazoline-sulfonamides as potential insecticidal agents against the Sphodroxia maroccana Ley
    El Mahmoudi A, Fegrouche R, Tachallait H, Lumaret JP, Arshad S, Karrouchi K, et al.
    Pest Manag Sci, 2023 Dec;79(12):4847-4857.
    PMID: 37500586 DOI: 10.1002/ps.7686
    BACKGROUND: Sphodroxia maroccana Ley is a pest of cork oak crops that damages the roots of seedlings and can severely impair cork oak regeneration. Since the banning of carbosulfan and chlorpyriphos, which were widely used against the larvae of Sphodroxia maroccana because of their harmful impact on the environment, until now there has been no pesticide against these pests. Therefore, it is particularly urgent to develop highly effective insecticidal molecules with novel scaffolds. Isoxazolines are a class of insecticides that act on γ-aminobutyric acid (GABA)-gated chloride channel allosteric modulators. In this work, a green synthesis of novel 3,5-disubstituted isoxazoline-sulfonamide derivatives was achieved in water via ultrasound-assisted four-component reactions, and their insecticidal activities against fourth-instar larvae of S. maroccana were evaluated.

    RESULTS: Most of the tested compounds showed insecticidal activity compared to fluralaner as positive control and commercially available insecticide. Especially, the isoxazoline-secondary sulfonamides containing halogens (Br and Cl) on the phenyl group attached to the isoxazoline, 6g (LC50  = 0.31 mg/mL), 6j (LC50  = 0.38 mg/mL), 6k (LC50  = 0.18 mg/mL), 6L (LC50  = 0.49 mg/mL), 6m (LC50  = 0.24 mg/mL), 6q (LC50  = 0.46 mg/mL), exhibited much higher larvicidal activity than fluralaner (LC50  = 0.99 mg/mL).

    CONCLUSION: Novel isoxazolines containing sulfonamide moieties were designed, synthesized and confirmed by two single-crystal structures of 4e and 6q. Their bioassay results showed significant larvicidal activity with significant morphological changes in vivo. These results will lay the foundation for the further discovery and development of isoxazoline-sulfonamide derivatives as novel crop protection larvicides of cork oak. © 2023 Society of Chemical Industry.

    Matched MeSH terms: Sulfonamides/pharmacology
  4. Illuminating Insights: Clinical Study Harnessing Pharmacoscintigraphy for Permeation Study of Radiolabeled Nimesulide Topical Formulation in Healthy Human Volunteers
    Sharma N, Khanna K, Kumar N, Karwasra R, Janakiraman AK, Rajagopal MS
    Assay Drug Dev Technol, 2023 Oct;21(7):325-330.
    PMID: 37801663 DOI: 10.1089/adt.2023.053
    An alternative to oral administration for the delivery of therapeutic substances is the topical route, which frequently has comparable efficacy but may have a better tolerability profile. Gamma scintigraphy is a noninvasive technique that involves the application of radioactive substances to conduct biodistribution studies of therapeutic substances delivered through various routes. Nimesulide (NSD) was radiolabeled with technetium pertechnetate (Technetium99m [99mTc]) and this radiolabeled drug complex (99mTc-NSD) was used to prepare a topical gel formulation. The permeation of the radiolabeled drug from the topical gel was determined by gamma scintigraphy on human volunteers. The region of interest was calculated for the quantification of permeated radiolabeled drugs. This was observed that the mean percentage permeation of 99mTc-NSD was found to be 0.32 ± 0.22 to 36.37 ± 2.86 at 5 and 240 min. It was demonstrated that gamma scintigraphy may be a noninvasive and reliable technique for the determination of drug permeation through topical routes.
    Matched MeSH terms: Sulfonamides*
  5. The "sulphonamides"
    Johns BM
    Journal of the Malaya Branch of the British Medical Association, 1939;3:95-97.
    Matched MeSH terms: Sulfonamides
  6. Some impressions on the sulphanilamide compounds in the treatment of venereal diseases
    Diamond WCE
    Journal of the Malaya Branch of the British Medical Association, 1939;3:80-92.
    Matched MeSH terms: Sulfonamides
  7. Exploring chromone sulfonamides and sulfonylhydrazones as highly selective ectonucleotidase inhibitors: Synthesis, biological evaluation and in silico study
    Younus HA, Saeed M, Mahmood A, Jadoon MSK, Hameed A, Asari A, et al.
    Bioorg Chem, 2023 May;134:106450.
    PMID: 36924652 DOI: 10.1016/j.bioorg.2023.106450
    Ectonucleotidases, a well-known superfamily of plasma membrane located metalloenzymes plays a central role in mediating the process of purinergic cell signaling. Major functions performed by these enzymes include the hydrolysis of extracellular nucleosides and nucleotides which are considered as important cell-signaling molecules. Any (patho)-physiologically induced disruption in this purinergic cell signaling leads to several disorders, hence these enzymes are important drug targets for therapeutic purposes. Among the major challenges faced in the design of inhibitors of ectonucleotidases, an important one is the lack of selective inhibitors. Access to highly selective inhibitors via a facile synthetic route will not only be beneficial therapeutically, but will also lead to an increase in our understanding of intricate interplay between members of ectonucleotidase enzymes in relation to their selective activation and/or inhibition in different cells and tissues. Herein we describe synthesis of highly selective inhibitors of human intestinal alkaline phosphatase (h-IAP) and human tissue non-specific alkaline phosphatase (h-TNAP), containing chromone sulfonamide and sulfonylhydrazone scaffolds. Compound 1c exhibited highest (and most selective) h-IAP inhibition activity (h-IAP IC50 = 0.51 ± 0.20 µM; h-TNAP = 36.5%) and compound 3k showed highest activity and selective inhibition against h-TNAP (h-TNAP IC50 = 1.41 ± 0.10 µM; h-IAP = 43.1%). These compounds were also evaluated against another member of ectonucleotidase family, that is rat and human ecto-5'-nucleotidase (r-e5'NT and h-e5'NT). Some of the compounds exhibited excellent inhibitory activity against ecto-5'-nucleotidase. Compound 2 g exhibited highest inhibition against h-e5'NT (IC50 = 0.18 ± 0.02 µM). To rationalize the interactions with the binding site, molecular docking studies were carried out.
    Matched MeSH terms: Sulfonamides/pharmacology; Sulfonamides/chemistry
  8. Erythema exudativum multiforme following sulphonamide therapy
    D'ABRERA VS
    Med J Malaya, 1957 Dec;12(2):427-34.
    PMID: 13515874
    Matched MeSH terms: Sulfonamides/adverse effects*
  9. Sulphonamide packs in wounds
    Yeoh BC
    Journal of the Malaya Branch of the British Medical Association, 1941;5:72-6.
    Matched MeSH terms: Sulfonamides
  10. Synthesis and in silico studies of novel sulfonamides having oxadiazole ring: As β-glucuronidase inhibitors
    Taha M, Baharudin MS, Ismail NH, Selvaraj M, Salar U, Alkadi KA, et al.
    Bioorg Chem, 2017 04;71:86-96.
    PMID: 28160943 DOI: 10.1016/j.bioorg.2017.01.015
    Novel sulfonamides having oxadiazole ring were synthesized by multistep reaction and evaluated to check in vitro β-glucuronidase inhibitory activity. Luckily, except compound 13, all compounds were found to demonstrate good inhibitory activity in the range of IC50=2.40±0.01-58.06±1.60μM when compared to the standard d-saccharic acid 1,4-lactone (IC50=48.4±1.25μM). Structure activity relationship was also presented. However, in order to ensure the SAR as well as the molecular interactions of compounds with the active site of enzyme, molecular docking studies on most active compounds 19, 16, 4 and 6 was carried out. All derivatives were fully characterized by 1H NMR, 13C NMR and EI-MS spectroscopic techniques. CHN analysis was also presented.
    Matched MeSH terms: Sulfonamides/chemical synthesis; Sulfonamides/pharmacology*; Sulfonamides/chemistry*
  11. Synthesis of some new N-(alkyl/aralkyl)-N-(4-methoxyphenethyl) benzene sulfonamides as antibacterial agents against Escherichia
    Abbasi MA, Fatima Z, Rehman AU, Siddiqui SZ, Ali Shah SA, Shahid M, et al.
    Pak J Pharm Sci, 2019 Sep;32(5):1957-1964.
    PMID: 31813858
    The present study comprises the synthesis of a new series of benzenesulfonamides derived from N-sulfonation of 2-(4-methoxyphenyl)-1-ethanamine (1). The synthesis was initiated by the reaction of 2-(4-methoxyphenyl)-1-ethanamine (1) with benzenesulfonyl chloride (2), to yield N-(4-methoxyphenethyl)benzenesulfonamide (3). This parent molecule 3 was subsequently treated with various alkyl/aralkyl halides (4a-j) in N,N-dimethylformamide (DMF) and in the presence of a weak base lithium hydride (LiH) to obtain various N-(alkyl/aralkyl)-N-(4-methoxyphenethyl) benzenesulfonamides (5a-j). The characterization of these derivatives was carried out by spectroscopic techniques like IR, 1H-NMR, and 13C-NMR. Elemental analysis also supported this data. The biofilm inhibitory action of all the synthesized compounds was carried out on Escherichia coli and some of the compounds were identified to be very suitable inhibitors of this bacterial strain. Furthermore, the molecules were also tested for their cytotoxicity behavior to assess their utility as less cytotoxic therapeutic agents.
    Matched MeSH terms: Sulfonamides/chemical synthesis*; Sulfonamides/pharmacology*; Sulfonamides/chemistry
  12. The use of the sulphonamide group in gynaecology and midwifery
    English JS
    Journal of the Malaya Branch of the British Medical Association, 1939;3:93-94.
    Matched MeSH terms: Sulfonamides
  13. Peroxymonosulfate activation by a metal-free biochar for sulfonamide antibiotic removal in water and associated bacterial community composition
    Hung CM, Chen CW, Huang CP, Shiung Lam S, Dong CD
    Bioresour Technol, 2022 Jan;343:126082.
    PMID: 34610427 DOI: 10.1016/j.biortech.2021.126082
    Antibiotic sulfamethoxazole (SMX) has been commonly found in various water matrices, therefore effective decontamination method is urgently needed. Metal-free pristine coconut-shell-derived biochar (CSBC), synthesized by thermochemical conversion at 700 °C, was used for activating peroxymonosulfate (PMS), an oxidant, to degrade SMX, a sulfonamide antibiotic, in water. SMX degradation, maximized at 0.05 mM concentration, was 85% in 30 min at pH 5.0 in the presence of 150 mg L-1 of CSBC. Remarkably, SMX removal reached 99% in a chloride-rich CSBC/PMS system. SMX degradation was mainly attributed to the role of CSBC in enhancing PMS activation to produce combined radical (SO4•-/HO•) and nonradical (1O2) reaction pathways. The most abundant genus in the CSBC/PMS system was Methylotenera, which belonged to the Proteobacteria phylum. Thus, from a perspective of biowaste-to-resource recycling and circular bioeconomy view point, CSBC is a potential catalytic activator of PMS for the removal of sulfonamide antibiotics from aqueous environments.
    Matched MeSH terms: Sulfonamides
  14. Fulltext Does baricitinib reduce mortality and disease progression in SARS-CoV-2 virus infected patients? A systematic review and meta analysis
    Manoharan S, Ying LY
    Respir Med, 2022 Oct;202:106986.
    PMID: 36150282 DOI: 10.1016/j.rmed.2022.106986
    BACKGROUND: There are conflicting reports on the results of several of the latest clinical trials related to the use of baricitinib in the management of COVID-19 patients. The aim of the current systematic review and meta-analysis was to evaluate the efficacy of baricitinib in COVID-19 patients.

    METHODS: Databases like ScienceDirect, PubMed/Medline, Publons, Google Scholar and other sources like ClinicalTrials.gov, Cochrane, medRxiv, Research Square and reference lists were thoroughly searched.

    RESULTS: Fifteen (15) articles which met the inclusion criteria were qualitatively and quantitatively analysed. Based on Cochrane and Newcastle-Ottawa Scale (NOS) risk of bias (RoB) analyses, 14/15 articles are grouped as high-quality. Meta-analyses revealed that randomised control trials (RCTs) and non-randomised control trials (nRCTs) statistically significantly reduced the mortality rate in COVID-19 patients, with a risk ratio (RR) in the fixed-effect model was RR = 0.64 [95% CI: 0.51 to 0.79; p 

    Matched MeSH terms: Sulfonamides
  15. Synthesis, Bacterial biofilm inhibition and cytotoxicity of new N-Alkyl/aralkyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamides
    Abbasi MA, Zeb A, Rehman A, Siddiqui SZ, Shah SAA, Shahid M, et al.
    Pak J Pharm Sci, 2020 Jan;33(1):41-47.
    PMID: 32122829
    The current research was commenced by reaction of 1,4-benzodioxane-6-amine (1) with 4-nitrobenzenesulfonyl chloride (2) in the presence of aqueous base under dynamic pH control at 9 to yield N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamide (3) which was further reacted with a series of alkyl/aralkyl halides (4a-i) in polar aprotic solvent using catalytic amount of lithium hydride which acts as base to afford some new N-alkyl/aralkyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamides (5a-i). The projected structures of all the synthesized derivatives were characterized by contemporary techniques i.e., IR, 1H-NMR and EIMS. The biofilm Inhibitory action of all synthesized molecules was carried out against Escherichia coli and Bacillus subtilis. It was inferred from their results that 5f and 5e exhibited suitable inhibitory action against the biofilms of these bacterial strains. Moreover, their cytotoxicity was also checked and it was concluded that these synthesized molecules displayed docile cytotoxicity.
    Matched MeSH terms: Sulfonamides/chemical synthesis*; Sulfonamides/pharmacology*; Sulfonamides/toxicity*; Sulfonamides/chemistry
  16. Ureteroscopy: the first line treatment for distal located ureteral stones smaller than 10 mm
    Kamarulzaman MN
    Urol J, 2014 Nov 01;11(5):1914.
    PMID: 25361715
    Matched MeSH terms: Sulfonamides/therapeutic use*
  17. The role of pazopanib on tumour angiogenesis and in the management of cancers: A review
    Chellappan DK, Chellian J, Ng ZY, Sim YJ, Theng CW, Ling J, et al.
    Biomed Pharmacother, 2017 Dec;96:768-781.
    PMID: 29054093 DOI: 10.1016/j.biopha.2017.10.058
    Pazopanib is a relatively new compound to be introduced into the chemotherapy field. It is thought to have decent anti-angiogenic properties, which gives an additional hope for the treatment of certain types of cancers. A systematic review solely discussing about pazopanib and its anti-angiogenic effect is yet to be published to date, despite several relevant clinical trials being conducted over the recent years. In this review, we aim to investigate the mechanism of pazopanib's anti-angiogenic effect and its effectiveness in treating several cancers. We have included, in this study, findings from electronically searchable data from randomized clinical trials, clinical studies, cohort studies and other relevant articles. A total of 352 studies were included in this review. From the studies, the effect of pazopanib in various cancers or models was observed and recorded. Study quality is indefinite, with a few decent quality articles. The most elaborately studied cancers include renal cell carcinoma, solid tumors, advanced solid tumors, soft tissue sarcoma, breast cancer and gynecological cancers. In addition, several less commonly studied cancers are included in the studies as well. Pazopanib had demonstrated its anti-angiogenic effect based on favorable results observed in cancers, which are caused by angiogenesis-related mechanisms, such as renal cell carcinoma, solid tumors, advanced solid tumors and soft tissue sarcoma. This review was conducted to study, analyze and review the anti-angiogenic properties of pazopanib in various cancers. The results obtained can provide a decent reference when considering treatment options for angiogenesis-related malignancies. Furthermore, the definite observations of the anti-angiogenic effects of pazopanib could provide newer insights leading to the future development of drugs of the same mechanism with increased efficiency and reduced adverse effects.
    Matched MeSH terms: Sulfonamides/therapeutic use*
  18. Inhibition of choline kinase as an antiamoebic approach in Entamoeba histolytica infection
    Teh ZH, Lim BH, See Too WC, Few LL
    Trop Biomed, 2023 Dec 01;40(4):430-438.
    PMID: 38308830 DOI: 10.47665/tb.40.4.008
    Entamoeba histolytica is the parasite responsible for amoebiasis, which can result in amoebic colitis or amoebic liver abscess. Metronidazole has been the conventional treatment for intestinal amoebiasis, but concerns regarding resistance have emerged due to the identification of resistance pathways in E. histolytica. This study investigates a novel anti-amoebic approach targeting the CDP-choline pathway. Inhibition studies were conducted using potential choline kinase (CK) inhibitors to inhibit the EhCK enzyme, and RNA interference was employed to knock down the EhCK gene. Km and Vmax of purified EhCK and hCKa2 proteins were determined by pyruvate kinase-lactate dehydrogenase (PK-LDH) coupled assay. The IC50 values for EhCK and hCKa2 were determined with several commercial CK inhibitors. Selected inhibitors were incubated with E. histolytica trophozoites for 48 hours to determine the EC50 for each inhibitor. Silencing of gene encoding EhCK was carried out using duplex siRNA and the gene expression level was measured by real-time qPCR. Based on the IC50 values, three of the inhibitors, namely CK37, flavopiridol and H-89 were more potent against EhCK than hCKa2. Trophozoites growth inhibition showed that only HDTAB, H-89 and control drug metronidazole could penetrate and induce cell death after 48-hour incubation. siRNA concentration of 10 µg/mL was used for the transfection of positive control GAPDH, EhCK, and non-targeting GFP siRNAs. RNAi experiment concluded with positive control GAPDH downregulated by 99% while the level of EhCK mRNA was downregulated by 47%. In this study, potential inhibitors of EhCK and siRNA have been identified, paving the way for further refinement and testing to enhance their potency against EhCK while sparing hCK. The utilization of these specific inhibitors and siRNA targeting EhCK represents a novel approach to impede the growth of E. histolytica by disrupting its phospholipid synthesis pathway.
    Matched MeSH terms: Sulfonamides*
  19. Synthesis 4-[2-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-ethyl]-benzenesulfonamides with subnanomolar carbonic anhydrase II and XII inhibitory properties
    Bozdag M, Alafeefy AM, Carta F, Ceruso M, Al-Tamimi AS, Al-Kahtani AA, et al.
    Bioorg Med Chem, 2016 09 15;24(18):4100-4107.
    PMID: 27396930 DOI: 10.1016/j.bmc.2016.06.052
    Condensation of substituted anthranilic acids with 4-isothiocyanatoethyl-benzenesulfonamide led to series of heterocyclic benzenesulfonamides incorporating 2-mercapto-quinazolin-4-one tails. These sulfonamides were investigated as inhibitors of the human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms hCA I and II (cytosolic isozymes), as well as hCA XII (a transmembrane, tumor-associated enzyme also involved in glaucoma-genesis). The new sulfonamides acted as medium potency inhibitors of hCA I (KIs of 28.5-2954nM), being highly effective as hCA II (KIs in the range of 0.62-12.4nM) and XII (KIs of 0.54-7.11nM) inhibitors. All substitution patterns present in these compounds (e.g., halogens, methyl and methoxy moieties, in positions 6, 7 and/or 8 of the 2-mercapto-quinazolin-4-one ring) led to highly effective hCA II/XII inhibitors. These compounds should thus be of interest as preclinical candidates in pathologies in which the activity of these enzymes should be inhibited, such as glaucoma (CA II and XII as targets) or some tumors in which the activity of isoforms CA II and XII is dysregulated.
    Matched MeSH terms: Sulfonamides/chemical synthesis; Sulfonamides/pharmacology*; Sulfonamides/chemistry*
  20. A review on carbon-based biowaste and organic polymer materials for sustainable treatment of sulfonamides from pharmaceutical wastewater
    Zango ZU, Khoo KS, Garba A, Lawal MA, Abidin AZ, Wadi IA, et al.
    Environ Geochem Health, 2024 Apr 03;46(4):145.
    PMID: 38568460 DOI: 10.1007/s10653-024-01936-1
    Frequent detection of sulfonamides (SAs) pharmaceuticals in wastewater has necessitated the discovery of suitable technology for their sustainable remediation. Adsorption has been widely investigated due to its effectiveness, simplicity, and availability of various adsorbent materials from natural and artificial sources. This review highlighted the potentials of carbon-based adsorbents derived from agricultural wastes such as lignocellulose, biochar, activated carbon, carbon nanotubes graphene materials as well as organic polymers such as chitosan, molecularly imprinted polymers, metal, and covalent frameworks for SAs removal from wastewater. The promising features of these materials including higher porosity, rich carbon-content, robustness, good stability as well as ease of modification have been emphasized. Thus, the materials have demonstrated excellent performance towards the SAs removal, attributed to their porous nature that provided sufficient active sites for the adsorption of SAs molecules. The modification of physico-chemical features of the materials have been discussed as efficient means for enhancing their adsorption and reusable performance. The article also proposed various interactive mechanisms for the SAs adsorption. Lastly, the prospects and challenges have been highlighted to expand the knowledge gap on the application of the materials for the sustainable removal of the SAs.
    Matched MeSH terms: Sulfonamides
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