Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences最新文献_第9页

Design, synthesis, and molecular docking study of novel cinnoline derivatives as potential inhibitors of tubulin polymerization. 新型肉桂碱衍生物作为微管蛋白聚合抑制剂的设计、合成和分子对接研究。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-03-28 DOI: 10.1515/znc-2022-0087

Eman Mohammad Mahmoud, Musa Shongwe, Ebrahim Saeedian Moghadam, Parsa Moghimi-Rad, Raphael Stoll, Raid Abdel-Jalil

{"title":"Design, synthesis, and molecular docking study of novel cinnoline derivatives as potential inhibitors of tubulin polymerization.","authors":"Eman Mohammad Mahmoud, Musa Shongwe, Ebrahim Saeedian Moghadam, Parsa Moghimi-Rad, Raphael Stoll, Raid Abdel-Jalil","doi":"10.1515/znc-2022-0087","DOIUrl":"https://doi.org/10.1515/znc-2022-0087","url":null,"abstract":"The preparation of a novel 4-methylbenzo[h] cinnolines entity via a three-step synthetic protocol is described. Cyclization of the naphthylamidrazones, in the presence of polyphosphoric acid (PPA), furnishes the respective target benzo[h]cinnolines directly. This one-pot synthesis involves intramolecular Friedel-Crafts acylation followed by instant elimination under heating conditions. It is noteworthy that the yield of the product from this step decreases dramatically if the heating is extended beyond 3 h. The target novel cinnolone derivatives were identified by mass spectrometry and their structures elucidated by spectroscopic techniques. Subsequently, molecular docking was performed to shed light on the putative binding mode of the newly synthesized cinnolines. The docking results indicate that these derivatives are potential inhibitors of tubulin polymerization and the best interaction was achieved with a computational ki = 0.5 nM and posed correctly over the lexibulin.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"78 3-4","pages":"123-131"},"PeriodicalIF":2.0,"publicationDate":"2023-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9086948","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

8-Amino-7-(aryl/hetaryl)fluoroquinolones. An emerging set of synthetic antibacterial agents. 8-Amino-7 -(芳基/ hetaryl)氟喹诺酮类原料药。一种新型的合成抗菌剂。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-03-28 DOI: 10.1515/znc-2022-0143

Ala'a A Al-Akhras, Jalal A Zahra, Mustafa M El-Abadelah, Lubna F Abu-Niaaj, Monther A Khanfar

{"title":"8-Amino-7-(aryl/hetaryl)fluoroquinolones. An emerging set of synthetic antibacterial agents.","authors":"Ala'a A Al-Akhras, Jalal A Zahra, Mustafa M El-Abadelah, Lubna F Abu-Niaaj, Monther A Khanfar","doi":"10.1515/znc-2022-0143","DOIUrl":"https://doi.org/10.1515/znc-2022-0143","url":null,"abstract":"This study reports the synthesis of seven new 8-amino-7-(aryl/hetaryl)fluoroquinolones and their antibacterial activity against 10 bacteria associated with microbial infections and foodborne illnesses. These fluoroquinolones are prepared via the reactions of selected aryl(hetaryl)boronic acids with ethyl-7chloro-6-fluoro-8-nitroquinolone-3-carboxylate, under Suzuki-Miyaura cross-coupling conditions. Nitro group reduction of the latter resulted in the corresponding 8-aminoquinolone-3-esters which upon hydrolysis formed the respective 8-amino-7-(aryl/hetaryl)-quinolone-3-carboxylic acids. The latter compounds were tested against selected Gram-negative bacteria (Escherichia coli, Salmonella typhimurium, Pseudomonas aeruginosa, Acinetobacter baumannii, and Klebsiella pneumonia) and Gram-positive bacteria (Enterococcus feacalis, Listeria monocytogenes, Streptococcus agalactiae, Staphylococcus epidermidis, and Staphylococcus aureus). The tested fluoroquinolones showed a significant antimicrobial activity against most of the tested bacterial strains. The antimicrobial activity of some of the tested compounds were comparable to or higher than a wide range of standard antibiotics including ampicillin, ciprofloxacin, and imipenem. The results highlight the new synthesized 8-amino-7-(aryl/hetaryl)fluroquinolones as promising candidates for new antimicrobial drugs to treat bacterial infections. This study highlights that the newly synthetic 8-amino-7-(aryl/hetaryl)fluroquinolones are promising candidates for new antimicrobial drugs to treat human diseases including foodborne illnesses.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"78 3-4","pages":"157-168"},"PeriodicalIF":2.0,"publicationDate":"2023-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9077932","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Thermodynamic control synthesis of spiro[oxindole-3,3'-pyrrolines] via 1,4-dipolar cycloaddition utilizing imidazo[1,5-a]quinoline. 咪唑[1,5-a]喹啉1,4偶极环加成法合成螺[氧吲哚-3,3'-吡咯]的热力学控制。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-03-28 DOI: 10.1515/znc-2022-0085

Areej M Jaber, Jalal A Zahra, Mustafa M El-Abadelah, Salim S Sabri, Dua'a S Sabbah

引用次数: 1

Design, synthesis and antimicrobial assessments of aminoacetylenic-piperazine nitroimidazole hybrid compounds. 氨基乙基-哌嗪-硝基咪唑杂化化合物的设计、合成及抗菌性能评价。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-03-28 DOI: 10.1515/znc-2022-0043

Anas J Rasras, Raed A Al-Qawasmeh, Mohamed El-Naggar, Ihsan Shehadi, Mahmoud M Elaasser, Yaseen A Al-Soud

引用次数: 0

Thiophene ring-opening reactions VI. Attempted cyclization towards [fused]-tricyclic system involving a thiolate anion and suitably located electrophilic carbon. 噻吩开环反应VI.对[融合]三环体系的尝试环化，包括一个硫代阴离子和合适位置的亲电碳。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-03-28 DOI: 10.1515/znc-2022-0080

Ahmad H Abdullah, Jalal A Zahra, Salim S Sabri, Firas F Awwadi, Ahmad Q Hussein, Mustafa M El-Abadelah

引用次数: 0

Nitroimidazoles Part 10. Synthesis, crystal structure, molecular docking, and anticancer evaluation of 4-nitroimidazole derivatives combined with piperazine moiety. 硝基咪唑第十部分。哌嗪基4-硝基咪唑衍生物的合成、晶体结构、分子对接及抗癌评价。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-03-28 DOI: 10.1515/znc-2022-0023

Yaseen A Al-Soud, Sadeekah O W Saber, Amneh Shtaiwi, Sondos O Alsawakhneh, Kafa' A S Alhelal, Qusay F A Salman, Luay Abu-Qatouseh, Monther A Khanfar, Raed A Al-Qawasmeh

{"title":"Nitroimidazoles Part 10. Synthesis, crystal structure, molecular docking, and anticancer evaluation of 4-nitroimidazole derivatives combined with piperazine moiety.","authors":"Yaseen A Al-Soud, Sadeekah O W Saber, Amneh Shtaiwi, Sondos O Alsawakhneh, Kafa' A S Alhelal, Qusay F A Salman, Luay Abu-Qatouseh, Monther A Khanfar, Raed A Al-Qawasmeh","doi":"10.1515/znc-2022-0023","DOIUrl":"https://doi.org/10.1515/znc-2022-0023","url":null,"abstract":"Piperazine-tagged imidazole derivatives 3a (symmetrical di-substituted piperazine) and 5-11 were synthesized through the combination of 4-nitroimidazole derivatives with piperazine moiety. The structural characterization was done by different physical and spectral techniques like NMR (1H and 13C) and mass spectrometry. The constituency of compound 3a was confirmed by X-ray structural analyses. All compounds were assessed for their antiproliferative inhibition potency against five human cancer cell lines namely MCF-7, PC3, MDA-231, A549 and Fibro dental. Compound 5 was found to be the most potent anticancer agents against MCF-7 cell line with IC50 values of (1.0 ± 0 µm) and against PC3 with IC50 value of (9.00 ± 0.028 µm). The molecular docking of compound 5 had been studied, and the results revealed that the newly designed 4-nitroimidazole combined with piperazine moiety derivatives bond to the hydrophobic pocket and polar contacts with high affinity.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"78 3-4","pages":"93-103"},"PeriodicalIF":2.0,"publicationDate":"2023-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9086453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Bioactive secondary metabolites from Trichoderma viride MM21: structure elucidation, molecular docking and biological activity. 绿色木霉MM21次生代谢产物的结构解析、分子对接及生物活性研究。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-03-28 DOI: 10.1515/znc-2021-0284

Mohamed Shaaban, Hamdi Nasr, Tahia K Mohamed, Samy F Mahmoud, Mohammad M El-Metwally, Ahmed B Abdelwahab

{"title":"Bioactive secondary metabolites from Trichoderma viride MM21: structure elucidation, molecular docking and biological activity.","authors":"Mohamed Shaaban, Hamdi Nasr, Tahia K Mohamed, Samy F Mahmoud, Mohammad M El-Metwally, Ahmed B Abdelwahab","doi":"10.1515/znc-2021-0284","DOIUrl":"https://doi.org/10.1515/znc-2021-0284","url":null,"abstract":"Four bioactive metabolites; ergosterol (1), peroxy ergosterol (2), α-cyclopiazonic acid (3) and kojic acid (4), were isolated from the fungal sp. Trichoderma viride MM21. Their structures were assigned by cumulative analysis of NMR and mass spectra, and comparison with literature. The antimicrobial activity of the fungus supernatant, mycelial cake, cumulative crude extract and compounds 1-4 was broadly studied against 11 diverse pathogens, revealing auspicious activity results. Based on the molecular docking, ergosterol (1) and peroxy ergosterol (2) were picked up to be computationally tested against topoisomerase IV of Staphylococcus aureus. The nominated enzyme is a possible target for the antibacterial activity of triterpenoidal/steroidal compounds. Compounds 1, 2 showed a deep inserting inside the enzyme groove recording a good binding affinity of -8.1 and -8.4 kcal/mol, respectively. Noteworthy that the antibacterial activity of ergosterol was higher (14-17 mm) than peroxy ergosterol (11-14 mm), although ergosterol formed only one hydrogen bond with the target, while peroxy ergosterol formed three hydrogen bonds. Such higher antibacterial activity of ergosterol may be attributed to its interference with other proteins included in this inhibition. The cytotoxic activity was tested against brine shrimp, revealing 100% mortality for the supernatant, crude extract and whole isolated compounds. Such strong cytotoxicity is attributed most likely to the abundant productivity/concentration of α-cyclopiazonic acid and kojic acid.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"78 3-4","pages":"149-156"},"PeriodicalIF":2.0,"publicationDate":"2023-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9077391","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Antibacterial, antioxidant, and cytotoxic activities of Syzygium aromaticum (L.) Merr. & Perry essential oil with identification of its chemical constituents. 香菇的抗菌、抗氧化和细胞毒活性稳定。& Perry精油及其化学成分的鉴定。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-03-28 DOI: 10.1515/znc-2022-0056

Wael A Al-Zereini, Ibrahim N Al-Trawneh, Mahmoud A Al-Qudah, Heba M TumAllah, Zead H Abudayeh, Tahani Hijazin

{"title":"Antibacterial, antioxidant, and cytotoxic activities of Syzygium aromaticum (L.) Merr. & Perry essential oil with identification of its chemical constituents.","authors":"Wael A Al-Zereini, Ibrahim N Al-Trawneh, Mahmoud A Al-Qudah, Heba M TumAllah, Zead H Abudayeh, Tahani Hijazin","doi":"10.1515/znc-2022-0056","DOIUrl":"https://doi.org/10.1515/znc-2022-0056","url":null,"abstract":"Aromatic plants embrace volatile compounds with efficiency in treating different diseases. In Jordan, Syzygium aromaticum flower buds (clove) are extensively used as folk medicine without awareness of its bio-safe dosage. Herein, clove buds were hydrodistilled using the Clevenger apparatus, and the resulting essential oil (CEO) was analyzed using Gas Chromatography-Mass Spectrometry (GC-MS). The antibacterial activity was evaluated against tested bacterial strains by agar diffusion test and micro-broth dilution assay. The antioxidant capacity was assessed using DPPH radical scavenging assay, while the cytotoxic potency was unraveled by determination of its anti-proliferative activity against MDA-MB-231 breast adenocarcinoma and normal Vero cell lines. CEO yield was 5.7 ± 1.3% (w/w); encompassed 24 volatile ingredients with eugenol as the principal compound (73.41%). The CEO inhibited the growth of both Gram-positive and Gram-negative bacterial test strains, causing the formation of 13.7 ± 1.5-17.3 ± 0.6 mm and 11.7 ± 1.5-20.7 ± 1.2 mm inhibition zones, respectively with MIC 1.25-5 μL/mL. Moreover, it showed antioxidant activity with IC50 0.0016 ± 0.0001 μL/mL (1.6 ± 0.1 μg/mL, 2.98 ± 0.4 µg Trolox®/µg CEO). Intriguingly, the CEO was cytotoxic against both cancerous and noncancerous cell lines at IC50 of 0.25 ± 0.02 μL/mL and 0.18 ± 0.01 μL/mL, respectively. Herein results unveil the potential application of CEO as a pharmaceutical remedy with considering its bio-safe dosage.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"78 3-4","pages":"105-112"},"PeriodicalIF":2.0,"publicationDate":"2023-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9086456","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Organic chemistry and medicinal applications. 有机化学和医药应用。

IF 1.8 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-02-24 Print Date: 2023-03-28 DOI: 10.1515/znc-2023-0013

Raid Abdel-Jalil, Raphael Stoll

引用次数: 0

Proximate analysis and fatty acid, mineral and soluble carbohydrate profiles of some brown macroalgae collected from Türkiye coasts. 从图尔基耶海岸采集的一些棕色大型藻类的近似分析及脂肪酸、矿物质和可溶性碳水化合物概况。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-02-24 Print Date: 2023-07-26 DOI: 10.1515/znc-2022-0195

Aysun Yucetepe, Elif Feyza Aydar, Emine Şükran Okudan, Beraat Özçelik, Gökhan Durmaz

{"title":"Proximate analysis and fatty acid, mineral and soluble carbohydrate profiles of some brown macroalgae collected from Türkiye coasts.","authors":"Aysun Yucetepe, Elif Feyza Aydar, Emine Şükran Okudan, Beraat Özçelik, Gökhan Durmaz","doi":"10.1515/znc-2022-0195","DOIUrl":"10.1515/znc-2022-0195","url":null,"abstract":"In this study, the fatty acid, carbohydrate, and mineral profiles and proximate composition of Halopteris scoparia, Padina pavonica, Zanardinia typus, Cladostephus spongiosum, Sargassum vulgare, and Sargassum acinarium brown macroalgae collected from Türkiye seas were determined. According to the results, the ash and total carbohydrate contents of all macroalgae ranged from 20.79 to 53.49% in dry weight (dw) and from 15.32 to 55.13% dw, respectively. Their protein, lipid and crude fiber contents changed between 4.22 and 9.89% dw, 0.25 and 0.90% dw, and 12.28 and 16.01% dw, respectively. Palmitic acid (29.36-48.55% dw) and oleic acid (8.92-20.92% dw) were at the highest levels in all brown macroalgae. In addition, they included prominent levels of saturated fatty acids (51.87-69.56% dw of total fatty acid content). Magnesium (6.97-18.78 mg/kg dw), potassium (1.34-3.78 mg/kg dw), iron (1.27-8.24 mg/kg dw), and manganese (63.10-252.23 μg/kg dw) were found to be the major minerals. The main soluble carbohydrates of macroalgae were found to be mannitol (1149.99-8676.31 mg/kg dw), glucose (368.78-1305.59 mg/kg dw), myo-inositol (225.96-956.78 mg/kg dw), fructose (137.05-689.21 mg/kg dw), and sucrose (189.55-328.06 mg/kg dw). This study revealed that brown macroalgae are particularly rich in potassium, magnesium, iron, manganese, and zinc and they may have potential for use in the food industry.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"78 7-8","pages":"261-269"},"PeriodicalIF":2.0,"publicationDate":"2023-02-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10260269","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0