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Synthesis and antinociceptive activity of potassium 1-alkoxy-6-aryl-2-cyano-4-[(3-cyano-4,5,6,7-tetrahydrobenzo[b]-thiophen-2-yl)amino]-1,6-dioxohexa-2,4-dien-3-olates 1-烷氧基-6-芳基-2-氰基-4-[（3-氰基-4,5,6,7-四氢苯并[b]-噻吩-2-基）氨基]-1,6-二氧己-2,4-二烯-3-油酸钾的合成及抗伤活性
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4608-4
D. V. Lipin, V. M. Shadrin, S. K. Metlyakova, P. S. Silaichev, R. R. Makhmudov, D. A. Shipilovskikh
{"title":"Synthesis and antinociceptive activity of potassium 1-alkoxy-6-aryl-2-cyano-4-[(3-cyano-4,5,6,7-tetrahydrobenzo[b]-thiophen-2-yl)amino]-1,6-dioxohexa-2,4-dien-3-olates","authors":"D. V. Lipin,&nbsp;V. M. Shadrin,&nbsp;S. K. Metlyakova,&nbsp;P. S. Silaichev,&nbsp;R. R. Makhmudov,&nbsp;D. A. Shipilovskikh","doi":"10.1007/s11172-025-4608-4","DOIUrl":"10.1007/s11172-025-4608-4","url":null,"abstract":"<div><p>The oxofuran ring opening in 2-[(2-oxofuran-3(2<i>H</i>)-ylidene)amino]-4,5,6,7-tetrahydrobenzo[<i>b</i>]thiophene-3-carbonitriles upon the reaction with alkyl cyanoacetates and Bu<sup>t</sup>OK gave new potassium 1-alkoxy-6-aryl-2-cyano-4-[(3-cyano-4,5,6,7-tetrahydrobenzo[<i>b</i>]thiophen-2-yl)amino]-1,6-dioxohexa-2,4-dien-3-olates. The synthesized compounds demonstrated pronounced antinociceptive activity and low toxicity (the toxicity class IV of practically nontoxic substances).</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"1145 - 1152"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073600","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effect of coordination of 1,2,4-triazole moiety in Cu(ii) and Zn(ii) compounds with 2-{[(4H-1,2,4-triazol-4-yl)imino]methyl}phenol on their antimicrobial activity Cu（ii）和Zn（ii）化合物中1,2,4-三唑部分与2-{[（4h -1,2,4-三唑-4-酰基）亚氨基]甲基}苯酚配位对抗菌活性的影响
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4593-7
A. A. Bovkunova, E. S. Bazhina, M. A. Shmelev, N. V. Gogoleva, A. A. Pavlov, E. A. Varaksina, I. V. Taydakov, L. N. Fetisov, A. E. Svyatogorova, N. O. Andros, A. A. Zubenko, A. V. Lyamin, D. D. Ismatullin, I. L. Eremenko, M. A. Kiskin
{"title":"Effect of coordination of 1,2,4-triazole moiety in Cu(ii) and Zn(ii) compounds with 2-{[(4H-1,2,4-triazol-4-yl)imino]methyl}phenol on their antimicrobial activity","authors":"A. A. Bovkunova,&nbsp;E. S. Bazhina,&nbsp;M. A. Shmelev,&nbsp;N. V. Gogoleva,&nbsp;A. A. Pavlov,&nbsp;E. A. Varaksina,&nbsp;I. V. Taydakov,&nbsp;L. N. Fetisov,&nbsp;A. E. Svyatogorova,&nbsp;N. O. Andros,&nbsp;A. A. Zubenko,&nbsp;A. V. Lyamin,&nbsp;D. D. Ismatullin,&nbsp;I. L. Eremenko,&nbsp;M. A. Kiskin","doi":"10.1007/s11172-025-4593-7","DOIUrl":"10.1007/s11172-025-4593-7","url":null,"abstract":"<div><p>The reactions of copper(<span>ii</span>) and zinc(<span>ii</span>) salts with 2-{[(4<i>H</i>-1,2,4-triazol-4-yl)imino]-methyl}phenol (HL) were studied. The reaction of copper(<span>ii</span>) trifluoroacetate with HL in MeOH affords the mononuclear complex [CuL<sub>2</sub>] (<b>1</b>). In the crystal, molecules <b>1</b> form a supramolecular layered structure through Cu⋯N contacts (2.74 Å). The reaction of zinc(<span>ii</span>) chloride with HL in the presence of Et<sub>3</sub>N gives the 2D coordination polymer [ZnL<sub>2</sub>]<sub><i>n</i></sub> (<b>2</b>), whereas this reaction using a protonating agent (HCl) instead of the organic base produces the mononuclear complex [Zn(HL)<sub>2</sub>Cl<sub>2</sub>] (<b>3</b>). The photoluminescent properties of compounds HL, <b>2</b>, and <b>3</b> were studied and their <sup>1</sup>H NMR spectra were measured. The electronic absorption spectra of all synthesized compounds in solution were recorded. The free ligand HL and compounds <b>1–3</b> were evaluated for antibacterial activity against <i>E. coli</i> and <i>S. aureus</i> strains, antifungal activity against the molds <i>A. fumigatus</i>, <i>R. oryzae</i> and the yeast fungi <i>C. albicans</i>, <i>C. glabrata</i>, and antiprotozoal activity against <i>Colpoda steinii</i>.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"986 - 1000"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073592","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
One-pot synthesis of new thiazole derivatives via the reaction of arylamines, carbon disulfide, and N-arylmaleimides and evaluations of their antiviral activity 芳胺、二硫化碳和n -芳基马来酰亚胺一锅反应合成新的噻唑衍生物并评价其抗病毒活性
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4605-7
A. A. Belokon, N. V. Stolpovskaya, A. V. Zorina, O. V. Pyankov, M. A. Prezent, M. E. Minyaev, Kh. S. Shikhaliev
{"title":"One-pot synthesis of new thiazole derivatives via the reaction of arylamines, carbon disulfide, and N-arylmaleimides and evaluations of their antiviral activity","authors":"A. A. Belokon,&nbsp;N. V. Stolpovskaya,&nbsp;A. V. Zorina,&nbsp;O. V. Pyankov,&nbsp;M. A. Prezent,&nbsp;M. E. Minyaev,&nbsp;Kh. S. Shikhaliev","doi":"10.1007/s11172-025-4605-7","DOIUrl":"10.1007/s11172-025-4605-7","url":null,"abstract":"<div><p>A one-pot reaction of arylamines with carbon disulfide and <i>N</i>-arylmaleimides at different ratios of reagents gave two types of substituted thiazolones: <i>N</i>-aryl-2-(3-aryl-4-oxo-2-thioxothiazolidin-5-yl)acetamides and <i>N</i>-aryl-2-(3-aryl-2-arylimino-4-oxothiazolidin-5-yl)acetamides. The reaction of arylamine with a small excess of carbon disulfide in acetonitrile led to <i>N</i>-aryldithiocarbamic acids, and treatment of the latter with <i>N</i>-arylmaleimides resulted in <i>N</i>-aryl-2-(3-aryl-4-oxo-2-thioxothiazolidin-5-yl)acetamides. The reaction of a twofold excess of arylamine with carbon disulfide in acetonitrile led to <i>N</i><sup>1</sup>,<i>N</i><sup>2</sup>-diarylthioureas, and treatment of the latter with <i>N</i>-arylmaleimides resulted in <i>N</i>-aryl-2-(3-aryl-2-arylimino-4-oxothiazolidin-5-yl)acetamides. A three-component mode at different ratios of <i>N</i>-arylmaleimide, arylamine, and carbon disulfide gave <i>N</i>-aryl-2-(3-aryl-4-oxo-2-thioxothiazolidin-5-yl)acetamides as the major reaction product. Evaluations of the antiviral activity of synthesized derivatives revealed that 2-[3-(4-methoxyphenyl)-4-oxo-2-thioxothiazolidin-5-yl]-<i>N</i>-(4-chlorophenyl)acetamide efficiently suppresses the replication of the SARS-CoV-2 virus.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"1120 - 1129"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073597","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Modern methods for the synthesis of biologically active compounds labeled with hydrogen isotopes 用氢同位素标记生物活性化合物的现代合成方法
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4583-9
V. P. Shevchenko, K. V. Shevchenko, L. A. Andreeva, I. Yu. Nagaev, N. F. Myasoedov
{"title":"Modern methods for the synthesis of biologically active compounds labeled with hydrogen isotopes","authors":"V. P. Shevchenko,&nbsp;K. V. Shevchenko,&nbsp;L. A. Andreeva,&nbsp;I. Yu. Nagaev,&nbsp;N. F. Myasoedov","doi":"10.1007/s11172-025-4583-9","DOIUrl":"10.1007/s11172-025-4583-9","url":null,"abstract":"<div><p>The review addresses methods for the introduction of hydrogen isotopes into organic compounds, which are then used as labeled building blocks in the synthesis of biologically active products. Hydrogen isotopes are introduced by either isotope exchange or chemical reactions. If a carbonyl group is present in the precursor of the biologically active compound, deuterium can be introduced both through isotope exchange and <i>via</i> the reduction of the ketone group. Labeled reagents such as [<sup>3</sup>H]methyl nosylate are also used to obtain labeled oligonucleotides. The introduction of hydrogen isotopes into estrone is performed using isotope exchange both in the solid state and in solution (D<sub>2</sub>O, CF<sub>3</sub>COOD). The replacement of the iodine atom with deuterium gives labeled analogs of xanthine, steroids, adamantane, carbohydrates, and other compounds. In some cases, to activate deuteration, deuterated silanes were synthesized and catalytic systems such as AgCO<sub>3</sub>/PPh<sub>3</sub>/K<sub>2</sub>CO<sub>3</sub>, Rh nanoparticles, and Pt<sup>II</sup>-based catalysts were used. Issues related to hydrogen spillover are discussed in the context of solid-phase isotope exchange.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"881 - 893"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073696","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of a new conjugate based on ethylenediamine-N,N,N′,N′-tetra(3-propionic acid), a promising radiopharmaceutical precursor 一种有前途的放射性药物前体乙二胺-N，N,N′，N′-四（3-丙酸）缀合物的合成
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4597-3
D. S. Khachatryan, A. V. Kolotaev, V. N. Osipov, E. A. Ruchko, N. V. Tsirulnikova
{"title":"Synthesis of a new conjugate based on ethylenediamine-N,N,N′,N′-tetra(3-propionic acid), a promising radiopharmaceutical precursor","authors":"D. S. Khachatryan,&nbsp;A. V. Kolotaev,&nbsp;V. N. Osipov,&nbsp;E. A. Ruchko,&nbsp;N. V. Tsirulnikova","doi":"10.1007/s11172-025-4597-3","DOIUrl":"10.1007/s11172-025-4597-3","url":null,"abstract":"<div><p>An optimal method for the synthesis of triethyl ethylenediamine-<i>N</i>,<i>N</i>,<i>N</i>′,<i>N</i>″-tetra-(3-propionate) was developed. Using the resulting promising bifunctional chelator, a new radiopharmaceutical drug precursor was obtained.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"1025 - 1033"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073708","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Regiospecific method for the synthesis of N9-alkylated 8-azapurines 区域特异性合成n9 -烷基化8-氮杂嘌呤的方法
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4596-4
K. V. Savateev, D. A. Gazizov, P. A. Slepukhin, V. L. Rusinov
{"title":"Regiospecific method for the synthesis of N9-alkylated 8-azapurines","authors":"K. V. Savateev,&nbsp;D. A. Gazizov,&nbsp;P. A. Slepukhin,&nbsp;V. L. Rusinov","doi":"10.1007/s11172-025-4596-4","DOIUrl":"10.1007/s11172-025-4596-4","url":null,"abstract":"<div><p>Regiospecific method for the synthesis of <i>N</i><sup>9</sup>-alkylated 8-azapurines was proposed based on the reconstructive methodology. It was shown that 2,5-diamino-4-alkylaminopyrimidines under the diazotization reaction conditions were converted into the corresponding 2-amino-<i>N</i><sup>9</sup>-alkyl-8-azapurines in high yields. A possibility for the synthesis of analogs of natural nucleosides, 8-azapurines containing hydroxy groups in the pseudoriboside moiety, was demonstrated, including the synthesis of analog of antiviral drug Penciclovir.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"1015 - 1024"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073589","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and functionalization of P(O)CH2NH- and P(O)CH2NSi-containing amines 含P(O)CH2NH-和P(O) ch2nsi胺的合成和功能化
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4599-1
Yu. N. Bubnov, A. A. Prishchenko, M. V. Livantsov, O. P. Novikova, L. I. Livantsova, S. V. Baranin
{"title":"Synthesis and functionalization of P(O)CH2NH- and P(O)CH2NSi-containing amines","authors":"Yu. N. Bubnov,&nbsp;A. A. Prishchenko,&nbsp;M. V. Livantsov,&nbsp;O. P. Novikova,&nbsp;L. I. Livantsova,&nbsp;S. V. Baranin","doi":"10.1007/s11172-025-4599-1","DOIUrl":"10.1007/s11172-025-4599-1","url":null,"abstract":"<div><p>Convenient syntheses of phosphorus-substituted amines containing P(O)CH<sub>2</sub>NH and P(O)CH<sub>2</sub>NSi moieties based on the reaction between <i>N</i>,<i>N</i>′,<i>N</i>″-trisubstituted hexahydro-1,3,5-triazines and trivalent phosphorus acid esters have been developed. Various functionalization reactions (2-carboxyethylation, 2-pyridylethylation, and acylation) of the NH and NSi units of the resulting synthons proceed under mild conditions and give new functionalized phosphorus-containing amines in high yields. The resulting compounds are of interest as promising biologically active substances, water-soluble polydentate ligands, and effective extractants.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"1041 - 1054"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073593","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and study of anti-inflammatory activity of N-alkyl-2-aroylhydrazinylidene-4-oxobutanamides n -烷基-2-芳基肼基-4-氧丁烷酰胺的合成及抗炎活性研究
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4606-6
E. I. Denisova, O. V. Zvereva, D. V. Lipin, S. V. Chashchina, I. N. Chernov, E. S. Denislamova, D. A. Shipilovskikh, N. M. Igidov
{"title":"Synthesis and study of anti-inflammatory activity of N-alkyl-2-aroylhydrazinylidene-4-oxobutanamides","authors":"E. I. Denisova,&nbsp;O. V. Zvereva,&nbsp;D. V. Lipin,&nbsp;S. V. Chashchina,&nbsp;I. N. Chernov,&nbsp;E. S. Denislamova,&nbsp;D. A. Shipilovskikh,&nbsp;N. M. Igidov","doi":"10.1007/s11172-025-4606-6","DOIUrl":"10.1007/s11172-025-4606-6","url":null,"abstract":"<div><p>The oxofuran ring opening of 4-substituted <i>N</i>′-(5-aryl-2-oxofuran-3(2<i>H</i>)-ylidene)-benzhydrazides upon the reaction with different alkylamines gave new modified <i>N</i>-alkyl-2-aroylhydrazinylidene-4-oxobutanamides. The synthesized compounds demonstrated pronounced anti-inflammatory activity <i>in vivo</i> and proved themselves as promising drug candidates for the treatment of inflammation.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"1130 - 1137"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073598","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and antihypoxic activity of 2-amino-1-aryl-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-1H-4,5-dihydropyrrole-3-carboxylic acid derivatives 2-氨基-1-芳基-5-（3,3-二甲基-2-氧基丁基）-4-氧基- 1h -4,5-二氢吡咯-3-羧酸衍生物的合成及抗氧活性研究
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4607-5
K. L. Gankova, S. S. Zykova, I. A. Gorbunova, E. S. Denislamova, D. A. Shipilovskikh, R. R. Makhmudov, I. N. Chernov, N. M. Igidov
{"title":"Synthesis and antihypoxic activity of 2-amino-1-aryl-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-1H-4,5-dihydropyrrole-3-carboxylic acid derivatives","authors":"K. L. Gankova,&nbsp;S. S. Zykova,&nbsp;I. A. Gorbunova,&nbsp;E. S. Denislamova,&nbsp;D. A. Shipilovskikh,&nbsp;R. R. Makhmudov,&nbsp;I. N. Chernov,&nbsp;N. M. Igidov","doi":"10.1007/s11172-025-4607-5","DOIUrl":"10.1007/s11172-025-4607-5","url":null,"abstract":"<div><p>A series of 2-amino-1-aryl-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-4,5-dihydro-1<i>H</i>-pyrrole-3-carboxylic acid derivatives was synthesized by the reaction of 4-arylamino-2-<i>tert</i>-butyl-5-oxo-2,5-dihydrofuran-2-yl acetates with cyanoacetic acid derivatives. Some of the synthesized compounds demonstrated antihypoxic effect thus proving themselves as promising candidates for more in-depth biological studies.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"1138 - 1144"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073599","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design of potential antiplatelet agents based on modifications of the 3-pyridylisoxazole scaffold 基于3-吡啶基利恶唑支架修饰的潜在抗血小板药物的设计
IF 1.7 4区 化学
Russian Chemical Bulletin Pub Date : 2025-05-15 DOI: 10.1007/s11172-025-4601-y
O. V. Demina, N. E. Belikov, A. Yu. Lukin, N. A. Podoplelova, M. A. Panteleev, A. A. Khodonov, S. D. Varfolomeev
{"title":"Design of potential antiplatelet agents based on modifications of the 3-pyridylisoxazole scaffold","authors":"O. V. Demina,&nbsp;N. E. Belikov,&nbsp;A. Yu. Lukin,&nbsp;N. A. Podoplelova,&nbsp;M. A. Panteleev,&nbsp;A. A. Khodonov,&nbsp;S. D. Varfolomeev","doi":"10.1007/s11172-025-4601-y","DOIUrl":"10.1007/s11172-025-4601-y","url":null,"abstract":"<div><p>Based on two modifications of the main scaffold, 3-(3-pyridyl)isoxazole, two series of compounds were prepared, namely, positional isomers (5-substituted 3-phenylisoxazoles) and bioisosteres (5-substituted 3-(3-pyridyl)-1,2,4-oxadiazoles). Both series of compounds showed anti-aggregatory activity in the study of human platelet aggregation initiated by arachidonic acid and the selective thromboxane A<sub>2</sub> receptor agonist U46619. According to the results of the biological studies, all three scaffolds can be used for further development of prototypes of anti-aggregatory agents.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"74 4","pages":"1069 - 1081"},"PeriodicalIF":1.7,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144073595","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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