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Heterocyclic Communications最新文献

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Design, synthesis, and biological activity of novel pomalidomide linked with diphenylcarbamide derivatives 新型泊马度胺二苯脲衍生物的设计、合成及生物活性研究
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0155
Bin Sun, Xiaofei Liu, Tao Ji, Xiaoguang Zhan, L. Mao, Peng Deng, Lin Shi
{"title":"Design, synthesis, and biological activity of novel pomalidomide linked with diphenylcarbamide derivatives","authors":"Bin Sun, Xiaofei Liu, Tao Ji, Xiaoguang Zhan, L. Mao, Peng Deng, Lin Shi","doi":"10.1515/hc-2022-0155","DOIUrl":"https://doi.org/10.1515/hc-2022-0155","url":null,"abstract":"Abstract Based on 2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindoline-1,3-dione as a raw material, a series of novel pomalidomide linked with diphenylcarbamide derivatives were synthesized through several step reactions of substitution, click reaction, and addition reaction. The structures of these compounds were confirmed by 1H NMR, 13C NMR, and MS. We discovered that some of the compounds are capable of suppressing indoleamine pyrrole-2,3-dioxygenase-1 activities in in vitro experiments, in which the inhibitory activity of 5b reached the level of benefits. Graphical abstract","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"174 - 180"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43705495","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
Study of the reactivity of aminocyanopyrazoles and evaluation of the mitochondrial reductive function of some products 氨基氰吡唑的反应性研究及部分产物的线粒体还原功能评价
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0001
Soumaya Bellili, N. J. Coltman, N. Hodges, F. Allouche
{"title":"Study of the reactivity of aminocyanopyrazoles and evaluation of the mitochondrial reductive function of some products","authors":"Soumaya Bellili, N. J. Coltman, N. Hodges, F. Allouche","doi":"10.1515/hc-2022-0001","DOIUrl":"https://doi.org/10.1515/hc-2022-0001","url":null,"abstract":"Abstract This research investigated the general high-throughput synthetic protocol for the accelerated synthesis of functionalized trifluoromethylpyrazolopyrimidines 3 and N-(5-cyano-3-methyl-1-phenyl-1H-pyrazol-4-yl) benzamide 4 from aminocyanopyrazole 1 precursors. The action of chlorosulfonyl isocyanate (CSI) with aminopyrazolo[3,4-d]pyrimidines 2 was found to produce triazolopyrimidinones 5 . The MTT test that quantifies mitochondrial reductive function demonstrated that in both cell lines tested (PE/CA-PJ41 and HePG2 cells), the benzamide compounds 4 are moderately toxic with PE/CA-PJ41 cells and more sensitive than HePG2 cells.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"11 - 17"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47742836","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: 1
Synthesis of 2,2-difluoro-2-arylethylamines as fluorinated analogs of octopamine and noradrenaline 作为章鱼胺和去甲肾上腺素氟化类似物的2,2-二氟-2-芳基乙胺的合成
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0005
A. Tarui, Erika Kamata, Koji Ebisu, Y. Kawai, Ryota Araki, Takeshi Yabe, Yukiko Karuo, Kazuyuki Sato, Kentaro Kawai, M. Omote
{"title":"Synthesis of 2,2-difluoro-2-arylethylamines as fluorinated analogs of octopamine and noradrenaline","authors":"A. Tarui, Erika Kamata, Koji Ebisu, Y. Kawai, Ryota Araki, Takeshi Yabe, Yukiko Karuo, Kazuyuki Sato, Kentaro Kawai, M. Omote","doi":"10.1515/hc-2022-0005","DOIUrl":"https://doi.org/10.1515/hc-2022-0005","url":null,"abstract":"Abstrtact A series of 2,2-difluoro-2-arylethylamines was synthesized as fluorinated analogs of octopamine and noradrenaline with the expectation of bioisosteric OH/F exchanges. The syntheses of these compounds were performed by a Suzuki–Miyaura cross-coupling reaction of 4-(bromodifluoroacetyl)morpholine with aryl boronic acids to produce the intermediate 2,2-difluoro-2-arylacetamides, followed by transformation of difluoroacetamide to difluoroethylamine.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"26 - 34"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41893696","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
Cyclization of N-acetyl derivative: Novel synthesis – azoles and azines, antimicrobial activities, and computational studies n -乙酰基衍生物的环化:新的合成-唑和氮，抗菌活性和计算研究
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0004
E. Hamed, M. Assy, N. Ouf, Doaa A. Elsayed, M. Abdellattif
{"title":"Cyclization of N-acetyl derivative: Novel synthesis – azoles and azines, antimicrobial activities, and computational studies","authors":"E. Hamed, M. Assy, N. Ouf, Doaa A. Elsayed, M. Abdellattif","doi":"10.1515/hc-2022-0004","DOIUrl":"https://doi.org/10.1515/hc-2022-0004","url":null,"abstract":"Abstract 2-Pyridone is considered as one of the most famous efficient pharmaceutical compounds. Many approaches were discovered to synthesize 2-pyridone. In this present research, chloroacetylation of benzylamine at simple conditions, EtONa/EtCOONa produced N-benzyl-2-chloroacetamide 2. Compound 2 was allowed to react with different reagents. These reagents are acetylacetone, ethyl cyanoacetate, ethyl acetoacetate, and diethyl malonate, creating 2-pyridone derivatives with a good yield. The structures of the prepared compounds were elucidated by spectral data (IR, 1HNMR, and 13CNMR). The synthesized compound was tested for its antimicrobial activity against the Gram-positive (Staphylococcus aureus) and the Gram-negative (Escherichia coli) bacteria. In addition, the antifungal activities of the compounds were tested against two fungi (Candida albicans and Aspergillus flavus). Molecular docking studies were applied using the Autodock vina method. Theoretical methods prove all the experimental results by using molecular docking using Autodock vina and by ADEMT studies. The docking results represent that compound 20 had the best docking free energy, and it is the effective compound toward the selected bacterial and fungal proteins. ADME studies showed that the only compound 18 could cross the blood–brain barrier, and compound 15 was predicted to be soluble.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"35 - 43"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44978076","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: 2
Sono and nano: A perfect synergy for eco-compatible Biginelli reaction 声纳和纳米:生态兼容的比基内利反应的完美协同作用
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0003
Marzieh Tahmasbi, Nadiya Koukabi, Ozra Armandpour
{"title":"Sono and nano: A perfect synergy for eco-compatible Biginelli reaction","authors":"Marzieh Tahmasbi, Nadiya Koukabi, Ozra Armandpour","doi":"10.1515/hc-2022-0003","DOIUrl":"https://doi.org/10.1515/hc-2022-0003","url":null,"abstract":"Abstract In this study, we evaluated the performance of nano-γ-Fe2O3–SO3H catalyst in the Biginelli reaction and synthesized 3,4-dihydropyrimidine-2-(1H)-ones. This reaction was carried out under solvent-free and ultrasonic irradiation conditions and belonged to one-pot multicomponent reactions (MCRs) with an adopted aromatic aldehyde, ethyl acetoacetate, and urea as starting materials for the beginning of the reaction. The synthesized materials were efficient in synthesizing 3,4-dihydropyrimidine-2-(1H)-ones via the Biginelli reaction under reaction conditions. Thus, the advantages of using nano-γ-Fe2O3–SO3H in the Biginelli reaction are short reaction time, high efficiency, green method, solvent free, and cost-effective. Furthermore, nano-γ-Fe2O3–SO3H as a heterogeneous catalyst can be recycled five times without significantly reducing catalytic activity. Graphical abstract","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"1 - 10"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44253436","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: 4
Synthesis of enhanced lipid solubility of indomethacin derivatives for topical formulations 局部制剂用消炎痛衍生物脂溶性增强的合成
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0013
M. Abualhasan, N. Jaradat, Raghad Maslamani, Dana Nofal, Linda Omar
{"title":"Synthesis of enhanced lipid solubility of indomethacin derivatives for topical formulations","authors":"M. Abualhasan, N. Jaradat, Raghad Maslamani, Dana Nofal, Linda Omar","doi":"10.1515/hc-2022-0013","DOIUrl":"https://doi.org/10.1515/hc-2022-0013","url":null,"abstract":"Abstract Indomethacin is a nonselective nonsteroidal anti-inflammatory drug with serious side effects such as depression, hallucination, and gastrointestinal irritation. This study aims to enhance indomethacin lipid solubility of indomethacin derivative to use it for the topical formulation since topical formulation may lower the unwanted side effects. The lipid solubility was achieved by adding various alkyl groups (methyl, ethyl, propyl, and isopropyl) to the drug via an ester linkage. The measured log p of these compounds was higher compared to the underivatized indomethacin. Furthermore, an ointment of each ester was formulated and was tested on mice skin using Franz diffusion. The best absorption was observed for methyl indomethacin with threefold increase in permeability compared to indomethacin. This study approves using derivatized indomethacin as a topical formulation with improved efficacy compared to the present gel formulation in the market.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"124 - 129"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44926464","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
Chemical constituents of plants from the genus Carpesium 石竹属植物的化学成分
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0012
Ning-Ning Shi, Cong-Cong Hou, Yan Liu, Kun-Yao Li, Sheng-Dan Mi, Bin Tong, Man-li Zhang
{"title":"Chemical constituents of plants from the genus Carpesium","authors":"Ning-Ning Shi, Cong-Cong Hou, Yan Liu, Kun-Yao Li, Sheng-Dan Mi, Bin Tong, Man-li Zhang","doi":"10.1515/hc-2022-0012","DOIUrl":"https://doi.org/10.1515/hc-2022-0012","url":null,"abstract":"Abstract Carpesium (Family – Compositae) is a genus with 24 species of mainly perennial herbs. Several species of this genus have served as folk medicine in China and Korea for their antipyretic, anti-inflammatory, analgesic, antifungal, antibacterial, and cytotoxic activity properties. Chemical constituents are mostly sesquiterpenes, diterpenes, glycosides, and several other types of compounds. This article summarizes the literature on the isolated and identified constituents from various Carpesium species and their various biological activities.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"95 - 123"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42268049","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: 2
Synthesis of fluoro-rich pyrimidine-5-carbonitriles as antitubercular agents against H37Rv receptor 富氟嘧啶-5-碳腈抗H37Rv受体结核药物的合成
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0010
K. Kapadiya, K. Kavadia, V. Khedkar, P. Dholaria, A. Jivani, R. Khunt
{"title":"Synthesis of fluoro-rich pyrimidine-5-carbonitriles as antitubercular agents against H37Rv receptor","authors":"K. Kapadiya, K. Kavadia, V. Khedkar, P. Dholaria, A. Jivani, R. Khunt","doi":"10.1515/hc-2022-0010","DOIUrl":"https://doi.org/10.1515/hc-2022-0010","url":null,"abstract":"Abstract The purpose of this study was to prepare various derivatives of 4-amino-2-(3-fluoro-5-(trifluoromethyl)phenyl)-6-arylpyrimidine-5-carbonitrile (6a–6h) using a three-step procedure. The derivatives were screened in vitro for activity against Mycobacterium tuberculosis strain H37Rv. The activity was expressed as the minimum inhibitory concentration (MIC) in μg/mL (μM). Eight compounds showed activity against Mtb H37Rv, and among them, 6f showed the best value of MIC, IC50 (53 μM) and IC90 (62 μM). Minimum bactericidal concentration of compound 6f was higher than its MIC and was more time-dependent than the concentration. Compound 6f was more active against M. tuberculosis H37Rv under low oxygen than metronidazole and did not show good potency in different treatments and non-tuberculous mycobacteria. Furthermore, a molecular docking study against mycobacterial enoyl-ACP reductase (InhA) could provide valuable insights into the plausible mechanism of action, which could set the theme for lead optimization. Graphical abstract","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"75 - 83"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48643901","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: 1
Reactions of 3-amino-1,2,4-triazine with coupling reagents and electrophiles 3-氨基-1,2,4-三嗪与偶联试剂和亲电试剂的反应
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0149
M. V. Bvumbi, Anza Imanuel Nemudzivhadi, Musiiwa Victoria Sengane, Simon Mnyakeni Moleele
{"title":"Reactions of 3-amino-1,2,4-triazine with coupling reagents and electrophiles","authors":"M. V. Bvumbi, Anza Imanuel Nemudzivhadi, Musiiwa Victoria Sengane, Simon Mnyakeni Moleele","doi":"10.1515/hc-2022-0149","DOIUrl":"https://doi.org/10.1515/hc-2022-0149","url":null,"abstract":"Abstract Analogs of a new heterocyclic system were obtained from the reactions of 3-amino-1,2,4-triazine with coupling reagents such as boronic acids, and terminal alkynes in the presence of a palladium catalyst. Other reactions such as amination of the triazine at position 5, followed by electrophilic reactions with phenyl isocyanates and benzoyl chlorides, were performed to form new monoureido and benzoylated compounds.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"157 - 163"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45652832","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
Novel benzodioxatriaza and dibenzodioxadiazacrown compounds carrying 1,2,4-oxadiazole moiety 新型含1,2,4-恶二唑基团的苯并二氮杂和二苯并二氮杂冠化合物
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2022-01-01 DOI: 10.1515/hc-2022-0150
B. Özer, Y. Dürüst
{"title":"Novel benzodioxatriaza and dibenzodioxadiazacrown compounds carrying 1,2,4-oxadiazole moiety","authors":"B. Özer, Y. Dürüst","doi":"10.1515/hc-2022-0150","DOIUrl":"https://doi.org/10.1515/hc-2022-0150","url":null,"abstract":"Abstract A series of benzo (dibenzo)dioxadiaza and triazamacrocyclic ether compounds carrying 1,2,4-oxadiazole group has been successfully synthesized through N-substitution with 3-p-phenylsubstituted-5-chloromethyl-1,2,4-oxadiazoles. The structures of all the novel macrocycles were confirmed by spectral/physical data including HRMS measurements. Graphical abstract","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"139 - 148"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42295520","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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