Esteban Aguilar-Llanos, Saskya E. Carrera-Pacheco, Rebeca González-Pastor, Johana Zúñiga-Miranda, Cristina Rodríguez-Pólit, J. C. Romero-Benavides, Jorge Heredia-Moya
{"title":"Synthesis and Evaluation of Biological Activities of Schiff Base Derivatives of 4-Aminoantipyrine and Cinnamaldehydes","authors":"Esteban Aguilar-Llanos, Saskya E. Carrera-Pacheco, Rebeca González-Pastor, Johana Zúñiga-Miranda, Cristina Rodríguez-Pólit, J. C. Romero-Benavides, Jorge Heredia-Moya","doi":"10.3390/ecsoc-26-13684","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13684","url":null,"abstract":"","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"10 3","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"120924864","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
P. Majerová, Dominika Pindjaková, Timotej Jankech, Ivana Gerhardtová, J. Kos, A. Kováč, J. Jampílek
: Recently, a series of thirty-eight 4-{[(benzyloxy)carbonyl]amino}-2-hydroxybenzoic acid amides designed as potential acetyl-and butyrylcholinesterase (AChE/BChE) inhibitors were described as potential drugs to alleviate the symptoms of Alzheimer’s disease (AD). Some of these compounds have shown promise for inhibiting either AChE or BChE. Since these compounds are structurally similar to agents inhibiting beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), the aim of the contribution was to verify how our compounds were able to affect this enzyme, which, when inhibited, blocks the formation of amyloid-β , but whose inhibition is associated with significant adverse effects in humans. At a concentration of 10 µ M, only benzyl {4-[(4-fluorophenyl)carbamoyl]-3-hydroxyphenyl}carbamate was found to show approximately 28% inhibition of BACE1 activity.
{"title":"Benzyl Carbamates of 4-Aminosalicylanilides as Possible BACE1 Modulators","authors":"P. Majerová, Dominika Pindjaková, Timotej Jankech, Ivana Gerhardtová, J. Kos, A. Kováč, J. Jampílek","doi":"10.3390/ecsoc-26-13680","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13680","url":null,"abstract":": Recently, a series of thirty-eight 4-{[(benzyloxy)carbonyl]amino}-2-hydroxybenzoic acid amides designed as potential acetyl-and butyrylcholinesterase (AChE/BChE) inhibitors were described as potential drugs to alleviate the symptoms of Alzheimer’s disease (AD). Some of these compounds have shown promise for inhibiting either AChE or BChE. Since these compounds are structurally similar to agents inhibiting beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), the aim of the contribution was to verify how our compounds were able to affect this enzyme, which, when inhibited, blocks the formation of amyloid-β , but whose inhibition is associated with significant adverse effects in humans. At a concentration of 10 µ M, only benzyl {4-[(4-fluorophenyl)carbamoyl]-3-hydroxyphenyl}carbamate was found to show approximately 28% inhibition of BACE1 activity.","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"12 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123657703","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Alejandro Corona-Díaz, Diana G. García García, Shirikant G. Pharande, Manuel A. Rentería-Gómez, Rocío Gámez-Montaño
{"title":"A One Pot Synthesis of Diketopiperazines via Multicomponent Reactions Based on Isocyanides","authors":"Alejandro Corona-Díaz, Diana G. García García, Shirikant G. Pharande, Manuel A. Rentería-Gómez, Rocío Gámez-Montaño","doi":"10.3390/ecsoc-26-13648","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13648","url":null,"abstract":"","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"131 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"127033762","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
: Aromatic heterocycles can be found in many molecules endowed with specific properties, in particular for applications in the fields of medicinal chemistry and materials science. In this group, we notably develop synthetic methodologies to selectively introduce iodine onto aromatic compounds and to use this heavy halogen in order to build heterocycles of interest. While we some-times employed direct iodinations on electron-enriched aromatic compounds, we mainly optimized deprotometallation–iodolysis sequences to functionalize substrates sensitive to nucleophilic attacks. In particular, hindered lithium amide–metal trap tandems have been designed to overcome the low tolerance of some functional groups (e.g., ketones or sensitive diazines) toward organolithiums. The aromatic iodides generated in these ways have been involved in transition metal–catalyzed cross-couplings to access original scaffolds (oxazoloquinoxalines, pyrazinoisatins, pyrazinocarbazoles, etc.). We specifically developed the use of aromatic iodides in the copper-mediated N -arylation of anilines, e.g., to reach triarylamines. Combined with subsequent cyclizations, these reactions allowed access to numerous heterocyclic compounds (such as acridones, acridines, other aza-aromatic polycycles and helicene-like structures) with potential applications. From some of the scaffolds obtained, biological evaluation in the frame of collaborations allowed properties of interest to be discovered (e
{"title":"Aromatic Iodides: Synthesis and Conversion to Heterocycles","authors":"F. Mongin, W. Erb, Frédéric Lassagne","doi":"10.3390/ecsoc-26-13641","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13641","url":null,"abstract":": Aromatic heterocycles can be found in many molecules endowed with specific properties, in particular for applications in the fields of medicinal chemistry and materials science. In this group, we notably develop synthetic methodologies to selectively introduce iodine onto aromatic compounds and to use this heavy halogen in order to build heterocycles of interest. While we some-times employed direct iodinations on electron-enriched aromatic compounds, we mainly optimized deprotometallation–iodolysis sequences to functionalize substrates sensitive to nucleophilic attacks. In particular, hindered lithium amide–metal trap tandems have been designed to overcome the low tolerance of some functional groups (e.g., ketones or sensitive diazines) toward organolithiums. The aromatic iodides generated in these ways have been involved in transition metal–catalyzed cross-couplings to access original scaffolds (oxazoloquinoxalines, pyrazinoisatins, pyrazinocarbazoles, etc.). We specifically developed the use of aromatic iodides in the copper-mediated N -arylation of anilines, e.g., to reach triarylamines. Combined with subsequent cyclizations, these reactions allowed access to numerous heterocyclic compounds (such as acridones, acridines, other aza-aromatic polycycles and helicene-like structures) with potential applications. From some of the scaffolds obtained, biological evaluation in the frame of collaborations allowed properties of interest to be discovered (e","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"59 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"132535703","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Isabel Velo-Heleno, Sandra Fernández-Fariña, Lara Rouco, M. Martínez‐Calvo, Rosa Pedrido
: Thiosemicarbazones are interesting organic skeletons due to their great coordinative versatility and their interesting biological and pharmacological properties, as well as their structural diversity. However, the isolation of their monovalent coinage metal complexes, such as Cu(I), Ag(I) and Au(I), is a partially studied field, since co-ligands with soft donor atoms such as phosphines are required. In this context, our research group has been studying a new family of ligands capable of stabilizing coinage complexes without the need for auxiliary co-ligands. To this end, it was decided to incorporate a phosphorus atom into the structure of a thiosemicarbazone kernel. This work presents the design, synthesis and structural characterization of a new phosphino-thiosemicarbazone ligand.
{"title":"Designing a Phosphino-Thiosemicarbazone Ligand Capable of Stabilizing Coinage Metal Ions","authors":"Isabel Velo-Heleno, Sandra Fernández-Fariña, Lara Rouco, M. Martínez‐Calvo, Rosa Pedrido","doi":"10.3390/ecsoc-26-13638","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13638","url":null,"abstract":": Thiosemicarbazones are interesting organic skeletons due to their great coordinative versatility and their interesting biological and pharmacological properties, as well as their structural diversity. However, the isolation of their monovalent coinage metal complexes, such as Cu(I), Ag(I) and Au(I), is a partially studied field, since co-ligands with soft donor atoms such as phosphines are required. In this context, our research group has been studying a new family of ligands capable of stabilizing coinage complexes without the need for auxiliary co-ligands. To this end, it was decided to incorporate a phosphorus atom into the structure of a thiosemicarbazone kernel. This work presents the design, synthesis and structural characterization of a new phosphino-thiosemicarbazone ligand.","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"2 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131012991","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Sadoqat Salimjanovna Khaydarova, Sevinch Qurolovna Siddikova, Alisher Khamidovich Khaitbaev
{"title":"Extraction of Sodium Alginate from Charophyceae Algae","authors":"Sadoqat Salimjanovna Khaydarova, Sevinch Qurolovna Siddikova, Alisher Khamidovich Khaitbaev","doi":"10.3390/ecsoc-26-13639","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13639","url":null,"abstract":"","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128824256","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
A. L. Makhamatkhanova, T. V. Tyumkina, U. Dzhemilev
: This work summarizes the results of a new approach to the synthesis of previously undescribed, hard-to-obtain five-membered cyclic organophosphorus compounds: 3-alkyl(aryl)- substituted phospholanes, α , ω -bisphospholanes, polycyclic phospholanes, 4,5-dialkyl(diaryl)- dis-ubstituted 2,3-dihydrophospholes, as well as their oxides and sulfides. Alumoles and alumolanes synthesized by the reaction of cycloalumination of available unsaturated compounds (terminal alkenes, α , ω -alkadienes, norbornene derivatives, symmetrical internal alkynes) with Et 3 Al in the presence of a Cp 2 ZrCl 2 catalyst were used as precursors. The substitution of aluminum atoms in cyclic organoaluminum compounds for phosphorus atoms takes place using alkyl(aryl)phosphorus (III) dichlorides. The developed one-pot method gives high yields of products under mild conditions.
{"title":"Approach to the Synthesis of Five-Membered Organophosphorus Compounds via Alumoles and Alumolanes","authors":"A. L. Makhamatkhanova, T. V. Tyumkina, U. Dzhemilev","doi":"10.3390/ecsoc-26-13637","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13637","url":null,"abstract":": This work summarizes the results of a new approach to the synthesis of previously undescribed, hard-to-obtain five-membered cyclic organophosphorus compounds: 3-alkyl(aryl)- substituted phospholanes, α , ω -bisphospholanes, polycyclic phospholanes, 4,5-dialkyl(diaryl)- dis-ubstituted 2,3-dihydrophospholes, as well as their oxides and sulfides. Alumoles and alumolanes synthesized by the reaction of cycloalumination of available unsaturated compounds (terminal alkenes, α , ω -alkadienes, norbornene derivatives, symmetrical internal alkynes) with Et 3 Al in the presence of a Cp 2 ZrCl 2 catalyst were used as precursors. The substitution of aluminum atoms in cyclic organoaluminum compounds for phosphorus atoms takes place using alkyl(aryl)phosphorus (III) dichlorides. The developed one-pot method gives high yields of products under mild conditions.","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"11 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114941927","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
: A metal-organic framework Zn 2 (BDC) 2 (DABCO) was employed as a reusable heterogeneous acidic catalyst in the acylation reaction of various benzaldehydes with acetic anhydride under microwave irradiation. The outstanding features of this efficient solvent-free method are short reaction time, ease of product separation, greatest yields, and the ability to reuse the catalyst several times.
{"title":"Chemo-Selective Protection of Aldehydes Functional Group Catalyzed by MOFs","authors":"Sakineh Mahdian, L. Panahi, M. Naimi-Jamal","doi":"10.3390/ecsoc-26-13645","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13645","url":null,"abstract":": A metal-organic framework Zn 2 (BDC) 2 (DABCO) was employed as a reusable heterogeneous acidic catalyst in the acylation reaction of various benzaldehydes with acetic anhydride under microwave irradiation. The outstanding features of this efficient solvent-free method are short reaction time, ease of product separation, greatest yields, and the ability to reuse the catalyst several times.","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128896638","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
I. Islamov, A. Yusupova, Snezhana Sharafutdinova, U. Dzhemilev
: Efficient methods for the synthesis of previously undescribed hybrid compounds based on monocarbonyl derivatives of curcumin and 5 Z ,9 Z -dienoic acid with yields of 58–66% are presented. The key monomer, (5 Z ,9 Z )-icosa-5,9-dienoic acid, was prepared using the stereoselective cross-cyclomagnesiation reaction of aliphatic and oxygen-containing 1,2-dienes catalyzed by Cp 2 TiCl 2 .
{"title":"A New Hybrid Molecule Based on (5Z,9Z)-icosa-5,9-dienoic Acid and Monocarbonyl Derivatives of Curcuminoids","authors":"I. Islamov, A. Yusupova, Snezhana Sharafutdinova, U. Dzhemilev","doi":"10.3390/ecsoc-26-13636","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13636","url":null,"abstract":": Efficient methods for the synthesis of previously undescribed hybrid compounds based on monocarbonyl derivatives of curcumin and 5 Z ,9 Z -dienoic acid with yields of 58–66% are presented. The key monomer, (5 Z ,9 Z )-icosa-5,9-dienoic acid, was prepared using the stereoselective cross-cyclomagnesiation reaction of aliphatic and oxygen-containing 1,2-dienes catalyzed by Cp 2 TiCl 2 .","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"13 40 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"115567609","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
L. Artiukh, O. Povnitsa, Yu. G. Shermolovich, S. Siry, S. Zahorodnia
: The search for new antiviral agents is an important task today. The aim of this study was to elucidate the impact of trifluoromethylthiolane derivatives on herpetic and adenoviral infections. It was found that the 2-hydroxy-2-trifluoromethylthiolane significantly inhibited Herpes simplex virus type 1 (HSV-1) reproduction, reducing the virus titer obtained de novo. Such activity indicates that virus offspring are formed, but the virus particles are not complete and are not able to cause an infection process. Therefore, trifluoromethylthiolane derivatives may be a potential compounds for the development on their basis agents for the treatment of herpetic infections.
{"title":"The Antiviral Activity of Trifluoromethylthiolane Derivatives","authors":"L. Artiukh, O. Povnitsa, Yu. G. Shermolovich, S. Siry, S. Zahorodnia","doi":"10.3390/ecsoc-26-13643","DOIUrl":"https://doi.org/10.3390/ecsoc-26-13643","url":null,"abstract":": The search for new antiviral agents is an important task today. The aim of this study was to elucidate the impact of trifluoromethylthiolane derivatives on herpetic and adenoviral infections. It was found that the 2-hydroxy-2-trifluoromethylthiolane significantly inhibited Herpes simplex virus type 1 (HSV-1) reproduction, reducing the virus titer obtained de novo. Such activity indicates that virus offspring are formed, but the virus particles are not complete and are not able to cause an infection process. Therefore, trifluoromethylthiolane derivatives may be a potential compounds for the development on their basis agents for the treatment of herpetic infections.","PeriodicalId":255032,"journal":{"name":"The 26th International Electronic Conference on Synthetic Organic Chemistry","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131281063","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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