Relevant bibliographies by topics / Benzenesulfonamide

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Academic literature on the topic 'Benzenesulfonamide'

Author: Grafiati
Published: 4 June 2021
Last updated: 1 February 2022

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Journal articles on the topic "Benzenesulfonamide"

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Sheikh, Tahir Ali, Islam Ullah Khan, William T. A. Harrison, and Ejaz. "N-[3-(Benzenesulfonamido)propyl]benzenesulfonamide." Acta Crystallographica Section E Structure Reports Online 67, no. 7 (June 18, 2011): o1737. http://dx.doi.org/10.1107/s1600536811020150.

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Ashfaq, Muhammad, M. Nawaz Tahir, Islam Ullah Khan, Muhammad Nadeem Arshad, and Syed Saeed-ul-Hassan. "N-Acetyl-4-(benzenesulfonamido)benzenesulfonamide." Acta Crystallographica Section E Structure Reports Online 65, no. 5 (April 30, 2009): o1180. http://dx.doi.org/10.1107/s1600536809015876.

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Szafrański, Krzysztof, Jarosław Sławiński, Łukasz Tomorowicz, and Anna Kawiak. "Synthesis, Anticancer Evaluation and Structure-Activity Analysis of Novel (E)- 5-(2-Arylvinyl)-1,3,4-oxadiazol-2-yl)benzenesulfonamides." International Journal of Molecular Sciences 21, no. 6 (March 23, 2020): 2235. http://dx.doi.org/10.3390/ijms21062235.

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To learn more about the structure–activity relationships of (E)-3-(5-styryl-1,3,4-oxadiazol-2-yl)benzenesulfonamide derivatives, which in our previous research displayed promising in vitro anticancer activity, we have synthesized a group of novel (E)-5-[(5-(2-arylvinyl)-1,3,4-oxadiazol-2-yl)]-4-chloro-2-R1-benzenesulfonamides 7–36 as well as (E)-4-[5-styryl1,3,4-oxadiazol-2-yl]benzenesulfonamides 47–50 and (E)-2-(2,4-dichlorophenyl)-5-(2-arylvinyl)-1,3,4-oxadiazols 51–55. All target derivatives were evaluated for their anticancer activity on HeLa, HCT-116, and MCF-7 human tumor cell lines. The obtained results were analyzed in order to explain the influence of a structure of the 2-aryl-vinyl substituent and benzenesulfonamide scaffold on the anti-tumor activity. Compound 31, bearing 5-nitrothiophene moiety, exhibited the most potent anticancer activity against the HCT-116, MCF-7, and HeLa cell lines, with IC50 values of 0.5, 4, and 4.5 µM, respectively. Analysis of structure-activity relationship showed significant differences in activity depending on the substituent in position 3 of the benzenesulfonamide ring and indicated as the optimal meta position of the sulfonamide moiety relative to the oxadizole ring. In the next stage, chemometric analysis was performed basing on a set of computed molecular descriptors. Hierarchical cluster analysis was used to examine the internal structure of the obtained data and the quantitative structure–activity relationship (QSAR) analysis with multiple linear regression (MLR) method allowed for finding statistically significant models for predicting activity towards all three cancer cell lines.
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Bouz, Ghada, Martin Juhás, Lluis Pausas Otero, Cristina Paredes de la Red, Ondřej Janďourek, Klára Konečná, Pavla Paterová, et al. "Substituted N-(Pyrazin-2-yl)benzenesulfonamides; Synthesis, Anti-Infective Evaluation, Cytotoxicity, and In Silico Studies." Molecules 25, no. 1 (December 29, 2019): 138. http://dx.doi.org/10.3390/molecules25010138.

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We prepared a series of substituted N-(pyrazin-2-yl)benzenesulfonamides as an attempt to investigate the effect of different linkers connecting pyrazine to benzene cores on antimicrobial activity when compared to our previous compounds of amide or retro-amide linker type. Only two compounds, 4-amino-N-(pyrazin-2-yl)benzenesulfonamide (MIC = 6.25 μg/mL, 25 μM) and 4-amino-N-(6-chloropyrazin-2-yl)benzenesulfonamide (MIC = 6.25 μg/mL, 22 μM) exerted good antitubercular activity against M. tuberculosis H37Rv. However, they were excluded from the comparison as they—unlike the other compounds—possessed the pharmacophore for the inhibition of folate pathway, which was proven by docking studies. We performed target fishing, where we identified matrix metalloproteinase-8 as a promising target for our title compounds that is worth future exploration.
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Gowda, B. Thimme, Roopa Nayak, Jozef Kožíšek, Miroslav Tokarčík, and Hartmut Fuess. "Benzenesulfonamide." Acta Crystallographica Section E Structure Reports Online 63, no. 6 (May 26, 2007): o2967. http://dx.doi.org/10.1107/s1600536807024221.

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Gelbrich, Thomas, Terence L. Threlfall, and Michael B. Hursthouse. "Eight isostructural 4,4′-disubstitutedN-phenylbenzenesulfonamides." Acta Crystallographica Section C Crystal Structure Communications 68, no. 10 (September 21, 2012): o421—o426. http://dx.doi.org/10.1107/s0108270112039297.

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The isostructural crystals of 4-cyano-N-(4-methoxyphenyl)benzenesulfonamide, C14H12N2O3S, (I),N-(4-methoxyphenyl)-4-(trifluoromethyl)benzenesulfonamide, C14H12F3NO3S, (II), 4-iodo-N-(4-methoxyphenyl)benzenesulfonamide, C13H12INO3S, (III), 4-bromo-N-(4-methoxyphenyl)benzenesulfonamide, C13H12BrNO3S, (IV), 4-chloro-N-(4-methoxyphenyl)benzenesulfonamide, C13H12ClNO3S, (V), 4-fluoro-N-(4-methoxyphenyl)benzenesulfonamide, C13H12FNO3S, (VI),N-(4-chlorophenyl)-4-methoxybenzenesulfonamide, C13H12ClNO3S, (VII), and 4-cyano-N-phenylbenzenesulfonamide, C13H10N2O2S, (VIII), contain infinite chains composed of N—H...O(sulfonyl) hydrogen-bonded molecules. The crystal structures of (I)–(VIII) have been compared using theXPac software and quantitative descriptors of isostructurality were generated [Gelbrich, Threlfall & Hursthouse (2012).CrystEngComm,14, 5454–5464]. Certain isostructural relationships in this series involve molecules with substantially different spatial demands,e.g.(VI) and (VIII) are related by the simultaneous interchange of F→CN on the benzenesulfonamide ring and OMe→H on theN-phenyl ring, which indicates that the geometry of the three-dimensional crystal-packing mode of (I)–(VIII) is unusually adaptable to different molecular shapes.
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Loughrey, Bradley T., Michael L. Williams, and Peter C. Healy. "4-(Benzylideneamino)benzenesulfonamide." Acta Crystallographica Section E Structure Reports Online 65, no. 9 (August 8, 2009): o2087. http://dx.doi.org/10.1107/s1600536809030256.

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Wang, Shu-Yan, Wan-Cheng Guo, and Ning Ma. "2-(Hydrazinocarbonyl)benzenesulfonamide." Acta Crystallographica Section E Structure Reports Online 63, no. 7 (June 15, 2007): o3192. http://dx.doi.org/10.1107/s1600536807027584.

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Chang, Jun, Tie-Jun Zhang, Chang-Xiao Liu, and Xue-Ming Zhao. "N-(2,4-Dimethylphenyl)benzenesulfonamide." Acta Crystallographica Section E Structure Reports Online 63, no. 9 (August 3, 2007): o3670. http://dx.doi.org/10.1107/s160053680703677x.

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Ibrahim, Saba, M. Nawaz Tahir, Nadeem Iqbal, Durre Shahwar, and Muhammad Asam Raza. "N-(4-Methoxyphenyl)benzenesulfonamide." Acta Crystallographica Section E Structure Reports Online 67, no. 2 (January 8, 2011): o298. http://dx.doi.org/10.1107/s1600536811000365.

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Dissertations / Theses on the topic "Benzenesulfonamide"

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Čapkauskaitė, Edita. "Synthesis of carbonic anhydrase inhibitors and analysis of their structure - activity relationship." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2012. http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2012~D_20121211_095540-78760.

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The aim of this work was formulated - the synthesis of potent human carbonic anhydrase inhibitors, and their structure - activity study. The synthesized 136 new compounds were subjected to the studies of their inhibitory activity towards CA I, II, VII, XII and XIII (VU IBT). An efficient method for N-and S-alkylation of heterocyclic compounds (benzimidazole), S-alkylation of heterocyclic and aromatic compounds (imidazole, benzothiazole, benzimidazothiadiazole, pyrimidine, benzenethiol) with 3 - and 4 - (bromoacetyl)benzenesulfonamides and 4 - and 5 - (bromoacetyl)-2-chlorobenzenesulfonamides has ben deveoped. 2-[(6-oksopyrimidine-2-yl)thio]acetylbenzenesulfonamides in dimethylsulfoxide solution were found to exists in two forms - open chain and cyclic. 4-(Hetarylmethylcarbonyl)benzenesulfonamides exibited more inhibitory potency to CA than the 3-(hetarylmethylcarbonyl)benzenesulfonamides. Among all compound studied S-alkylated benzenethiol derivatives exibit the best CA inhibitory properties, while 1,3-thiazole derivatives – the lowest. Sulfonamide group position on the benzene ring is more important for CA binding than the acidic properties of sulfonamide group. The inhibitors having the selectivity of any one CA were selected from synthesized compounds. Most of the compounds possess selectivity to CA I and CA XIII, while selectivity to CA XII almost is not observed. The benzenesulfonamide ring position in CA II active site is unique to each class of compounds as showed in... [to full text]
Šio darbo tikslas – potencialių žmogaus karboanhidrazių (CA) slopiklių sintezė ir jų struktūros – aktyvumo tyrimas. CA slopinimo tyrimams susintetinti 136 įvairiais heterociklais pakeisti benzensulfonamidai ir išmatuotas jų CA I, II, VI, XII ir XIII slopinimo aktyvumas (VU BTI mokslininkai). Paruoštos efektyvios benzimidazolų N- ir S-alkilinimo, imidazolų, benztiazolo, benzimidazotiadiazolo, pirimidinų, benzenalkiltiolių S-alkilinimo 3- ir 4-(bromacetil)benzensulfonamidais bei 4- ir 5-(bromacetil)-2-chlorbenzensulfonamidais metodikos. Nustatyta, kad [(6-oksopirimidin-2-il)tio]acetilbenzensulfonamidai tirpaluose egzistuoja atviroje ir ciklinėje formose. Ištyrus benzensulfonamidinio ir heterociklinio/aromatinio fragmentų struktūros įtaka CA slopinančioms savybėms nustatyta, kad benzensulfonamidinės dalies įtaka CA slopinančiam aktyvumui yra didesnė nei heterociklinės/aromatinės. Sulfonamidinės grupės padėties benzeno žiede įtaka jungimuisi prie CA yra reikšmingesnė nei sulfonamidinės grupės rūgštingumo įtaka. Tiriant atrankumą vienai CA nustatyta, kad iš visų junginių daugiausiai atrankių yra CA I ir XIII, o CA XII atrankių junginių beveik nėra. Daugiausiai kuriai nors CA atrankių junginių yra tarp 4-(hetarilmetilkarbonil)benzensulfonamidų, bei tarp 1,3-tiazolo ir benzenalkiltiolio darinių. Remiantis rentgenostruktūrine CA II, XII ir XIII kompleksų (VU BTI) su kai kuriais slopikliais analize, paaiškintas sumažėjęs junginių giminingumas CA XII, lyginant su CA II, sumažėjęs... [toliau žr. visą tekstą]
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Čapkauskaitė, Edita. "Karboanhidrazių slopiklių sintezė ir jų struktūros - aktyvumo tyrimas." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2012. http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2012~D_20121211_095550-70885.

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Šio darbo tikslas – potencialių žmogaus karboanhidrazių (CA) slopiklių sintezė ir jų struktūros – aktyvumo tyrimas. CA slopinimo tyrimams susintetinti 136 įvairiais heterociklais pakeisti benzensulfonamidai ir išmatuotas jų CA I, II, VI, XII ir XIII slopinimo aktyvumas (VU BTI mokslininkai). Paruoštos efektyvios benzimidazolų N- ir S-alkilinimo, imidazolų, benztiazolo, benzimidazotiadiazolo, pirimidinų, benzenalkiltiolių S-alkilinimo 3- ir 4-(bromacetil)benzensulfonamidais bei 4- ir 5-(bromacetil)-2-chlorbenzensulfonamidais metodikos. Nustatyta, kad [(6-oksopirimidin-2-il)tio]acetilbenzensulfonamidai tirpaluose egzistuoja atviroje ir ciklinėje formose. Ištyrus benzensulfonamidinio ir heterociklinio/aromatinio fragmentų struktūros įtaka CA slopinančioms savybėms nustatyta, kad benzensulfonamidinės dalies įtaka CA slopinančiam aktyvumui yra didesnė nei heterociklinės/aromatinės. Sulfonamidinės grupės padėties benzeno žiede įtaka jungimuisi prie CA yra reikšmingesnė nei sulfonamidinės grupės rūgštingumo įtaka. Tiriant atrankumą vienai CA nustatyta, kad iš visų junginių daugiausiai atrankių yra CA I ir XIII, o CA XII atrankių junginių beveik nėra. Daugiausiai kuriai nors CA atrankių junginių yra tarp 4-(hetarilmetilkarbonil)benzensulfonamidų, bei tarp 1,3-tiazolo ir benzenalkiltiolio darinių. Remiantis rentgenostruktūrine CA II, XII ir XIII kompleksų (VU BTI) su kai kuriais slopikliais analize, paaiškintas sumažėjęs junginių giminingumas CA XII, lyginant su CA II, sumažėjęs... [toliau žr. visą tekstą]
The aim of this work was formulated - the synthesis of potent human carbonic anhydrase inhibitors, and their structure - activity study. The synthesized 136 new compounds were subjected to the studies of their inhibitory activity towards CA I, II, VII, XII and XIII (VU IBT). An efficient method for N-and S-alkylation of heterocyclic compounds (benzimidazole), S-alkylation of heterocyclic and aromatic compounds (imidazole, benzothiazole, benzimidazothiadiazole, pyrimidine, benzenethiol) with 3 - and 4 - (bromoacetyl)benzenesulfonamides and 4 - and 5 - (bromoacetyl)-2-chlorobenzenesulfonamides has ben deveoped. 2-[(6-oksopyrimidine-2-yl)thio]acetylbenzenesulfonamides in dimethylsulfoxide solution were found to exists in two forms - open chain and cyclic. 4-(Hetarylmethylcarbonyl)benzenesulfonamides exibited more inhibitory potency to CA than the 3-(hetarylmethylcarbonyl)benzenesulfonamides. Among all compound studied S-alkylated benzenethiol derivatives exibit the best CA inhibitory properties, while 1,3-thiazole derivatives – the lowest. Sulfonamide group position on the benzene ring is more important for CA binding than the acidic properties of sulfonamide group. The inhibitors having the selectivity of any one CA were selected from synthesized compounds. Most of the compounds possess selectivity to CA I and CA XIII, while selectivity to CA XII almost is not observed. The benzenesulfonamide ring position in CA II active site is unique to each class of compounds as showed in... [to full text]
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Joly, Jean-Patrick. "Conception, synthèse et étude de nouvelles molécules bioactives. Propriétés antivirales et antimélanome." Thesis, Nice, 2013. http://www.theses.fr/2013NICE4129.

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Malgré des progrès importants réalisés ces dernières années, la lutte contre les infections virales (SIDA, hépatites etc.) et les cancers demeurent un problème de santé mondiale. Ce bref bilan met en évidence la nécessité de développer de nouvelles molécules pour contourner les limites des traitements disponibles actuellement. Cette thèse, articulée autour de trois grands thèmes, s’inscrit dans ce contexte. Nous avons d’abord mis au point de manière rationnelle de nouveaux ligands d’ARN capables de se lier sélectivement à certaines structures secondaires de type tige-boucle ou tige-renflement de l’ARN TAR du VIH-1. Ces ligands interagissent avec l’ARN grâce à l’action coopérative de deux motifs de reconnaissance : (i) une nucléobase modifiée qui peut reconnaitre spécifiquement une paire de base de l’ARN et (ii) des acides aminés qui agissent avec les bases non appariées de l’ARN. Ces deux motifs sont reliés grâce à une matrice aliphatique (ligands non nucléosidiques) ou une matrice 2-désoxyribose (ligands nucléosidiques). Des études biophysiques et biologiques ont été menés en collaboration avec l’équipe du Dr. L. Briant (CEAPBS, UMR5236-CNRS) pour connaitre leur activité antivirale et leur site d’interaction sur la cible. Nous avons ensuite développé des molécules de type benzènesulfonamide thiazoles pour cibler le mélanome résistant aux inhibiteurs de B-Raf. Des modulations effectuées sur ce squelette nous ont permis d’établir des relations structure/activité, en collaboration avec l’équipe de Dr. S. Rocchi (C3M, INSERM U895). Enfin, nous avons développé une stratégie de modification post-synthétique d’oligonucléotides en position anomérique par réaction clic
Despite significant progress made in recent years, the fight against viral infections (AIDS, Hepatitis, etc.) and cancer remains a global health problem. This brief summary underlines the need for new compounds in order to overcome the limitations of currently available drugs. To this end, the main objective of this thesis is to address these issues by the investigation of three major research projects. We first developed new RNA ligands that selectively bind to RNA secondary structures such as the stem-loop or the stem-bulge of HIV-1 TAR RNA. These ligands interact with RNA thanks to the presence of two RNA binding domains acting in a cooperative manner: (i) a modified nucleobase that can specifically recognize an RNA base pair and (ii) basic amino acids that interact with strong affinity with surrounding free RNA nucleobases. These two patterns are connected by an aliphatic matrix (non-nucleoside ligands) or a 2-desoxyribose matrix (nucleoside-based ligands). Biophysical and biological studies were conducted in collaboration with the team of Dr. L. Briant (CEAPBS, UMR5236-CNRS) in order to study their antiviral activity and their mode of action. We next developed new bioactive molecules featuring a thiazole benzenesulfonamide scaffold to target melanoma cells resistant to B-Raf inhibitors. The modular synthesis of a large number of analogs allowed us to establish the structure/activity relationships, in collaboration with the team of Dr. S. Rocchi (C3M, INSERM U895). Finally, we developed a straightforward and convenient strategy for post-synthetic modification of oligonucleotides at the anomeric position using click chemistry
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Glöckner, Steffen [Verfasser], and Klebe [Akademischer Betreuer]. "Thermodynamic, Kinetic and Crystallographic Investigations of Benzenesulfonamides as Ligands of Human Carbonic Anhydrase II / Steffen Glöckner ; Betreuer: Klebe." Marburg : Philipps-Universität Marburg, 2020. http://d-nb.info/1224046749/34.

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Bassetto, Júnior Carlos Alberto Zanutto. "Estudo da atividade bloqueadora de N-Alquilbenzenossulfonamidas em canais iônicos, com enfase em canais para potássio." Universidade Estadual Paulista (UNESP), 2016. http://hdl.handle.net/11449/140287.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
Esta tese teve como objetivo estudar as moléculas orgânicas (N-alquilbenzenossulfonamidas) como inibidoras de canais para potássio do tipo KV3.1, heterologamente expressos em células L-929. Com o presente estudo constatou-se que as moléculas, N-alquilbenzenossulfonamidas, produzem efeitos inibitórios sobre KV3.1. Através da técnica de whole cell patch clamp, observou-se que os valores de IC50 para as moléculas que bloquearam o canal foram 13,5 μM, 16,9 μM, 25,9 μM, 34,2 μM, 34,9 μM e 60 μM, respectivamente, para 4-cloro-3-nitro-N-butilbenzenossulfonamida (SMD2), 4-cloro-3-nitro-N-furfutilbenzenossulfonamida (SMD3), 4-[N-(3’aminopropil)-2-pirrolidona]-3-nitro-N-butilbenzenossulfonamida (SMD2_APP), 4-[N-(3’aminopropil)-2-pirrolidona]-3-nitro-N-furfurilbenzenossulfonamida (SMD3_APP), 4-cloro-N-butilbenzenossulfonamida (SMD2_SN) e 4-cloro-N-furfurilbenzenossulfonamida (SMD3_SN). O efeito de todas as moléculas mostrou-se reversível quanto à ligação com o canal e todas atuaram como bloqueadores de canal aberto. Em SMD2, molécula que mostrou o menor valor de IC50, observou-se um deslocamento de -8 mV em relação ao controle, nas curvas de condutância versus voltagem, nas cinéticas de ativação e na recuperação a partir da inativação em relação à voltagem. O SMD2 não alterou as constantes de tempo de desativação, embora tenha mudado as constantes de ativação e inativação, além de ter induzido o fenômeno de tail crossover. Observou-se que para potenciais mais despolarizados, ocorreu o alívio do bloqueio (Block Relief). Não foi observado o efeito da dependência do pH para o bloqueio e SMD2 não mudou a seletividade do canal. Constatou-se que pulsos despolarizantes de curta duração induzem efeitos menos intensos, ao passo que pulsos despolarizantes mais longos, produzem efeitos mais intensos de SMD2 sobre o canal. Além disso, foi observado que, quanto mais o canal é usado, ou seja, aberto, mais ele é bloqueado por SMD2. Todos esses dados sugerem que SMD2 não interage com o estado fechado e nem com o estado inativado do canal, mas sim com seu estado aberto, apresentando também um efeito dependente de uso. De um ponto de vista farmacológico, isso indica que SMD2 pode ser uma molécula importante na modulação da atividade dos canais KV3.1, presentes em células com altas frequências de disparos de potencial de ação, podendo constituir uma nova classe de moduladores farmacológicos desses canais.
This thesis had the aim of studying the organic molecules (N-alkylbenzenesulfonamides) that block KV3.1 potassium channel heterologously expressed in L-929 cells. It was found that N-alkylbenzenesulfonamides have restrained effects on KV3.1. Through the whole cell patch clamp technique, it was observed that the values of IC50, for molecules that block the channel, were 13,5 μM, 16,9 μM, 25,9 μM, 34,2 μM, 34,9 μM and 60 μM, respectively 4-Chloro-3-nitro-N-butylbenzenesulfonamide (SMD2), 4-Chloro-3-nitro-N-furfurylbenzene-sulfonamide (SMD3), 4-[N-(3′-Aminopropyl)-2-pyrrolidone]-3-nitro-N-butylbenzenesulfona-mide (SMD2_APP), 4-[N-(3′-Aminopropyl)-2-pyrrolidone]-3-nitro-N-furfurylbenzene-sulfonamide (SMD3_APP), 4-Chloro-N-butyllbenzenesulfonamide (SMD2_SN) e 4-Chloro-N-furfurylbenzenesulfonamide(SMD3_SN). The effect of all molecules was reversible regards to the linking with the channel and all act as open channel blocker. In SMD2, molecule which showed the smallest value of IC50, it was observed a displacement of -8 mV compared to control, for conductance curves versus voltage, for the kinetics of activation and for the recovery from inactivation in relation to voltage. SMD2 did not change the deactivation of time constants, although it changed the activation and inactivation constants, and more, SMD2 have induced tail crossover phenomenon. It was observed that, for more depolarized potentials, there was a block relief. It was not observed the effect of pH dependence for the block and SMD2 did not change the channel selectivity. It was observed that, short duration depolarizing pulses prompt less intense effects, whereas long duration depolarizing pulses prompt more intense effects of SMD2 on the channels. Furthermore, it was observed that the more the channel is used, in an open state, the more it is blocked by SMD2. All of these data suggest that SMD2 does not interact neither with the closed state nor the inactivated state of channel, but with its open state presenting an use-dependent manner, also showing a use-dependent effect. In a pharmacological point of view, this indicates that SMD2 may be an important molecule in the modulation of the activity in the KV3.1 channels, presents in cells with high frequency of firing of action potential and may constitute a new class of pharmacological modulators.
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Olusegun-Osoba, Elizabeth Oluwakemi. "Strategies towards the synthesis of 4-(3-methyl-but-1-enyl)-3,5,3',4'-tetrahydroxystilbene (arachidin-1) and resveratrol analogues." Thesis, University of Hertfordshire, 2015. http://hdl.handle.net/2299/17118.

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Stilbene phytoalexins such as resveratrol, 1, and the arachidins, including arachidin-1,2, are naturally synthesised by peanut (Arachis hypogaea) plants. The peanut phytoalexins are polyphenolic compounds consisting of a stilbene backbone, with a number of derivatives also possessing a prenyl moiety. These distinctive phytoalexins have gained attention, as they exhibit various biological activities, for instance arachidin-1, 2, has been reported to be more potent than resveratrol, 1, in the inhibition of lipopolysaccharide-induced expression of cyclooxygenase-2 (COX-2) and COX-2 mRNA, in vitro at doses that were low in cytotoxicity. Additionally the various arachidins have recently been shown to exhibit their anti-inflammatory properties, through the inhibition of a number of inflammatory mediator pathways. In this work, various routes into the synthesis of arachidin-1, 2, are described, via use of the Horner-Wadsworth-Emmons (HWE) reaction. Three different methodologies were explored, the first approach involving silyl ether (TIPS or TBDMS) protected benzaldehydes, proved unsuccessful due to cleavage of the silyl ether protecting groups, in basic and/or acidic conditions. This led to an alternative approach, whereby formation of the stilbene backbone proceeded via the regioselective demethylation of an acetal in the presence of sodium metal, subsequent electrophilic substitution using iodomethane and finally acetal hydrolysis of the acetal, gave the isolated aldehyde in moderate yield (52 %). Coupling of the aldehyde with the substituted benzylphosphonate, via the HWE reaction gave the desired trans-stilbene in good yield (86 %), however incorporation of the prenyl side chain proved to be challenging via the Wohl-Ziegler bromination. Further adaptation of the aforementioned route, whereby alkylation using diethyl iodomethylphosphonate, enabled the incorporation of the prenyl moiety and the subsequent construction of the trans-stilbene backbone, gave the 4-(3-methyl-but-1- enyl)-3,5,3',4'-tetramethoxystilbene, 3, albeit in poor yield (47 %). The final step involving demethylation using BBr3 gave arachidin-1, 2, also in poor yield (30 %), nevertheless this approach has been proved to be a successful route for the total synthesis of arachidin-1, 2, however optimised studies are required in order to obtain the desired compound in quantitative yields. Synthetic analogues of resveratrol, 1, are also known for their biological activities, including anti-inflammatory and chemopreventative properties. Recently, the anti-proliferative activity of a number of stilbenesulfonamides, against the National Cancer Institute's 60 (NCI-60) human tumour cell line has been reported. Furthermore, the anti-inflammatory effects of novel heterocyclic methylsulfone and sulfonamide analogues, via inhibition of the COX-2 protein have also been published, however both synthetic routes described require a total of six or seven steps, from the sulfanilamide and are limited to the synthesis of primary sulphonamides (SO2NH2). In this work, an efficient three step synthesis has been designed and successfully implemented, proceeding via chlorosulfonation of diethyl benzylphosphonate, to form the sulfonyl chloride intermediate. Aminolysis of the sulfonyl chloride intermediate was then performed, using a range of primary, secondary and cyclic alkyl amines, as well as aromatic amines; including ammonia, dimethylamine, morpholine and diphenylamine. Finally, formation of the stilbene backbone with various substituted aldehydes, via the HWE reaction offered a short, versatile and alternative route to the synthesis of novel primary, secondary and tertiary trans-stilbene benzenesulfonamides and heterocyclic analogues, in yields of 42 - 100 %. The activity of a selection of the synthesised stilbene benzenesulfonamides was evaluated against the human lung adenocarcinoma epithelial cell line (A549). Amongst the compounds tested, analysis of the data showed that the novel analogue, 4, was found to be the most potent compound, with a GI50 of 0.1 μM. Comparison with the previously published data found analogue, 4, to be approximately 500-fold more potent than the lead compound resveratrol, 1, (GI50 = 51.64 μM) and approximately twice as potent than 5-fluorouracil (GI50 = 0.189μM), a chemotherapy drug used to treat various forms of cancer 8. Overall, these results demonstrate that the total synthesis of trans-arachidin-1, 2, can be achieved via a five step methodology. A versatile route to the synthesis of novel stilbene benzenesulfonamides has also been successfully achieved, amongst the compounds synthesised one appears to show promising anticancer activity, and warrants further investigation (i.e. in vitro studies using other cancer cell lines, and the synthesis of additional compounds using analogue, 4, as a lead compound).
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Chen, Kuan-Yu, and 陳冠妤. "Design and Synthesis of Benzenesulfonamide Derivatives as Potential Cell Cycle Targeting Inhibitors." Thesis, 2001. http://ndltd.ncl.edu.tw/handle/42965097474336956258.

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碩士
國立臺灣大學
藥學研究所
89
This thesis is aimed to design and synthesize benzenesulfonamide derivatives as potential cell cycle inhibitors. There are two series of target compounds, which are carbazolylbenzenesulfonamides (23a-h) and phenylazoindolylbenzenesulfnamides (24a-c). Via Japp-Klingemann reaction, ethyl pyruvate o-nitrophenylhydrazone (26a,b) was prepared from 2-nitroaniline (27). The Fischer indolization of 26a,b gave ethyl 7-nitro-1H-indole-2-carboxylate (28). Hydrolysis of 28 gave 7-nitro-1H-indole-2-carboxylic acid (29), which was decarboxylated to form the key intermediate 7-nitro-1H-indole (30). Reduction of 30 then coupled with benzenesulfonyl chlorides to afford the corresponding indolylbenzenesulfonamides 21a-h. Condensation of 21a-h with hexane-2,5-dione gave the corresponding target compounds 23a-h. In addition, azo-coupling of 21b,d with benzenediazonium salts (34b,c) gave the target compounds 24a-c. The preliminary cytotoxicity assays of 23a-h and 24a-c exhibited potentiality against TSGH, Hepa G2, HT 29 and KB cell lines. More importantly, our designed compounds 23a-h and 24a-c are almost all more potent than the corresponding indole derivative 21a-h. In particular, N-(5,8-dimethyl-9H-carbazol-1-yl)-4-methoxybenzene-sulfonamide (23c) displayed excellent inhibitory activities with IC50 being 0.5, 0.4, 0.4 and 0.8 M against TSGH, Hepa G2, HT 29 and KB cell lines. The N-(5,8-dimethyl-9H-carbazol-1-yl)-4-methylbenzene-sulfonamide (23b) also showed good inhibitory activities with IC50 less than 2 M against all four cell lines. Both the electron-donating (23b,c and 23f) and electron-withdrawing (23d,e and 23g) 4-substituted compunds were more potent than the unsubstituted derivatives 23a. This result indicated a possible favorable effect from a para substituent. Target compounds 24a,c also displayed higher inhibitory potency than the corresponding indole derivatives 21d against TSGH, Hepa G2, HT 29 and KB cell lines. These results provided compelling evidence that target compounds 23 and 24 would be potential antitumor drug candidates which might aim at cell cycle.
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Lee, Hsueh-Yun, and 李學耘. "Design and Synthesis of 1,4-Dimethylcarbazole and Ellipticine Analogues Containing Benzenesulfonamide Moiety as Potential Anti-cancer Agents." Thesis, 2010. http://ndltd.ncl.edu.tw/handle/52140611308061909449.

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博士
臺灣大學
藥學研究所
98
Abstract An attempt to develop potent agents to arrest cell cycle, E7010 (6) was chosen as the lead compound. Based on conformational restriction approach, to constrain the secondary amine linkage between pyridine and benzene in E7010 was proposed. Accordingly, 1,4-dimethylcarbazole motif was considered to be an essential scaffold. In the result, 18a demonstrated activities against several cancer cell lines, especially for HeLa, HT-29 and Hep3B cancer cell lines with GI50 in the range of 0.02 to 0.07 µM. Besides, carbazolyl sulfonamide 26b also exhibited potent cytotoxic activities. It inhibited A549 cell with GI50 at 0.08 µM. Compounds containing methyl (22a) and ethyl (23a) on sulfonamide nitrogen lead to not only enhance the potency but also to provide better activities against AGS and PC-3 cell lines. Since ellipticine has a common skeleton of 1,4-dimethylcarbazole, to promote the activities of 18a, the 1,4-dimethylcarbazole of 18a was replaced with ellipticine. Therefore, ellipticine derivatives within benzenesulfonamide are developed. According to the initial biological assays, the attachment of benzenesulfonamide to ellipticine reduced the activities. Although ellipticine sulfonamide (30) didn’t demonstrate promising results, the research focus on the C-7 of ellipticine is still interesting. To explore the substituents on this position may provide opportunity to search potent anticancer agents. To improve the total synthesis of ellipticine based on Saxton’s approach, the one-pot synthesis of secondary amine 47 is considered to shorten the reaction time and improve the reaction yield compared to original approach. The long-lasting problematic low yield in the D-ring cyclization of ellipticine (27) by Saxton’s approach was dramatically improved through N-(1,4-dimethylcarbazol-3-ylmethyl)-N-tosylaminoacetaldehyde diethyl acetal (56) with microwave irradiation. The yield of D-ring cyclization of ellipticine was improved to 75%. The overall yield of ellipticne starting from indole was significantly increased by 25-folds. Microwave was also used in the synthesis of 9-bromoellipticine and 9-nitroellipticine. Hence, this new approach is superior to reported methods in yields, reaction time, and it provides efficient access to a broad spectrum of ellipticine derivatives.
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CHU, Heng-Feng, and 朱恒峰. "Evaluating the therapeutic potential of benzenesulfonamides on Alzheimer." Thesis, 2011. http://ndltd.ncl.edu.tw/handle/v544tx.

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Wu, Mine-Fong, and 吳旻峰. "Investigating the effects of phenylazo benzenesulfonamides on the structure related neurotoxicity of Aβ1-42." Thesis, 2008. http://ndltd.ncl.edu.tw/handle/10182421912193386390.

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碩士
國立陽明大學
生物藥學研究所
96
Alzheimer’s disease is the most common neuron degenerative disease with more than 20 million cases world wide. This disease is caused by misfolding and aggregation of a small peptide amyloid-��. In our study, we prepared Abeta1-42 fibrils and oligomers by artificially synthesized Abeta1-42 peptide in vitro. The structure and maturation processes were analyzed by atomic force microscopy. We found that Abeta1-42 oligomer was stacked into doughnut-like or globular structure, and Abeta1-42 fibril underwent a progressive maturation processe by self-twisting. The toxicological study showed that only Abeta1-42 oligomer, but not Abeta1-42 fibril, was toxic to immature primary rat cortical neurons and caused cell necrosis. We also proved that both Abeta1-42 fibril and oligomer attached to the immature-synaptic structure. However, only Abeta1-42 oligomer caused neurite fragmentation and induced aggregation of pre-synaptic protein synapsin I. Abeta1-42 oligomer also induced overexpression of NMDA receptor1 and microtubule associate protein tau. Our study on tau phosphorylation in the immature neurons also showed that Abeta1-42 oligomer induced tau hyper-phosphorylation. In the mature neurons, Abeta1-42 oligomer reduced NMDA-induced calcium influx and reduced the level of synapsin I. Six phenylazo benzenesulfonamide compounds were able to inhibit Abeta1-42 oligomer formation and protected neurons against Abeta1-42 oligomer-induced reducing of synapsin I.
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Book chapters on the topic "Benzenesulfonamide"

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Gooch, Jan W. "Butyl Benzenesulfonamide." In Encyclopedic Dictionary of Polymers, 101–2. New York, NY: Springer New York, 2011. http://dx.doi.org/10.1007/978-1-4419-6247-8_1735.

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Hirota, E., K. Kuchitsu, T. Steimle, J. Vogt, and N. Vogt. "76 C6H7NO2S Benzenesulfonamide." In Molecules Containing Three or Four Carbon Atoms and Molecules Containing Five or More Carbon Atoms, 247. Berlin, Heidelberg: Springer Berlin Heidelberg, 2014. http://dx.doi.org/10.1007/978-3-642-41504-3_207.

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Winkelmann, Jochen. "Diffusion coefficient of 4-amino-N-2-pyrimidinyl-benzenesulfonamide into water, tris(hydroxymethyl)-aminomethane and hydrogen chloride solution." In Diffusion in Gases, Liquids and Electrolytes, 1502. Berlin, Heidelberg: Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-540-73735-3_1272.

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Winkelmann, Jochen. "Diffusion coefficient of 4-amino-N-(4,6-dimethyl-2-pyrimidinyl)- benzenesulfonamide into water, tris(hydroxymethyl)-aminomethane and hydrogen chloride solution." In Diffusion in Gases, Liquids and Electrolytes, 1534. Berlin, Heidelberg: Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-540-73735-3_1303.

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Čapkauskaitė, Edita, and Daumantas Matulis. "Organic Synthesis of Substituted Chlorinated Benzenesulfonamides as Selective Inhibitors of Several CA Isoforms." In Carbonic Anhydrase as Drug Target, 143–52. Cham: Springer International Publishing, 2019. http://dx.doi.org/10.1007/978-3-030-12780-0_10.

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Dudutienė, Virginija, and Daumantas Matulis. "Organic Synthesis of Substituted Fluorinated Benzenesulfonamides as Selective Inhibitors of CA IX and Other Isoforms." In Carbonic Anhydrase as Drug Target, 153–61. Cham: Springer International Publishing, 2019. http://dx.doi.org/10.1007/978-3-030-12780-0_11.

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"Butyl benzenesulfonamide." In Encyclopedic Dictionary of Polymers, 139. New York, NY: Springer New York, 2007. http://dx.doi.org/10.1007/978-0-387-30160-0_1700.

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Navnath Pansare, Dattatraya, and Rohini Narayan Shelke. "Synthesis and Anticancer Evaluation of Benzenesulfonamide Derivatives." In Heterocycles - Synthesis and Biological Activities. IntechOpen, 2020. http://dx.doi.org/10.5772/intechopen.88139.

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Koutentis, P. A., and H. A. Ioannidou. "From -[2,2-Dichloro-2-phenyl-1-(thioacetylamino)ethyl]benzenesulfonamide." In Science of Synthesis Knowledge Updates KU 2010/4, 1. Georg Thieme Verlag KG, 2010. http://dx.doi.org/10.1055/sos-sd-111-00195.

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"4-[5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide." In Encyclopedia of Cancer, 2609. Berlin, Heidelberg: Springer Berlin Heidelberg, 2016. http://dx.doi.org/10.1007/978-3-662-46875-3_100050.

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Conference papers on the topic "Benzenesulfonamide"

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Szafrański, Krzysztof, Jarosław Sławiński, and Anna Kawiak. "Optimization of 4-chloro-5-[5-(2-arylvinyl)-1,3,4-oxadiazol-2-yl]benzenesulfonamide structure towards anticancer activity." In 5th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/ecmc2019-06318.

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Prokes, Jiri. "THE INFLUENCE OF CONDITIONS ON THE DEGRADATION OF SODIUM N-CHLORO-BENZENESULFONAMIDE AND SODIUM P-TOLUENESULFONAMIDE FROM INDUSTRIAL WASTEWATERS." In 14th SGEM GeoConference on ECOLOGY, ECONOMICS, EDUCATION AND LEGISLATION. Stef92 Technology, 2014. http://dx.doi.org/10.5593/sgem2014/b51/s20.099.

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Redda, Kinfe Ken, Madhavi Gangapuram, Suresh Eyunni, Bereket Mochona, Nelly Mateeva, and Tiffany W. Ardley. "Abstract 3903: Synthesis of substituted N-{4-[(2-hydroxyethyl)sulfanyl]-3,6-dihydropyridin-1(2h)-yl} benzamide/benzenesulfonamide as antiinflamatory and anticancer agents." In Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-3903.

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Farah, Said M., Madhavi Gangapuram, Nelly Mateeva, Bereket Mochona, Tiffany W. Ardley, and Kinfe K. Redda. "Abstract 3263: Synthesis of substituted N-(4-(6-methyl-1H-benzo[d]imidazol-2-yl)-5,6-dihydropyridin-1(2H)-yl) benzamide/benzenesulfonamide as anticancer agents." In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-3263.

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Iyappan, M., E. Dhineshkumar, and C. Anbuselvan. "Synthesis of Schiff based E-4-(((1H-indol-3-yl)methylene) amino)-N-(pyrimidin-2-yl)benzenesulfonamide it’s highly sensitive and selective of turn-on chemosensor for recognition of Pb2+ ion." In RECENT TRENDS IN PURE AND APPLIED MATHEMATICS. AIP Publishing, 2019. http://dx.doi.org/10.1063/1.5135199.

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