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1

Baraa G. Alani, Khulood S Salim, Alaa Saleh Mahdi, and Ahmed Alaa Al-Temimi. "Sulfonamide derivatives: Synthesis and applications." International Journal of Frontiers in Chemistry and Pharmacy Research 4, no. 1 (2024): 001–5. http://dx.doi.org/10.53294/ijfcpr.2024.4.1.0021.

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Sulfonamides belong to an important class of compounds which showed wide ranges of biological activities like antibacterial, antiviral, diuretic, hypo-glycemic, anticancer, anti-inflammatory and recently anti-covid-19. Over the last few decades, various pharmacological activities of sulfonamide conjugates were published. Moreover, many lead compounds with sulfonamide functionality are also in clinical trial for the treatment of various medical conditions. For these reasons, development of an efficient process for the synthesis of sulfonamides has always been in the focus for research in organi
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2

Sadawarte, Gautam, Samadhan Jagatap, Mukesh Patil, Vasant Jagrut, and Jamatsing Darbarsing Rajput. "Synthesis of substituted pyridine based sulphonamides as an antidiabetic agent." European Journal of Chemistry 12, no. 3 (2021): 279–83. http://dx.doi.org/10.5155/eurjchem.12.3.279-283.2118.

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This research work describes the synthesis of a new series of heterocyclic compounds, namely sulfonamide derivatives. Sulfonamides are a diverse class of organic compounds having significant and potent biological activities. Diverse synthetic methods have been engaged to build up its various derivatives for different biological functions. In this study, the production of novel pyridine-based heterocyclic compounds having sulfonamide moieties has been elaborated. The obtained sulfonamide-based pyridine scaffold was used to investigate their alpha-amylase inhibition activity. The structures of f
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3

Hossan, Aisha SM. "Synthesis of new thiophene dyes clubbed with sulfonamide for the creation of antibacterial polyester fabrics." Textile Research Journal 90, no. 3-4 (2019): 376–85. http://dx.doi.org/10.1177/0040517519868176.

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The current study targets to synthesize some new sulfonamido-hydroxythiophene dyes for dyeing polyester fabrics with estimated antibacterial activity. The structure of sulfonamide dyes was adapted by conducting with sulfadimidine and sulfamethaxole through the coupling reaction. The synthesized derivatives were established by spectroscopic tools (Fourier transform infrared spectroscopy, proton nuclear magnetic resonance). Hydroxy-thiophene-containing sulfonamides were utilized for dyeing polyester fabric. The prepared sulfonamido-hydroxythiophene dyes were applied on polyester fabrics after es
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4

Irfan, Ali, Laila Rubab, Mishbah Ur Rehman, et al. "Coumarin sulfonamide derivatives: An emerging class of therapeutic agents." Heterocyclic Communications 26, no. 1 (2020): 46–59. http://dx.doi.org/10.1515/hc-2020-0008.

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AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treat
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5

Supuran, Claudiu T. "Thienothiopyransulfonamides as Complexing Agents for the Preparation of Dual Carbonic Anhydrase Inhibitors." Metal-Based Drugs 2, no. 6 (1995): 327–30. http://dx.doi.org/10.1155/mbd.1995.327.

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Co(II); Zn(II) and Cu(II) complexes of two new sulfonamide carbonic anhydrase (CA) inhibitors, derivatives of thienothiopyran-2-sulfonamide, were prepared and characterized by analytic, spectroscopic, magnetic and conductimetric measurements. The new complexes are more potent CA inhibitors than the parent sulfonamides, with IC50 values around 0.1 nM, against isozyme CA II.
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6

Moskalik, Mikhail Yu, Vera V. Astakhova, and Bagrat A. Shainyan. "Oxidative sulfamidation as a route to N-heterocycles and unsaturated sulfonamides." Pure and Applied Chemistry 92, no. 1 (2020): 123–49. http://dx.doi.org/10.1515/pac-2018-1219.

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AbstractOxidative sulfamidation is a promising approach to the synthesis of numerous organic compounds, including N-heterocycles or unsaturated species having the sulfonamide group, which is a key structural motif of synthetic antimicrobial drugs. The formed products can undergo further reactions leading to a wide variety of functionalized sulfonamides. This review summarizes the current state of knowledge on the oxidative reactions of sulfonamides and their derivatives with unsaturated and CH-active compounds with an emphasis on dienes as substrates. This produces a diverse range of compounds
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7

Pastewska, Monika, Beata Żołnowska, Strahinja Kovačević, et al. "Modeling of Anticancer Sulfonamide Derivatives Lipophilicity by Chemometric and Quantitative Structure-Retention Relationships Approaches." Molecules 27, no. 13 (2022): 3965. http://dx.doi.org/10.3390/molecules27133965.

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Sulfonamides are a classic group of chemotherapeutic drugs with a broad spectrum of pharmacological action, including anticancer activity. In this work, reversed-phase high-performance liquid chromatography and biomimetic chromatography were applied to characterize the lipophilicity of sulfonamide derivatives with proven anticancer activities against human colon cancer. Chromatographically determined lipophilicity parameters were compared with obtained logP, employing various computational approaches. Similarities and dissimilarities between experimental and computational logP were studied usi
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8

Kamal, Mehnaz. "Synthesis, in silico toxicity prediction, and in vitro antibacterial activity of new 4-amino-N-arylbenzenesulfonamide derivatives." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 01 (2025): 63. https://doi.org/10.59467/ijhc.2025.35.63.

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A significant class of compounds with a variety of biological applications is sulfonamides. The present work deals with the synthesis of 4-amino-N-arylbenzenesulfonamide derivatives (1-8) by the reaction of acetanilide-4- sulfonyl chloride and 4-substituted arylamine followed by hydrolysis to deprotect the acetyl group and give free amino group. Using disc diffusion, the synthesized derivatives were tested for in vitro antibacterial activities against Pseudomonas aeruginosa and Staphylococcus aureus. Ampicillin was used as a reference standard drug. Prediction of chemical toxicity was determin
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9

Varani, Tania, Majid Abdouss, Parisa Azerang, and Azar Tahghighi. "Acetylenic Sulfones and Acetylenic Sulfonamide Analogs: A Novel and Preferable Antimicrobial Drugs Based on Computational Strategies." Journal of Computational Biophysics and Chemistry 21, no. 01 (2021): 115–22. http://dx.doi.org/10.1142/s2737416521410027.

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This study was done to report virtual screening and molecular docking studies of sulfacetamide derivatives as new antimicrobial drugs, belonging to the pharmacological class of sulfonamides. For this purpose, sulfonamide functional groups from a library of chemical structures were converted into acetylenic sulfone and acetylenic sulfonamide functional groups to introduce a new class of antimicrobial drugs with mechanisms of action of dihydropteroate synthase inhibitors (DHPS). Initially, a library of compounds containing approximately 170 acetylenic sulfone ligands was created by similarity se
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10

Azevedo-Barbosa, Helloana, Danielle Ferreira Dias, Lucas Lopardi Franco, Jamie Anthony Hawkes, and Diogo Teixeira Carvalho. "From Antibacterial to Antitumour Agents: A Brief Review on The Chemical and Medicinal Aspects of Sulfonamides." Mini-Reviews in Medicinal Chemistry 20, no. 19 (2020): 2052–66. http://dx.doi.org/10.2174/1389557520666200905125738.

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Sulfonamides have been in clinical use for many years, and the development of bioactive substances containing the sulfonamide subunit has grown steadily in view of their important biological properties such as antibacterial, antifungal, antiparasitic, antioxidant, and antitumour properties. This review addresses the medicinal chemistry aspects of sulfonamides; covering their discovery, the structure- activity relationship and the mechanism of action of the antibacterial sulfonamide class, as well as the physico-chemical and pharmacological properties associated with this class. It also provide
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11

Alshibl, Hanan M., Ebtehal S. Al-Abdullah, Mogedda E. Haiba, et al. "Synthesis and Evaluation of New Coumarin Derivatives as Antioxidant, Antimicrobial, and Anti-Inflammatory Agents." Molecules 25, no. 14 (2020): 3251. http://dx.doi.org/10.3390/molecules25143251.

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New pyranocoumarin and coumarin-sulfonamide derivatives were prepared and evaluated for their antioxidant, antimicrobial, and/or anti-inflammatory activities. Coumarin-sulfonamide compounds 8a–d demonstrated significant antioxidant activity, while 7c,d, 8c,d, and 9c,d exhibited antimicrobial activity equal to or higher than the standard antimicrobials against at least one tested microorganism. Regarding the anti-inflammatory testing, pyranocoumarins 2b, 3a,b and 5c and coumarin-sulfonamide compound 9a showed more potent antiproteinase activity than aspirin in vitro; however, five compounds wer
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12

Arrighi, Giulia, Adrián Puerta, Andrea Petrini, et al. "Squaramide-Tethered Sulfonamides and Coumarins: Synthesis, Inhibition of Tumor-Associated CAs IX and XII and Docking Simulations." International Journal of Molecular Sciences 23, no. 14 (2022): 7685. http://dx.doi.org/10.3390/ijms23147685.

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(1) Background: carbonic anhydrases (CAs) are attractive targets for the development of new anticancer therapies; in particular, CAs IX and XII isoforms are overexpressed in numerous tumors. (2) Methods: following the tail approach, we have appended a hydrophobic aromatic tail to a pharmacophore responsible for the CA inhibition (aryl sulfonamide, coumarin). As a linker, we have used squaramides, featured with strong hydrogen bond acceptor and donor capacities. (3) Results: Starting from easily accessible dimethyl squarate, the title compounds were successfully obtained as crystalline solids,
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13

Stenfors, Brock Anton, and Felix Nyuangem Ngassa. "The synthesis and crystallographic characterization of 4-methylbenzenesulfonamide derivatives." European Journal of Chemistry 12, no. 2 (2021): 109–16. http://dx.doi.org/10.5155/eurjchem.12.2.109-116.2064.

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The sulfonamide moiety is present among a variety of biologically significant compounds. A facile synthesis is necessary to produce a variety of sulfonamides with the potential to improve human health. Herein, we report a facile methodology for the synthesis of 4-methylbenzenesulfonamides, amenable to a broad range of nitrogen nucleophiles. Implementing a semi-miscible biphasic solvent system resulted in higher yields, decreased reaction times, and a simplified workup over preliminary methods. Additionally, the crystal structures of five novel sulfonamide compounds and two polymorphs, have bee
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14

Hughes, Robert, and Rolf H. Prager. "Potential GABAB Receptor Antagonists. VIII. The Synthesis of 3-Amino-N-aryl-2-hydroxy- propane-1-sulfonamides and Analogues of Baclofen Containing Nitro Groups." Australian Journal of Chemistry 50, no. 1 (1997): 19. http://dx.doi.org/10.1071/c96149.

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3-Amino-N-aryl-2-hydroxypropane-1-sulfonamides were synthesized by the reaction of the corresponding epoxy sulfonamide with sodium azide, followed by reduction to the corresponding amine. The synthesis of 3-nitropropan-1-amine and two 2-thienyl derivatives is also reported. 3-Amino-2-hydroxy-N-(4-nitrophenyl)propane-1-sulfonamide and 3-nitropropan-1-amine were found to be specific antagonists of GABA at the GABAB receptor. Substitution of the amino group by alkyl or aryl groups reduced the activity.
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15

Y. Saour, Kawkab, Ridha I. Al-Bayati, and Mohammed K. Hadi. "Synthesis of New Coumarin and 2-quinolone Derivatives with Expected Biological Activities." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) 21, no. 2 (2017): 42–50. http://dx.doi.org/10.31351/vol21iss2pp42-50.

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A series of new coumarin and N-amino-2-quinolone derivatives have been synthesized. The reaction of coumarin (1) with excess of Hydrazine hydrate 98% yielded 1-amino-2-quinolone (2), Compound (2) was reacted with different Sulfonyl chloride to yield Sulfonamides [ N-(2-oxoquinolin-1(2H)-yl) methane sulfonamide (3), N-(2-oxoquinolin-1(2H)-yl) Benzene sulfonamide (4) and 4-methyl-N-(2-oxoquinolin-1(2H)-yl) benzene sulfonamide (5) ], while reaction of 2-(4-methyl-2-oxo-2H-chromen-7-yloxy) acetic acid (8) with different amines yielded compounds [ 2-(4-methyl-2-oxo-2H-chromen-7-yloxy)-N-(2-oxoquino
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16

Zare, Abdolkarim, Alireza Hasaninejad, Ahmad Reza Moosavi Zare, Abolfath Parhami, Hashem Sharghi та Ali Khalafi-Nezhad. "Zinc oxide as a new, highly efficient, green, and reusable catalyst for microwave-assisted Michael addition of sulfonamides to α,β-unsaturated esters in ionic liquids". Canadian Journal of Chemistry 85, № 6 (2007): 438–44. http://dx.doi.org/10.1139/v07-050.

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A simple, clean, and efficient procedure for the green synthesis of some N-alkyl derivatives of sulfonamides is described. Microwave-assisted Michael addition of sulfonamides to α,β-unsaturated esters, in the presence of catalytic amount of zinc oxide (ZnO) in 1-butyl-3-methylimidazolium bromide ([bmim]Br), affords the title compounds in high yields and short reaction times.Key words: zinc oxide, green chemistry, microwave, Michael addition, sulfonamide, ionic liquid.
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17

Supuran, Claudiu, Alessio Innocenti, Antonio Mastrolorenzo, and Andrea Scozzafava. "Antiviral Sulfonamide Derivatives." Mini-Reviews in Medicinal Chemistry 4, no. 2 (2004): 189–200. http://dx.doi.org/10.2174/1389557043487402.

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18

TUĞRAK SAKARYA, Mehtap, Halise İnci GÜL, Cem YAMALI, Yeliz DEMİR, and İlhami GÜLÇİN. "İMİDAZOLİNON BAZLI SÜLFONAMİD TÜREVLERİ: SENTEZ, KARAKTERİZASYON VE BAZI METABOLİK ENZİMLERE KARŞI İNHİBİTÖR ÖZELLİKLERİ." Ankara Universitesi Eczacilik Fakultesi Dergisi 47, no. 3 (2023): 21. http://dx.doi.org/10.33483/jfpau.1311157.

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Objective: The purpose of the work was to investigate new synthetic compounds of imidazolinone-based sulfonamide derivatives as potent and selective enyzme inhibitors. A number of compounds synthesized and their inhibitory action against acetylcholine esterase (AChE), and human (h) carbonic anhydrase (CA) isoforms I and II were investigated. Material and Method: The identity of the compounds has been confirmed by HRMS, 1H NMR, and 13C NMR. The pharmacological potential of the compounds has been determined by in vitro enzyme-based assays. Result and Discussion: In this study, a series of imidaz
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19

Stephenson, Rachel J., Fran Wolber, Paul G. Plieger та David R. K. Harding. "Synthesis and Characterization of Bradykinin Derivatives Based on a β-Cyclodextrin Core". Australian Journal of Chemistry 69, № 3 (2016): 328. http://dx.doi.org/10.1071/ch15460.

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Mono-6A-fluorenylmethyloxycarbonylamino-mono-6X-succinyl-β-cyclodextrin (1), an amino acid-based bi-functionalized derivative of β-cyclodextrin (β-CD), has been functionalized with the bioactive peptide, bradykinin and/or sulfonamides using fluorenylmethyloxycarbonyl (Fmoc) solid phase peptide synthesis (SPPS). The all-in-one molecule contains a carrier (cyclodextrin), targeting agent (bradykinin), and/or model drug (sulfonamide). Varying combinations of these bradykinin-focussed molecules have been synthesized using Fmoc SPPS on Rink amide resin. The positioning of the sulfonamide group, the
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20

Fantacuzzi, Marialuigia, Marialucia Gallorini, Nicola Gambacorta, et al. "Design, Synthesis and Biological Evaluation of Aromatase Inhibitors Based on Sulfonates and Sulfonamides of Resveratrol." Pharmaceuticals 14, no. 10 (2021): 984. http://dx.doi.org/10.3390/ph14100984.

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A library of sulfonate and sulfonamide derivatives of Resveratrol was synthesized and tested for its aromatase inhibitory potential. Interestingly, sulfonate derivatives were found to be more active than sulfonamide bioisosteres with IC50 values in the low micromolar range. The sulfonate analogues 1b–c and 1j exhibited good in vitro antiproliferative activity on the MCF7 cell line, evidenced by MTT and LDH release assays. Structure–activity relationships suggested that electronic and lipophilic properties could have a different role in promoting the biological response for sulfonates and sulfo
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21

Moskalik, Mikhail Yu. "Sulfonamides with Heterocyclic Periphery as Antiviral Agents." Molecules 28, no. 1 (2022): 51. http://dx.doi.org/10.3390/molecules28010051.

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Sulfonamides are the basic motifs for a whole generation of drugs from a large group of antibiotics. Currently, research in the field of the new sulfonamide synthesis has received a “second wind”, due to the increase in the synthetic capabilities of organic chemistry and the study of their medical and biological properties of a wide spectrum of biological activity. New reagents and new reactions make it possible to significantly increase the number of compounds with a sulfonamide fragment in combination with other important pharmacophore groups, such as, for example, a wide class of N-containi
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22

DOMINGUES, M. ROSÁRIO M., M. GRAÇA SANTANA-MARQUES, A. J. FERRRER-CORREIA, AUGUSTO C. TOMÉ, MARIA G. P. M. S. NEVES, and JOSÉ A. S. CAVALEIRO. "Liquid Secondary Ion Mass Spectrometry and Collision-induced Dissociation Mass Spectrometry of Sulfonamide Derivatives of meso-Tetraphenylporphyrin." Journal of Porphyrins and Phthalocyanines 03, no. 03 (1999): 172–79. http://dx.doi.org/10.1002/(sici)1099-1409(199903)3:3<172::aid-jpp118>3.0.co;2-c.

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Liquid secondary ion mass spectrometry (LSIMS) and collision-induced dissociation (CID) were used for the characterization of sulfonamide derivatives of meso-tetraphenylporphyrin (TPP). The spectra obtained using LSIMS show abundant molecular ions and fragment ions from losses of the sulfonamide moieties. The main fragmentation observed in the LSI mass spectra and in the CID spectra of the protonated or cationized molecules involves the loss of one sulfonamide group. In addition, in the CID spectra of these compounds the fragment ions formed by the elimination of two, three and/or four sulfona
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23

N. Omar, Tagreed. "Synthesis of Schiff Bases of Benzaldehyde and Salicylaldehyde as Anti-inflammatory Agents." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512) 16, no. 2 (2017): 5–11. http://dx.doi.org/10.31351/vol16iss2pp5-11.

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Three Schiff bases from Benzaldehyde and Salicylaldehyde have been synthesized (A, 1and 2) and two of them (1and 2) have been tested for anti-inflammatory activity. The p-aminobenzene sulfonamide has been synthesized from acetanilide through the addition of excess chlorosulfonic acid then concentrated ammonia solution; Schiff base of this derivative (2) exhibited good level of activity against egg-white induced edema in rat hind paw, while the other tested derivative exhibited no activity.&#x0D; Key words: Schiff bases, sulfonamide derivatives, salicylaldehyde
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24

Shukla, Karuna S. "Synthesis and Characterization of Aromatic-Heterocyclic Derivatives of Sulphonamides as Potential Antimicrobial Agents." International Journal of Pharmaceutical Sciences and Nanotechnology 7, no. 1 (2014): 2393–98. http://dx.doi.org/10.37285/ijpsn.2014.7.1.12.

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The incidence of microbial infection is increasing world-wide despite active research on the discovery and development of novel anti-microbial agents. Then emergence of multi-resistant strains of bacteria has increased the problem of drug resistance dramatically. The development and use of new anti-microbial agents is one of the ways to combat the emergence of anti-microbial resistance. The literature survey reveals that the sulfonamide derivatives as privileged pharmacophore for wide range of biological activities including anti-microbial activity. So a series of (3a-3e and 6a-6c) sulfonamide
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25

Komissarova, N. G., A. V. Orlov, and L. V. Spirikhin. "Synthesis of Betulonic and Betulinic Acids Derivatives with Sulfonamide Fragment Linked to the Triterpene Core by Amidoalkane Spaser." Žurnal obŝej himii 94, no. 6 (2024): 722–33. http://dx.doi.org/10.31857/s0044460x24060063.

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A series of potentially biologically active sulfonamides of betulonic and betulinic acids with a sulfonamide fragment containing residues of dibutylamine or N-heterocycles, which is linked to a triterpene core by an amidoethane or amidopropane spacer, was synthesized. Betulonic acid sulfonamides were obtained by chlorohydride conjugation of acid with 2-aminoethane and 3-aminopropanesulfonamides and used as precursor compounds for the transition to similar betulinic acid derivatives by selective reduction of the 3-keto group with the action of NaBH4 in EtOH. The structure of all synthesized tri
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26

Waheed, Saima, Fakiha Nazakat, Nasir Abbas, et al. "Synthesis of 2-(4-Methyl-Phenoxymethyl) Benzoic Acid; Cresol and its Metal Coordinate Complexes." FRONTIERS IN CHEMICAL SCIENCES 5, no. 2 (2024): 35–43. https://doi.org/10.52700/fcs.v5i2.98.

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A series of phenoxymethylbenzoic acid derivatives were synthesized by reacting p-cresol with phthalide. The resulting phenoxymethyl benzoic acid was converted into corresponding acid chloride by reacting with cyanuric chloride. These phenoxymethyl benzoyl chlorides were then reacted with various aminobenzenesulfonamides and synthesize d new sulfonamide derivatives. The targeted sulfonamides were subjected to structural characterization by contemporary spectroscopic techniques like UV-visible and FT-IR. The presence of a peak at 3400/cm confirmed the existence of amide functionality, and furthe
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27

Almarhoon, Zainab, Saied Soliman, Hazem Ghabbour, and Ayman El-Faham. "A Facile and Eco-Friendly Method for the Synthesis of Sulfonamide and Sulfonate Carboxylic Acid Derivatives—X-ray Structure, Hirshfeld Analysis and Spectroscopic Characterizations." Crystals 9, no. 1 (2019): 35. http://dx.doi.org/10.3390/cryst9010035.

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The search for a simple and efficient method for the synthesis of sulfonamide and sulfonate derivatives under mild and eco-friendly conditions is of continuing interest. Sulfonyl chlorides are still the best choice as starting materials for the preparation of target products. Here, we report a simple, efficient and eco-friendly method for the synthesis of sulfonamide and sulfonate carboxylic acid derivatives under green conditions using water and sodium carbonate as HCl scavengers to produce the products with high yields and purities. Two derivatives, 4-(tosyloxy)benzoic acid (5a) and 4-((4-me
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28

Mohamed, Abdel-Maboud I. "Spectrophotometric Determination of Some Benzene Sulfonamides with 7,7,8,8-Tetracyanoquinodimethane." Journal of AOAC INTERNATIONAL 72, no. 6 (1989): 885–89. http://dx.doi.org/10.1093/jaoac/72.6.885.

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Abstract A new spectrophotometric method for the determination of some unsubstituted benzene sulfonamides is presented. The method is based on the interaction of these derivatives with 7,7,8,8-tetracyanoquinodimethane at pH 9.0-9.5 to produce intense blue products. The quantitation of the products was carried out at 578 nm. Beer’s law was obeyed over a wide range of concentrations for all sulfonamide compounds studied. Optimum analytical conditions were determined, and the color produced was stable for at least 90 min at 25 °C. Analytical data for determination of sulfonamide compounds in pure
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29

Pacheco, Paulo Anastácio Furtado, Daniel Tadeu Gomes Gonzaga, Natalia Lidmar von Ranke, et al. "Synthesis, Biological Evaluation and Molecular Modeling Studies of Naphthoquinone Sulfonamides and Sulfonate Ester Derivatives as P2X7 Inhibitors." Molecules 28, no. 2 (2023): 590. http://dx.doi.org/10.3390/molecules28020590.

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ATP acts in the extracellular environment as an important signal, activating a family of receptors called purinergic receptors. In recent years, interest in the potential therapeutics of purinergic components, including agonists and antagonists of receptors, has increased. Currently, many observations have indicated that ATP acts as an important mediator of inflammatory responses and, when found in high concentrations in the extracellular space, is related to the activation of the P2X7 purinergic receptor. In this sense, the search for new inhibitors for this receptor has attracted a great dea
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30

Dash, Rudra Narayan, Alok Kumar Moharana, and Bharat Bhusan Subudhi. "Sulfonamides: Antiviral Strategy for Neglected Tropical Disease Virus." Current Organic Chemistry 24, no. 9 (2020): 1018–41. http://dx.doi.org/10.2174/1385272824999200515094100.

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The viral infections are a threat to the health system around the globe. Although more than 60 antiviral drugs have been approved by the FDA, most of them are for the management of few viruses like HIV, Hepatitis and Influenza. There is no antiviral for many viruses including Dengue, Chikungunya and Japanese encephalitis. Many of these neglected viruses are increasingly becoming global pathogens. Lack of broad spectrum of action and the rapid rise of resistance and cross-resistance to existing antiviral have further increased the challenge of antiviral development. Sulfonamide, as a privileged
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31

Liu, Zhi-Wei, Fan Liu, Chun-Tao Shao, Guo-Ping Yan, and Jiang-Yu Wu. "Synthesis and Characterization of Sulfonamide-Containing Naphthalimides as Fluorescent Probes." Molecules 29, no. 12 (2024): 2774. http://dx.doi.org/10.3390/molecules29122774.

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A tumor-targeting fluorescent probe has attracted increasing interest in fluorescent imaging for the noninvasive detection of cancers in recent years. Sulfonamide-containing naphthalimide derivatives (SN-2NI, SD-NI) were synthesized by the incorporation of N-butyl-4-ethyldiamino-1,8-naphthalene imide (NI) into sulfonamide (SN) and sulfadiazine (SD) as the tumor-targeting groups, respectively. These derivatives were further characterized by mass spectrometry (MS), nuclear magnetic resonance spectroscopy (1H NMR), Fourier transform infrared spectroscopy (FT-IR), ultraviolet–visible spectroscopy
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32

Hlotov, Serhii, Olga Shablykina, and Volodymyr Khilya. "4-(1-Oxo-1H-isochromen-3-yl)benzenesulfonamides and their effect on cancer cell growth." Ukrainica Bioorganica Acta 16, no. 2 (2021): 30–33. http://dx.doi.org/10.15407/bioorganica2021.02.030.

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Sulfonamide derivatives of 3-phenyl-1H-isochromen-1-one were synthesized by reaction of 4-(1-oxo-1H-isochromen-3-yl)benzenesulfonyl chloride with amines. The specific parameters of chlorosulfonation of 3-phenyl-1H-isochromen-1-one have been identified; the procedure for synthesis of 4-(1-oxo-1H-isochromen-3-yl)benzenesulfonyl chloride and its by-product (disulfochloride) was optimized. The evaluation of anticancer activity of obtained sulfonamides showed no appreciable cytotoxicity
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33

Prisyazhnyuk, Vladimir, Matthias Jachan, Irene Brüdgam, Reinhold Zimmer та Hans-Ulrich Reissig. "Addition of lithiated methoxyallene to aziridines – a novel access to enantiopure piperidine and β-amino acid derivatives". Collection of Czechoslovak Chemical Communications 74, № 7-8 (2009): 1069–80. http://dx.doi.org/10.1135/cccc2009012.

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Addition of lithiated methoxyallene to aziridine derivatives provided the expected primary addition products. The less substituted carbon of the aziridine ring was attacked selectively. The primary adducts could be converted to enantiopure piperidine derivatives or β-amino acid derivatives. The unexpected reactions lead to a tricyclic sulfonamide and to alkynyl-substituted aminoethers. The efficient two-step conversion of a piperidone derivative to a benzomorphan demonstrates the potential of this approach to biologically active compounds.
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34

Inagaki, Fuyuhiko, Shisen Hira, and Chisato Mukai. "Silver(I)-Catalyzed Deprenylation of Allylsulfonamide Derivatives." Synlett 28, no. 16 (2017): 2143–46. http://dx.doi.org/10.1055/s-0036-1589066.

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The silver(I)-catalyzed deprenylation of sulfonamide bearing prenyl functional groups on the nitrogen atom has been developed. In this reaction, the prenyl moiety was selectively eliminated without allyl or benzyl cleavage on the nitrogen atom. In addition, geranyl was also applicable for this elimination reaction. Furthermore, sulfonamide possessing two prenyl groups underwent a double deprenylation to form the corresponding deprenylated sulfonamide. Thus, a novel reactivity between the silver cation and double bond was observed.
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35

Allahyani, Mamdouh, Mazen Almehmadi, Osama Abdulaziz, et al. "Synthesis and in vitro antimicrobial screening of some 5-methyl-2-substituted phenyl-3- (phenylsulfonyl)thiazolidin-4-ones." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 04 (2024): 499. https://doi.org/10.59467/ijhc.2024.34.499.

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The synthesis of some new thiazolidine-sulfonamide derivatives was achieved in two steps. In the first step, appropriate aryl aldehyde reacted with benzene sulfonamide to yield N-arylidene benzene sulfonamide derivatives (1a-h). In the second step, compounds (1a-h) reacted with thiolactic acid to give the 5-methyl-2-substituted phenyl-3-(phenylsulfonyl) thiazolidin-4-one derivatives (2a-h). The compounds 2a-h were screened for their in vitro antimicrobial activity by agar disc diffusion method. The results showed that compounds 2b, 2c, and 2d exhibited anti-microbial activity against the teste
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36

Amira, E. Ali, Elmekabaty Ahmed, M. Elabbasy Hanaa, F. Atia Mohamed, E. Bad Gamila, and El-Aziz S. Fouda Abd. "Benzene Sulfonamide Derivatives as Inhibitors for Steel Dissolution in Sulfuric Acid Solution." Indian Journal of Science and Technology 16, no. 37 (2023): 3073–89. https://doi.org/10.17485/IJST/v16i37.259.

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Abstract <strong>Objectives:</strong>&nbsp;To examine the effectiveness of various benzene sulfonamide derivatives in preventing the corrosion of carbon steel in H2SO4 and to identify the dominating active form of the used compounds throughout the adsorption process in order to better understand the mechanism of their action.&nbsp;<strong>Methods:</strong>&nbsp;N-(4-(2-Aminothiazol-4-yl) phenyl) benzene sulfonamide (A) and N-(4-(2-thioxo-1, 2-dihydropyrimidim&mdash;4-yl) phenyl) benzene sulfonamide (B) were the tested compounds and were chosen based on molecular structure. To examine the effec
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37

Ma, Juan, and Guo-Hua Gong. "Discovery of Novel 3,4-Dihydro-2(1H)-Quinolinone Sulfonamide Derivatives as New Tubulin Polymerization Inhibitors with Anti-Cancer Activity." Molecules 27, no. 5 (2022): 1537. http://dx.doi.org/10.3390/molecules27051537.

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In this paper, a small series of novel quinoline sulfonamide derivatives was synthesized, and their structure of the target compounds were confirmed by 1H NMR and MS. The screening of the news target compounds’ in vitro cytotoxic activities against tumor cell lines by the MTT method was performed. Among them, compound D13 (N-(4-methoxybenzyl)-2-oxo-N-(3,4,5-trimethoxyphenyl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide exhibited the strongest inhibitory effect on the proliferation of HeLa (IC50: 1.34 μM), and this value correlated well with the inhibitory activities of the compound against tubuli
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38

Sajid Mahmood. "Design, Synthesis and Biological Assessment of N-Substituted Pronestyl Sulfonamide Analogues." Power System Technology 48, no. 1 (2024): 1062–71. https://doi.org/10.52783/pst.371.

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Pronestyl sulfonamide N-(2-(diethylamino)ethyl-4-(phenylsulfonamido)benzamide) and their derivatives were synthesized to check antibacterial activity. Procainamide (Pronestyl) was reacted with benzene sulphonyl chloride in the presence of 10% Na2CO3 at room temperature to form the product N-(2-(diethylamino)ethyl-4-(phenylsulfonamido)benzamide) (3). This synthesized compound was used further for the synthesis of pronestyl sulfonamide derivatives (5a-f) by the reaction of alkyl/aralkyl halides with Pronestyl sulfonamide by using LiH and DMF. The antibacterial activity of these compounds were pe
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39

Mikulová, Mária Bodnár, Dáša Kružlicová, Daniel Pecher, Claudiu T. Supuran, and Peter Mikuš. "Synthetic Strategies and Computational Inhibition Activity Study for Triazinyl-Substituted Benzenesulfonamide Conjugates with Polar and Hydrophobic Amino Acids as Inhibitors of Carbonic Anhydrases." International Journal of Molecular Sciences 21, no. 10 (2020): 3661. http://dx.doi.org/10.3390/ijms21103661.

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Various sulfonamide derivatives are intensively studied as anticancer agents owing to their inhibitory activity against human tumor-associated carbonic anhydrase isoforms. In this work, different synthetic procedures for the series of 1,3,5-triazinyl-aminobenzenesulfonamide conjugates with amino acids, possessing polar uncharged, negatively charged, and hydrophobic side chain, were studied and optimized with respect to the yield/purity of the synthesis/product as well as the time of synthetic reaction. These procedures were compared to each other via characteristic HPLC-ESI-DAD/QTOF/MS analyti
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40

Irfan, Ali, Sajjad Ahmad, Saddam Hussain, et al. "Recent Updates on the Synthesis of Bioactive Quinoxaline-Containing Sulfonamides." Applied Sciences 11, no. 12 (2021): 5702. http://dx.doi.org/10.3390/app11125702.

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Quinoxaline is a privileged pharmacophore that has broad-spectrum applications in the fields of medicine, pharmacology and pharmaceutics. Similarly, the sulfonamide moiety is of considerable interest in medicinal chemistry, as it exhibits a wide range of pharmacological activities. Therefore, the therapeutic potential and biomedical applications of quinoxalines have been enhanced by incorporation of the sulfonamide group into their chemical framework. The present review surveyed the literature on the preparation, biological activities and structure-activity relationship (SAR) of quinoxaline su
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41

Angeli, Andrea, Niccolò Paoletti, and Claudiu T. Supuran. "Five-Membered Heterocyclic Sulfonamides as Carbonic Anhydrase Inhibitors." Molecules 28, no. 7 (2023): 3220. http://dx.doi.org/10.3390/molecules28073220.

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The development of heterocyclic derivatives has progressed considerably over the past decades, and many new carbonic anhydrase inhibitors (CAIs) fall into this field. In particular, five-membered heterocyclic sulfonamides have been generally shown to be more effective inhibitors compared to six-membered rings ones. Despite the importance of oxygen and nitrogen five-membered heterocyclic aromatic rings in medicinal chemistry, the installation of sulfonamide moiety on such heterocycles has not received much attention. On the other hand, 1,3,4-thiadiazole/thiadiazoline ring-bearing sulfonamides a
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42

Hussein, Modather F. "New sulfonamide hybrids: synthesis, in vitro antimicrobial activity and docking study of some novel sulfonamide derivatives bearing carbamate/acyl-thiourea scaffolds." Mediterranean Journal of Chemistry 7, no. 5 (2018): 370–85. http://dx.doi.org/10.13171/mjc751912111445mh.

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In this study, the novel hybrids sulfonamide carbamates were synthesized by treatment of N-substituted 4-isothiocyanatophenyl sulfonamides with ethyl carbamate in dry 1,4-dioxane at reflux temperature in the presence of triethylamine. Also, treatment of Phenylacetylisothiocyanate with sulfanilamide in refluxing acetonitrile afforded the corresponding hybrid sulfonamide acylthiourea derivatives. The anti-microbial activities of the synthesized compounds were evaluated. Ethyl ({4-[(5-methyl-1,2-oxazol-3-yl)sulfamoyl)-phenyl]carbamothioyl)- carbamate and 2-Phenyl-N-((4-(N-thiazol-2-yl)sulfamoyl)-
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43

Hafez, Hend N., Sulaiman A. Alsalamah, and Abdel-Rhman B. A. El-Gazzar. "Synthesis of thiophene and N-substituted thieno[3,2-d] pyrimidine derivatives as potent antitumor and antibacterial agents." Acta Pharmaceutica 67, no. 3 (2017): 275–92. http://dx.doi.org/10.1515/acph-2017-0028.

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Abstract A novel series of carbamothioylamino-benzene-sulfonamide-thiophene-carboxylates 4a-c and thieno[3,2-d]pyrimidin-2-yl-amino-benzene-sulfonamides 5a-c were synthesized in a series of synthetic steps and were used as key intermediates for the synthesis of thienotriazolopyrimidine-benzene-sulfonamide derivatives 6a-c and 7a-c. Thieno[3,2-d]pyrimidinones (8 and 9) were also prepared. Compound 9 was used as an intermediate for the synthesis of imidazole/1,2,4-triazole and tetrazine functionalized thieno[3,2-d]pyrimidine derivatives (10–12). Pyrrole derivatives/pyrrolopyrimidine/pyrrolotriaz
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44

Takatsuki, Keigo, and Tadashi Kikuchi. "Gas Chromatographic-Mass Spectrometric Determination of Six Sulfonamide Residues in Egg and Animal Tissues." Journal of AOAC INTERNATIONAL 73, no. 6 (1990): 886–92. http://dx.doi.org/10.1093/jaoac/73.6.886.

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Abstract A gas chromatographlc-mass spectrometric method using selected Ion monitoring mode for simultaneous determination of 6 sulfonamides in egg and edible animal tissues has been developed. Sulfonamides are extracted from a sample with acetonltrlle. The extract Is passed through a silica cartridge column and concentrated. Dlazomethane in ether Is added to methylate sulfonamides. After evaporation, the residue Is dissolved In methylene chloride and cleaned up by silica gel column chromatography. The methylene chloride eluate containing sulfonamide-methyl derivatives Is evaporated to dryness
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45

Tsai, Chin-En, and Fusao Kondo. "Liquid Chromatographic Determination of Fluorescent Derivatives of Six Sulfonamides in Bovine Serum and Milk." Journal of AOAC INTERNATIONAL 78, no. 3 (1995): 674–78. http://dx.doi.org/10.1093/jaoac/78.3.674.

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Abstract A rapid and sensitive liquid chromatographic (LC) method with fluorometric detection was developed to detect sulfadiazine, sulfathiazole, sulfamethazine, sulfamonomethoxine, sulfamethoxazole, and sulfadimethoxine residues in bovine serum and milk. p-Aminobenzoic acid (PABA) was added as an internal standard. The sulfonamides were extracted from samples and derivatized with fluorescamine, and 50 μL was injected into a NovaPak C18 LC column and eluted with acetonitrile– 10 mM potassium phosphate (30 + 70, v/v). The sulfonamides were detected fluorometrically (excitation, 390 nm; emissio
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46

Ametsetor, Ebenezer, Kwabena Fobi, and Richard A. Bunce. "Synthesis and Elimination Pathways of 1-Methanesulfonyl-1,2-dihydroquinoline Sulfonamides." Molecules 28, no. 7 (2023): 3256. http://dx.doi.org/10.3390/molecules28073256.

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A series of new Morita–Baylis–Hillman acetates were prepared and reacted with methanesulfonamide (K2CO3, DMF, 23 °C) to produce tertiary dihydroquinoline sulfonamides in high yields. Subsequent efforts to eliminate the methylsulfonyl group from these derivatives (K2CO3, DMF, 90 °C) as a route to quinolines were met with mixed results. Although dihydroquinoline sulfonamides prepared from ethyl acrylate and acrylonitrile generally underwent elimination to give excellent yields of quinolines, those generated from 3-buten-2-one failed to undergo elimination and instead decomposed. The failure of t
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47

Zhang, Shu-Guang, Yu-Qiang Wan, Ya Wen, and Wei-Hua Zhang. "Novel Coumarin 7-Carboxamide/Sulfonamide Derivatives as Potential Fungicidal Agents: Design, Synthesis, and Biological Evaluation." Molecules 27, no. 20 (2022): 6904. http://dx.doi.org/10.3390/molecules27206904.

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Coumarin compounds have a variety of biological activities such as anti-tumor, anti-coagulation, anti-HIV, anti-fungal, and insecticidal. Amide and sulfonamide compounds have been used as fungicides for half a century, and dozens of varieties have been developed so far. This study focused on the introduction of carboxamide and sulfonamide moieties in a coumarin core to discover novel derivatives. Based on this strategy, we synthesized two series of novel carboxamide and sulfonamide substituted coumarin derivatives, and their fungicidal activity was also investigated. Some designed compounds po
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48

Gornowicz, Agnieszka, Anna Szymanowska, Mariusz Mojzych, Robert Czarnomysy, Krzysztof Bielawski, and Anna Bielawska. "The Anticancer Action of a Novel 1,2,4-Triazine Sulfonamide Derivative in Colon Cancer Cells." Molecules 26, no. 7 (2021): 2045. http://dx.doi.org/10.3390/molecules26072045.

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Cancer therapy is one of the most important challenges of modern medical and chemical sciences. Among the many methods of combating cancer, chemotherapy plays a special role. Imperfect modern chemotherapy justifies continuing the search for new, more effective, and safe drugs. Sulfonamides are the classic group of chemotherapeutic drugs with a broad spectrum of pharmacological activity. Recent literature reports show that sulfonamide derivatives have anti-tumor activity in vitro and in vivo. The aim of the study was to synthesize a novel 1,2,4-triazine sulfonamide derivative and check its anti
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49

Mader, Mary M., Chuan Shih, Eileen Considine, et al. "Acyl sulfonamide anti-proliferatives. Part 2: Activity of heterocyclic sulfonamide derivatives." Bioorganic & Medicinal Chemistry Letters 15, no. 3 (2005): 617–20. http://dx.doi.org/10.1016/j.bmcl.2004.11.041.

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50

Salisbury, Craig D. C., Jason C. Sweet, and Roger Munro. "Determination of Sulfonamide Residues in the Tissues of Food Animals Using Automated Precolumn Derivatization and Liquid Chromatography with Fluorescence Detection." Journal of AOAC INTERNATIONAL 87, no. 5 (2004): 1264–68. http://dx.doi.org/10.1093/jaoac/87.5.1264.

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Abstract A liquid chromatographic method for the determination of sulfachloropyridazine, sulfadiazine, sulfadimethoxine, sulfadoxine, sulfaethoxypyridazine, sulfamethazine, sulfaquinoxaline, and sulfathiazole residues in the muscle, liver, and kidney of food animals using sulfapyridine as internal standard is reported. Tissues are extracted using a modified version of AOAC Official Method 983.31 (Sulfonamide Residues in Animal Tissues). The sample extract is reconstituted in pH 3.0 buffer–acetonitrile (60 + 40) and filtered into an autosampler vial. Using a programmable autosampler of a liquid
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