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Green synthesis, molecular docking and in vitro biological evaluation of novel hydrazones, pyrazoles, 1,2,4-triazoles and 1,3,4-oxadiazoles 新型肼、吡唑、1,2,4-三唑和 1,3,4-恶二唑的绿色合成、分子对接和体外生物学评价
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-10-24 DOI: 10.1080/00397911.2024.2417362
Ahmed Younis , Asmaa F Kassem , Wael M Aboulthana , Ashraf A Sediek
{"title":"Green synthesis, molecular docking and in vitro biological evaluation of novel hydrazones, pyrazoles, 1,2,4-triazoles and 1,3,4-oxadiazoles","authors":"Ahmed Younis ,&nbsp;Asmaa F Kassem ,&nbsp;Wael M Aboulthana ,&nbsp;Ashraf A Sediek","doi":"10.1080/00397911.2024.2417362","DOIUrl":"10.1080/00397911.2024.2417362","url":null,"abstract":"<div><div>Ultrasonic waves were used for synthesis of novel hydrazones, bishydrazones, pyrazoles, 1,2,4-triazole and 1,3,4-oxadiazole. The structural formulae of the synthesized compounds were elucidated in terms of elemental and spectroscopic analyses. All synthesized compounds were estimated by testing total antioxidant capacity, iron‐reducing power, the scavenging activity against ABTS and DPPH radicals in addition to testing anti‐diabetic, anti‐Alzheimer and anti‐arthritic activities. All compounds displayed good to potent bioactivity. Compounds <strong>6, 10</strong> exhibit the highest antioxidant and free radicals scavenging activities. Furthermore, compounds <strong>6, 10</strong> demonstrate the strongest inhibition of α‐amylase and α-glucosidase. Compound <strong>12</strong> exhibit strongest acetylcholinesterase inhibition among prepared compounds. However, compounds <strong>18a,b, 19</strong> show a significantly higher inhibition percentage for protein denaturation and proteinase. The most bioactive prepared compounds <strong>6</strong>, <strong>10</strong> and <strong>12</strong> were investigated toward docking methodology against appropriate protein.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 22","pages":"Pages 1984-2002"},"PeriodicalIF":1.8,"publicationDate":"2024-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142586756","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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 structural characterization of a novel large type double-layered cyclophanes based on the reaction of bis(N-alkylene benzothiazolium) dibromide and triethylamine 基于双（N-亚烷基苯并噻唑）二溴化物和三乙胺反应的新型大型双层环烷的合成及其结构特征
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-10-18 DOI: 10.1080/00397911.2024.2415435
Zhen-zhong Wei , Xing-bao Chi
{"title":"Synthesis and structural characterization of a novel large type double-layered cyclophanes based on the reaction of bis(N-alkylene benzothiazolium) dibromide and triethylamine","authors":"Zhen-zhong Wei ,&nbsp;Xing-bao Chi","doi":"10.1080/00397911.2024.2415435","DOIUrl":"10.1080/00397911.2024.2415435","url":null,"abstract":"<div><div>The synthesis of a novel large type double-layered cyclophanes has been successfully accomplished by free radical coupling reaction with the bis(<em>N</em>-alkylene benzothiazolium) dibromide salts as their important synthetic intermediates. The structures of the two-layered cyclophanes and the synthetic intermediates have been elucidated based on the NMR data and X-ray structural analysis, respectively. The two-layered cyclophanes consist of two different geometries, <em>anti</em>-two cyclic lactam amide rings inside and two bridges of disulfide bonds outside, which are unique and novel structures. Their physical properties were investigated by UV–Vis and redox potential, too.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 22","pages":"Pages 1940-1949"},"PeriodicalIF":1.8,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142586757","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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
Solvent-free and efficient heterogeneous Biginelli reactions catalyzed by copper (II)-incorporated iminophenol-based porous organic polymer 铜(II)掺杂亚氨基苯酚基多孔有机聚合物催化的无溶剂高效异相比吉内利反应
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-10-16 DOI: 10.1080/00397911.2024.2416529
Pradeepruban Joseph , Pintu K. Kundu
{"title":"Solvent-free and efficient heterogeneous Biginelli reactions catalyzed by copper (II)-incorporated iminophenol-based porous organic polymer","authors":"Pradeepruban Joseph ,&nbsp;Pintu K. Kundu","doi":"10.1080/00397911.2024.2416529","DOIUrl":"10.1080/00397911.2024.2416529","url":null,"abstract":"<div><div>The copper (II)-incorporated iminophenol containing porous polymer (<strong>Cu-TAzo-TAPB</strong>), which was reported to be a recyclable catalyst for click reactions, is now exploited as an efficient catalyst in the solvent-free one-pot process to make 3,4-dihydropyrimidinone derivatives (DHPMs) by a three-component condensation reaction of urea/thiourea, aldehydes, and active methylene compounds. Usually, these reactions are complicated to carry out in a neutral medium. We describe here an eco-friendly method to produce Biginelli products with 5 mol% catalyst loading with a simple isolation technique. The high product yields show the effective Biginelli reaction technique. The catalyst is highly stable and easily recoverable for reuse without significant loss of catalytic efficiency.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 22","pages":"Pages 1974-1983"},"PeriodicalIF":1.8,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142586759","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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
Cobalt(II) catalyzed Michael-type hydroamination of activated olefins 钴（II）催化活化烯烃的迈克尔型加氢反应
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-10-16 DOI: 10.1080/00397911.2024.2414410
Rajagopal Rajesh , Joseph Prince Devassy , Rasheed Nihala , Rajesh Kunjanpillai
{"title":"Cobalt(II) catalyzed Michael-type hydroamination of activated olefins","authors":"Rajagopal Rajesh ,&nbsp;Joseph Prince Devassy ,&nbsp;Rasheed Nihala ,&nbsp;Rajesh Kunjanpillai","doi":"10.1080/00397911.2024.2414410","DOIUrl":"10.1080/00397911.2024.2414410","url":null,"abstract":"<div><div>The aza-Michael addition reaction of primary and secondary amines to <em>α</em>,<em>β</em>-unsaturated olefins viz; acrylonitrile, phenyl vinyl sulfone and dimethyl maleate has been carried out using 5–10 mol% Co(NO<sub>3</sub>)<sub>2</sub>.6H<sub>2</sub>O as a catalyst in <em>t</em>-BuOMe at 80–100 °C, giving rise to the desired <em>β</em>-aminocarbonyl compounds or sulfones in moderate to good yields. A wide range of aromatic amines, even those bearing electron withdrawing groups could be added to activated olefins via this strategy. Addition of (hetero)aromatic amines were also feasible, while in case of 2-aminopyridine the reaction was found to be effective only when AgOTf was added along with the catalyst. The aliphatic amines; benzylamine, dibenzylamine, di-<em>n</em>-butylamine were also smoothly added to acrylonitrile and phenyl vinyl sulfone. The methodology describes cobalt(II) nitrate as an eco-friendly, cheap and shelf available catalyst suitable for performing the Michael-type hydroamination reactions.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 22","pages":"Pages 1959-1973"},"PeriodicalIF":1.8,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142586760","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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
Copper(II)-catalyzed dehydration of primary amides to nitriles with the aid of trichloroacetonitrile 铜(II)催化伯胺在三氯乙腈帮助下脱水成腈纶
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-10-15 DOI: 10.1080/00397911.2024.2415442
Xiaoyun Ma , Xiaoyan Wan , Jun Zhao
{"title":"Copper(II)-catalyzed dehydration of primary amides to nitriles with the aid of trichloroacetonitrile","authors":"Xiaoyun Ma ,&nbsp;Xiaoyan Wan ,&nbsp;Jun Zhao","doi":"10.1080/00397911.2024.2415442","DOIUrl":"10.1080/00397911.2024.2415442","url":null,"abstract":"<div><div>A method for the preparation of nitriles from primary amides using trichloroacetonitrile and a catalytic amount of cupric acetate is described. Using this method, amides including aromatic amides, aromatic heterocyclic amides and aliphatic amides were converted into the corresponding nitriles in moderate to good yields. Trichloroacetonitrile reacted with amide in the presence of cupric acetate to form trichloroacetamide, which has been isolated and confirmed.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 22","pages":"Pages 1950-1958"},"PeriodicalIF":1.8,"publicationDate":"2024-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142586758","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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 biological evaluation of 1, 2, 3-triazole incorporated pyrrole derivatives as anticancer agents 作为抗癌剂的 1, 2, 3-三唑并吡咯衍生物的合成和生物学评价
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-10-15 DOI: 10.1080/00397911.2024.2408605
Somaiah Nalla , S. Aravind , Sri Charitha Annam , K. V. Padmavathi , Tasqeeruddin Syed , Mannam Subbarao
{"title":"Synthesis and biological evaluation of 1, 2, 3-triazole incorporated pyrrole derivatives as anticancer agents","authors":"Somaiah Nalla ,&nbsp;S. Aravind ,&nbsp;Sri Charitha Annam ,&nbsp;K. V. Padmavathi ,&nbsp;Tasqeeruddin Syed ,&nbsp;Mannam Subbarao","doi":"10.1080/00397911.2024.2408605","DOIUrl":"10.1080/00397911.2024.2408605","url":null,"abstract":"<div><div>A new series of 1,2,3-triazole skeleton incorporated pyrrole derivatives (<strong>11a–j</strong>) were developed and their chemical structures were confirmed by analytical data. Further, the anticancer profile of these newly derived compounds <strong>11a–j</strong> was assessed against four types of human cancer cell lines such as human breast cancer (MCF-7), lung cancer (A549), colon cancer (Colo-205) and ovarian cancer (A2780) by employing of the MTT method and was compared with etoposide used as a positive control. Most of the examined derivatives displayed moderate to good activity compared with the positive control. Among them, five compounds <strong>11a, 11b, 11c, 11d</strong>, and <strong>11e</strong> showed more potent activity. Particularly, compound <strong>11a</strong> showed superior activity.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 21","pages":"Pages 1828-1841"},"PeriodicalIF":1.8,"publicationDate":"2024-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142528223","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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
Sequential Knoevenagel condensation/cyclization reaction using Meldrum’s acid 使用梅尔德鲁姆酸的克诺文纳格尔缩合/环化顺序反应
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-10-11 DOI: 10.1080/00397911.2024.2413165
Shoko Yamazaki , Kohtaro Katayama , Yuta Mouri , Yuki Iwataki , Yuji Mikata , Tsumoru Morimoto
{"title":"Sequential Knoevenagel condensation/cyclization reaction using Meldrum’s acid","authors":"Shoko Yamazaki ,&nbsp;Kohtaro Katayama ,&nbsp;Yuta Mouri ,&nbsp;Yuki Iwataki ,&nbsp;Yuji Mikata ,&nbsp;Tsumoru Morimoto","doi":"10.1080/00397911.2024.2413165","DOIUrl":"10.1080/00397911.2024.2413165","url":null,"abstract":"<div><div>Sequential Knoevenagel condensation/cyclization using cyclic active methylene compounds such as Meldrum’s acid have been studied. The reaction of 2-(1-phenylvinyl)benzaldehyde and Meldrum’s acid, dimedone, or 1,3-indandione with piperidine/AcOH or L-proline at room temperature for 17–18 h gave cyclized indene derivatives in 63–80% yield. The reaction of 2-(3,5-dimethoxyphenyl)benzaldehyde and Meldrum’s acid at room temperature for 17 h gave a fluorene derivative in 98% yield. Furthermore, the reaction of 2-(3,5-dimethoxybenzyl)benzaldehyde and Meldrum’s acid with piperidine at room temperature for 18 h gave a dihydroanthracene derivative bearing Meldrum’s acid in 83% yield. The reaction of 2-(3,5-dimethoxybenzyl)benzaldehyde and Meldrum’s acid with piperidine at 110 °C for 2 h gave Meldrum’s acid fragmentated dihydroanthracene derivative in 48% yield. The reaction mechanisms of the cyclization steps and Meldrum’s acid fragmentation have been examined by the DFT calculations.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 21","pages":"Pages 1893-1907"},"PeriodicalIF":1.8,"publicationDate":"2024-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142528230","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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
An efficient synthesis, characterization, and in silico studies of novel chromenes, thiophenes, pyrazolo[1,5-a]pyrimidines, and pyrimidines as potential antimicrobial and anticancer agents using the bio-buffer tris(hydroxymethyl)aminomethane (THAM) 使用生物缓冲剂三（羟甲基）氨基甲烷（THAM）高效合成、表征和硅学研究新型铬、噻吩、吡唑并[1,5-a]嘧啶和嘧啶，将其作为潜在的抗菌剂和抗癌剂
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-10-10 DOI: 10.1080/00397911.2024.2410933
Nadia Hanafy Metwally , Zinab Atwa Saad
{"title":"An efficient synthesis, characterization, and in silico studies of novel chromenes, thiophenes, pyrazolo[1,5-a]pyrimidines, and pyrimidines as potential antimicrobial and anticancer agents using the bio-buffer tris(hydroxymethyl)aminomethane (THAM)","authors":"Nadia Hanafy Metwally ,&nbsp;Zinab Atwa Saad","doi":"10.1080/00397911.2024.2410933","DOIUrl":"10.1080/00397911.2024.2410933","url":null,"abstract":"<div><div>Novel 2-imino-6-(aryldiazenyl)-2<em>H</em>-chromene-3-carboxamides <strong>6a–e</strong>, 2-amino-4<em>H</em>-cyclopenta or benzo[<em>b</em>]thiophene-3-carboxamides <strong>10a,b</strong>, 2,7-diaminopyrazolo[1,5-<em>a</em>]pyrimidine-6-carboxamides <strong>13a–e</strong>, pyrimidine-5-carboxamides <strong>14</strong>, <strong>15</strong> and 3-amino-1<em>H</em>-pyrazole-4-carboxamide <strong>16</strong> were synthesized from the reaction of 2-cyano-<em>N</em>-(1,3-dihydroxy-2-(hydroxyl-methyl) propan-2-yl) acetamide <strong>2</strong> with 4-arylazosalicylaldehydes <strong>5a-e</strong>, cyclopentanone and/or cyclohexanone, guanidine derivatives and hydrazine hydrate, respectively. Some new compounds were evaluated for antibacterial activity <em>in vitro</em>, and exhibited good efficacy compared to gentamicin. Compound <strong>4c</strong> showed greater activity against gram negative bacteria (<em>Klebsiella pneumonia</em> and <em>Pseudomonas aeruginosa</em>) than standard antibiotic. Compound <strong>4c</strong> with two withdrawing groups also showed the higher activity (38.7 ± 0.6) against fungi (<em>Candida albicans</em>) than the Nystatin (20 ± 0.5). On the other hand, compounds <strong>13a</strong>, <strong>13c,</strong> and <strong>13e</strong> have strong cytotoxic activity among the tested compounds in the three selected cancer cell lines (HePG2, MCF7 and Hela). Physicochemical characterization by Swiss ADME predication was also performed for some synthesized compounds exhibiting better biological and antimicrobial properties.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 21","pages":"Pages 1871-1892"},"PeriodicalIF":1.8,"publicationDate":"2024-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142528228","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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, antiproliferative activity, and in silico studies of quinoline-based pyrimidinedione and thiazolidinedione derivatives 基于喹啉的嘧啶二酮和噻唑烷二酮衍生物的合成、抗增殖活性及硅学研究
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-10-04 DOI: 10.1080/00397911.2024.2409872
Abdullah Y. A. Alzahrani , Eman A. E. El-Helw , Sayed K. Ramadan
{"title":"Synthesis, antiproliferative activity, and in silico studies of quinoline-based pyrimidinedione and thiazolidinedione derivatives","authors":"Abdullah Y. A. Alzahrani ,&nbsp;Eman A. E. El-Helw ,&nbsp;Sayed K. Ramadan","doi":"10.1080/00397911.2024.2409872","DOIUrl":"10.1080/00397911.2024.2409872","url":null,"abstract":"<div><div>Cancer affects millions of people worldwide. PDK1 enzyme (co-crystallized with BIM-1) controls the proliferation of breast cancer cells. Aiming to resemble BIM-1’s binding, quinoline-based pyrimidinediones and thiazolidinediones were synthesized starting from 2-chloro-3-formylquinoline. Compared with doxorubicin (reference), in vitro antiproliferative activity against MCF7 and HCT116 cancer cell lines showed the most potency of thiobarbiturate <strong>3</strong> and thiazolidinedione <strong>4</strong>. <em>In silico</em> molecular docking, DFT, and pharmacokinetics simulations supported the findings. The docking analysis toward PDK1 enzyme showed that most amino acids interacting with co-crystallized ligand (BIM-1) were successfully bonded to our docked substances, especially thiobarbiturate <strong>3</strong> with highest S-score closer to BIM-1. In DFT calculations, this compound exhibited the lowest energy gap and highest softness leading to more response to radical surface interactions. The compounds with significant antiproliferative activity exhibited high electrophilicity values. ADME analysis showed its desirable drug-likeness and oral bioavailability. This work may contribute to developing new potent antiproliferative agents.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 21","pages":"Pages 1842-1856"},"PeriodicalIF":1.8,"publicationDate":"2024-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142528229","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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
Potential MRSA inhibitory activity of some new benzofuran-pyrazolo[1,5-a]pyrimidine hybrids attached to arene units via methylene or azo linkage 通过亚甲基或偶氮连接与炔单元相连的一些新型苯并呋喃-吡唑并[1,5-a]嘧啶杂化物的潜在 MRSA 抑制活性
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-28 DOI: 10.1080/00397911.2024.2409875
Sherif M. H. Sanad , Ahmed E. M. Mekky
{"title":"Potential MRSA inhibitory activity of some new benzofuran-pyrazolo[1,5-a]pyrimidine hybrids attached to arene units via methylene or azo linkage","authors":"Sherif M. H. Sanad ,&nbsp;Ahmed E. M. Mekky","doi":"10.1080/00397911.2024.2409875","DOIUrl":"10.1080/00397911.2024.2409875","url":null,"abstract":"<div><div>MRSA, a resistant bacteria causing severe infections, is targeted by researchers developing new anti-resistance compounds. The study aimed to investigate the MRSA inhibitory activity of two series of benzofuran-pyrazolo[1,5-<em>a</em>]pyrimidines <strong>1</strong> and <strong>2</strong>, attached to arene units <em>via</em> methylene or azo linkage, respectively. The desired products were prepared, in 82–92% yields, by reacting benzofuran-based enaminone <strong>4</strong> with the appropriate 1<em>H</em>-pyrazole-3,5-diamines <strong>5</strong> in pyridine at reflux for 5–6 h. The new hybrids showed a wide spectrum of antibacterial activity against different ATCC strains. Products with azo linkage and para-substituted arene units with electron-releasing groups demonstrated higher antibacterial activity. 3-((4-Methoxyphenyl)diazenyl)-linked pyrazolo[1,5-<em>a</em>]pyrimidine <strong>2e</strong> demonstrates activity that exceeded the reference ciprofloxacin with MIC/MBC values of 1.8/3.6 µM against <em>S. aureus</em> and <em>E. coli</em> strains. Also, it demonstrated more effective MRSA inhibitory activity than the reference linezolid, with MIC/MBC values of 3.6/14.4 and 1.8/7.2 µM against MRSA ATCC:33591 and ATCC:43300 strains, respectively.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 21","pages":"Pages 1857-1870"},"PeriodicalIF":1.8,"publicationDate":"2024-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142528128","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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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