Heteroatom Chemistry最新文献

Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives 一些新的2,3-二氢-1,5-苯二氮卓类衍生物的抗癌和抗菌活性

4区化学

Heteroatom Chemistry Pub Date : 2023-11-06 DOI: 10.1155/2023/3390122

Felix Odame, Tatenda Madanhire, Clement Tettey, David Neglo, Francisca Adzaho, Daniel Sedohia, Eric C. Hosten

{"title":"Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives","authors":"Felix Odame, Tatenda Madanhire, Clement Tettey, David Neglo, Francisca Adzaho, Daniel Sedohia, Eric C. Hosten","doi":"10.1155/2023/3390122","DOIUrl":"https://doi.org/10.1155/2023/3390122","url":null,"abstract":"A series of 2,3-dihydro-1,5-benzodiazepine derivatives have been synthesized and characterized using IR, NMR, GC-MS, single crystal XRD, and microanalysis. The results of their antibacterial activity against methicillin-resistance Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Bacillus subtilis, Streptococcus mutans, Pseudomonas aeruginosa, Salmonella typhi, and Streptococcus pyrogens indicated that most of the compounds were bacteriostatic (0.125−4 mg/mL) and also exhibited good biofilm inhibition (0.21−72.69%). The compounds were found to be synergistic when used in combination with other antibiotics. The antiproliferative and cytotoxic effects were also investigated against PC-3 prostate cancer and RAW 264.7 macrophage cell lines, respectively, using the MTT assay. Apart from compounds 6 and 7, a good number of the compounds (1, 2, 3, 4, 5, and 8) were selectively toxic to the prostate cancer cells at 20 µM, whilst sparing the normal cells. Compound 3 demonstrated the highest antiprostate cancer effect by reducing the viability of PC-3 cells to (13.75%), which was followed by compounds 1 (47.72%), 2 (48.18%), 4 (62.61%), 5 (66.70%), and 8 (69.55%).","PeriodicalId":12816,"journal":{"name":"Heteroatom Chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135590201","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

Novel Thioethers of Dihydroartemisinin Exhibiting Their Biological Activities 新型双氢青蒿素硫醚类化合物的生物活性研究

IF 0.3 4区化学

Heteroatom Chemistry Pub Date : 2023-02-09 DOI: 10.1155/2023/6761186

Ngoc-Hung Truong, Thị Ngọc Lam Trần, K. Hoang, D. Ninh, Viet Duc Le, Duc Anh Le, V. Luu

引用次数: 1

Synthesis, Spectral Characterization, and Biological Activities of Some Metal Complexes Bearing an Unsymmetrical Salen-Type Ligand, (Z)-1-(((2-((E)-(2-Hydroxy-6-methoxybenzylidene)amino)phenyl)amino) methylene) Naphthalen-2(1H)-one 非对称Salen型配体（Z）-1-（（（2-（（E）-（2-羟基-6-甲氧基亚苄基）氨基）苯基）氨基）亚甲基）萘-2（1H）-酮金属配合物的合成、光谱表征和生物活性

IF 0.3 4区化学

Heteroatom Chemistry Pub Date : 2023-02-04 DOI: 10.1155/2023/4563958

Quang Trung Nguyen, Phuong Nam Pham Thi, Quang Do Bui, Van Tuyen Nguyen

引用次数: 1

Synthesized Phosphonium Compounds Demonstrate Resistant Modulatory and Antibiofilm Formation Activities against Some Pathogenic Bacteria 合成的磷化合物对某些病原菌具有抗性调节和抗生物膜形成活性

IF 0.3 4区化学

Heteroatom Chemistry Pub Date : 2022-09-26 DOI: 10.1155/2022/7411957

Cedric Dzidzor Kodjo Amengor, Cynthia Amaning Danquah, E. B. A. Adusei, F. K. Kekessie, Francis Ofosu-Koranteng, Paul Peprah, B. Harley, E. Orman, J. Adu, Yussif Saaka

{"title":"Synthesized Phosphonium Compounds Demonstrate Resistant Modulatory and Antibiofilm Formation Activities against Some Pathogenic Bacteria","authors":"Cedric Dzidzor Kodjo Amengor, Cynthia Amaning Danquah, E. B. A. Adusei, F. K. Kekessie, Francis Ofosu-Koranteng, Paul Peprah, B. Harley, E. Orman, J. Adu, Yussif Saaka","doi":"10.1155/2022/7411957","DOIUrl":"https://doi.org/10.1155/2022/7411957","url":null,"abstract":"A library of six compounds with new hybrids in a single molecule triazole ring attached to the phosphonium salts was synthesized. Click chemistry was, however, used to synthesize the 1-, 2-, and 3-triazole intermediates as a tether for the hybrid phosphonium salts. Their antibacterial activity against Gram-positive bacteria (Staphylococcus aureus and Enterococcus faecalis), Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa), and Mycobacterium smegmatis mc2155 was determined using the HT-SPOTi assay. Compound 2 showed the most effective antimicrobial activity as it inhibited the growth of Pseudomonas aeruginosa and Staphylococcus aureus at 0.0125 µg/mL and 31.25 µg/mL, respectively. From the FICI data, compounds 2ET-TOL (2) and RABYL-TOL (4) successfully modulated the activities of amoxicillin against Pseudomonas aeruginosa and Staphylococcus aureus. All the test compounds exhibited a concentration-dependent biofilm formation inhibition against S. aureus, except P-Z (compound 6). Compounds P-MEOXY (1) and 2ET-TOL (2) exhibited mild activity against P. aeruginosa with compound 4 showing antimycobacterial activity at 500 µg/mL.","PeriodicalId":12816,"journal":{"name":"Heteroatom Chemistry","volume":null,"pages":null},"PeriodicalIF":0.3,"publicationDate":"2022-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44750461","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: 1

Synthesis, Structure, and Antifungal Activities of 3-(Difluoromethyl)-Pyrazole-4-Carboxylic Oxime Ester Derivatives 3-(二氟甲基)-吡唑-4-羧基肟酯衍生物的合成、结构和抗真菌活性

IF 0.3 4区化学

Heteroatom Chemistry Pub Date : 2022-08-28 DOI: 10.1155/2022/6078017

Bin Wang, Wei-Ting Chen, Li-Jing Min, L. Han, Na-Bo Sun, Xinghai Liu

引用次数: 2

Isolation, Synthesis, and Fungicidal Activity of Isopropyl (3-methyl-1-oxo-1-((1-((4-(prop-2-yn-1-yloxy)phenyl)thio)propan-2-yl)amino)butan-2-yl)carbamate Diastereomers against Phytophthora capsici 3-甲基-1-氧代-1-（（1-（（4-（丙-2-炔-1-基氧基）苯基）硫基）丙-2-基）氨基）丁-2-基氨基甲酸异丙酯双立体异构体的分离、合成及其对辣椒疫霉的杀菌活性

IF 0.3 4区化学

Heteroatom Chemistry Pub Date : 2022-08-05 DOI: 10.1155/2022/4678338

Lei Tian, Yang Gao, Xing-Jie Peng, Cheng Zhang, Wei-Guang Zhao, Xing-Hai Liu

引用次数: 0

Triazoles Synthesis & Applications as Nonsteroidal Aromatase Inhibitors for Hormone-Dependent Breast Cancer Treatment 三唑类非甾体芳香化酶抑制剂的合成及其在激素依赖性乳腺癌症治疗中的应用

IF 0.3 4区化学

Heteroatom Chemistry Pub Date : 2022-04-28 DOI: 10.1155/2022/5349279

Huda R. M. Rashdan, Ihsan A. Shehadi

{"title":"Triazoles Synthesis & Applications as Nonsteroidal Aromatase Inhibitors for Hormone-Dependent Breast Cancer Treatment","authors":"Huda R. M. Rashdan, Ihsan A. Shehadi","doi":"10.1155/2022/5349279","DOIUrl":"https://doi.org/10.1155/2022/5349279","url":null,"abstract":"In the last few years, nonsteroidal aromatase inhibitors (AIs) have been emerged as promising agents for treating hormone-dependent breast cancer in postmenopausal women because of their inhibitory effect on estrogen synthesis. Indeed, these compounds can block the activity of aromatase, the enzyme that intervenes in the last steps of estrogen production pathway. Triazoles are the core structures of nonsteroidal AIs. The nitrogen atom of the triazole moiety plays a fundamental role in the aromatase functionality by interacting with the iron ions of the heme group. In general, AIs possess numerous advantages as they quench the last step of estrogen synthesis without any inhibitory effects on the production of other steroids produced via the same pathway. Some AIs as anastrozole, letrozole, and vorozole have already been approved by the Food and Drug Administration in the treatment of breast cancer. The previously mentioned compounds present severe and adverse effects as polycystic ovary syndrome (PCOS), resistance onset on long-term treatments, and a higher risk of bone fractures. This review focuses intensively on the role of AIs in the treatment of hormone-sensitive types of cancers, especially the role of triazoles as nonsteroidal AIs. Also, the review provides an overview about the chemistry of triazoles along with the different methods by which the \u0000 \u0000 v\u0000 \u0000 -triazoles and s-triazoles are synthesized.","PeriodicalId":12816,"journal":{"name":"Heteroatom Chemistry","volume":null,"pages":null},"PeriodicalIF":0.3,"publicationDate":"2022-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44011713","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: 8

Reexamining Povarov Reaction’s Scope and Limitation in the Generation of HCV-NS4A Peptidomimetics 对Povarov反应在HCV-NS4A类多肽产生中的作用范围和局限性的再研究

IF 0.3 4区化学

Heteroatom Chemistry Pub Date : 2022-02-10 DOI: 10.1155/2022/8181543

M. Khayat, A. Omar, M. Elfaky, Yosra A. Muhammad, Elaf A. Felemban, K. El-Say, M. El‐Araby

{"title":"Reexamining Povarov Reaction’s Scope and Limitation in the Generation of HCV-NS4A Peptidomimetics","authors":"M. Khayat, A. Omar, M. Elfaky, Yosra A. Muhammad, Elaf A. Felemban, K. El-Say, M. El‐Araby","doi":"10.1155/2022/8181543","DOIUrl":"https://doi.org/10.1155/2022/8181543","url":null,"abstract":"Chronic Hepatitis C is a global health threat and a silent killer. Regardless of the profound progress in preventing and treating this disease, research continues to discover new direct antiviral agents (DAAs), especially against novel targets. Our research has been directed to leverage the NS4A binding site to develop peptidomimetic inhibitors of the hepatitis C virus (HCV) NS3 protease. In previous reports, we could provide evidence of tunability of this site by peptide and nonpeptide NS3/4A inhibitors. In this report, we used structure-based techniques to design 1,2,3,4-tetrahydro-1,7-naphthyridine derivative as NS4A core mimics that cover the region between residues Ile-25′ to Arg-28′. The synthetic plan featured the Povarov reaction as an efficient strategy to construct the 1,7-naphthyridine core. Although this reaction has been reported in many literatures, critical assessments for its scope and limitations are scarce. In our work, we found that Povarov was extremely sensitive to alkene and aldehyde reactants. Moreover, using pyridine amines was not as successful as anilines. The most striking results were the lack of stability of compounds during purification and storage. The four compounds that survived the stability problems (1a-1d) did not show significant binding potency with NS3, because their structures were too simple to resemble the originally planned compounds.","PeriodicalId":12816,"journal":{"name":"Heteroatom Chemistry","volume":null,"pages":null},"PeriodicalIF":0.3,"publicationDate":"2022-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49304458","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

Cyclization Reactions Involving 2-Aminoarenetellurols and Derivatives of α,β-Unsaturated Carboxylic Acids 2-氨基芳烃四元及α，β-不饱和羧酸衍生物的环化反应

IF 0.3 4区化学

Heteroatom Chemistry Pub Date : 2021-12-22 DOI: 10.1155/2021/7140222

J. A. Patel, Aundrea M. Lee, D. V. Franklin, F. Fronczek, T. Junk

引用次数: 0

A Remarkably Efficient Phase-Transfer Catalyzed Amination of α-Bromo-α, β-Unsaturated Ketones in Water 相转移催化α-溴-α， β-不饱和酮在水中的高效胺化反应

IF 0.3 4区化学

Heteroatom Chemistry Pub Date : 2021-01-04 DOI: 10.1155/2021/6616458

Alemayehu Mekonnen, A. Tesfaye

引用次数: 1