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Novel Hydralazine Schiff Base Derivatives and Their Antimicrobial, Antioxidant and Antiplasmodial Properties 新型肼嗪席夫碱衍生物及其抗菌、抗氧化和抗等离子体性质
有机化学国际期刊(英文) Pub Date : 2020-03-05 DOI: 10.4236/ijoc.2020.101001
A. F. Awantu, Y. Fongang, Godfred A. Ayimele, E. Nantia, P. Fokou, F. Boyom, Celine K. Ngwang, B. Lenta, S. Ngouela
{"title":"Novel Hydralazine Schiff Base Derivatives and Their Antimicrobial, Antioxidant and Antiplasmodial Properties","authors":"A. F. Awantu, Y. Fongang, Godfred A. Ayimele, E. Nantia, P. Fokou, F. Boyom, Celine K. Ngwang, B. Lenta, S. Ngouela","doi":"10.4236/ijoc.2020.101001","DOIUrl":"https://doi.org/10.4236/ijoc.2020.101001","url":null,"abstract":"Two novel Schiff bases, 3-[1-(2-(phthalazin-1-yl)hydrazono)ethyl)-1,3-oxa- zinane (PHEO) and 2-[(2-(phthalazin-1-yl)hydrazono)methyl]phenol (PHMP), derived from hydralazine hydrochloride, an effective drug against hypertension, were synthesized and characterized by spectroscopic methods, Infrared (IR), Proton Nuclear Magnetic Resonance (1H NMR) and Carbon-13 Nuclear Magnetic Resonance (13C NMR). PHEO showed low antimicrobial activity against one bacterial strain with MIC value of 250 μg/ml while PHMP showed interesting activity against 4 bacterial strains with MIC of 31.25 - 250 μg/ml compared to the standard drug, amoxicillin. PHEO and PHMP showed higher reducing activity on ferric ions compared to Vitamin C. On lipid peroxidation, PHEO showed higher inhibition while PHMP showed lower inhibition compared to Vitamin C. Both compounds presented lower stimulating effect and lower catalase activity compared to the standard Vitamin C. PHEO and PHMP showed less than 80% inhibition in the preliminary antiplasmodial assay and so were not considered for the dose-response studies.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42660638","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 4
Mannich-Type Reaction of Aldimines with 2-Silyloxydienes Catalyzed by Ammonium Chloride 氯化铵催化醛亚胺与2-硅氧基二烯的Mannich型反应
有机化学国际期刊(英文) Pub Date : 2019-11-25 DOI: 10.4236/ijoc.2019.94014
Shoichi Fukumoto, Miho Shigenobu, K. Ishimaru
{"title":"Mannich-Type Reaction of Aldimines with 2-Silyloxydienes Catalyzed by Ammonium Chloride","authors":"Shoichi Fukumoto, Miho Shigenobu, K. Ishimaru","doi":"10.4236/ijoc.2019.94014","DOIUrl":"https://doi.org/10.4236/ijoc.2019.94014","url":null,"abstract":"Reaction of imines with 2-silyloxydiene catalyzed by ammonium chloride has been perfectly proceeded under environmentally friendly conditions to give Mannich-type product selectively. The reaction would proceed via Mannich-type mechanism, not cyclization/ring-opening process. Cyclopropanation of the corresponding Mannich-type product gave the precursor of prasugrel skeleton in high yield.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-11-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42760536","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Trisubstituted Aryl Cyclohexanecarboxylates (TACC): A Simple, New Molecular Scaffold for Antibiotics Design 三取代芳基环己anecarboxylates (TACC):一种简单的新型抗生素设计分子支架
有机化学国际期刊(英文) Pub Date : 2019-09-18 DOI: 10.4236/ijoc.2019.93013
Olusegun B. Olubanwo, Arianna H. Kazez, D. Carney, J. Sello
{"title":"Trisubstituted Aryl Cyclohexanecarboxylates (TACC): A Simple, New Molecular Scaffold for Antibiotics Design","authors":"Olusegun B. Olubanwo, Arianna H. Kazez, D. Carney, J. Sello","doi":"10.4236/ijoc.2019.93013","DOIUrl":"https://doi.org/10.4236/ijoc.2019.93013","url":null,"abstract":"A new class of potential antibacterial agents has been synthesized on a new molecular scaffold of cyclohexane carboxylate. We have tagged this new class of compounds TACCs (Trisubstituted Aryl Cyclohexanecarboxylate). These new molecules are structural analogues of an Activators of Self-Compartmentalizing Proteases 4 and 5 (ACP 4 and 5), and were synthesized to circumvent the drug-like property (drug-ability) challenges and liability noted in ACP 4 and 5. A pseudo-Robinson annulation protocol was used to furnish this new class of potential antibiotics. Structure-activity relationship (SAR) study was done to identify the pharmacophore(s) in this molecular scaffold. A selection of these compounds was used in our preliminary antibacterial inhibitory activities’ studies on Bacillus mycoides and Bacillus subtilis. These preliminary studies show that the TACCs exhibited equal, and in some cases better, antibacterial activity than ACP 4 and 5.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43141068","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Facile Synthesis of Bis-Trifluoromethyl 1,8-Dioxo-Octahydroxanthene Derivatives 双-三氟甲基1,8-二氧八羟基蒽衍生物的简易合成
有机化学国际期刊(英文) Pub Date : 2019-08-13 DOI: 10.4236/IJOC.2019.93011
Cosmas O. Okoro, M. A. Ogunwale, A. Oyedele
{"title":"Facile Synthesis of Bis-Trifluoromethyl 1,8-Dioxo-Octahydroxanthene Derivatives","authors":"Cosmas O. Okoro, M. A. Ogunwale, A. Oyedele","doi":"10.4236/IJOC.2019.93011","DOIUrl":"https://doi.org/10.4236/IJOC.2019.93011","url":null,"abstract":"Xanthene and Xanthenediones are structural components of several bioactive and semi-synthetic molecules. This work described an expeditious synthesis of novel and hitherto unreported bis-trifluoromethyl xanthene dione derivatives. The reaction of two equivalents of 5-trifluoromethyl cyclohexane-1,3- dione with substituted aromatic aldehydes in the presence of ethanol containing 1 - 2 drops of HCl was facile under microwave irradiation. Short reaction time (25 min), good to excellent yields (80% - 95%), good atom economy, and simple workup are the major advantages of the above procedure. Moreover, the fluorinated products represent synthetically useful stable intermediates that could find applications in pharmaceutical, agricultural and material industries.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-08-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43661372","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Water Chemistry in Oil and Gas Operations: Scales Properties and Composition 石油和天然气作业中的水化学:鳞片性质和组成
有机化学国际期刊(英文) Pub Date : 2019-07-10 DOI: 10.4236/ijoc.2019.93012
A. Taha, M. Amani
{"title":"Water Chemistry in Oil and Gas Operations: Scales Properties and Composition","authors":"A. Taha, M. Amani","doi":"10.4236/ijoc.2019.93012","DOIUrl":"https://doi.org/10.4236/ijoc.2019.93012","url":null,"abstract":"Oil and gas operations depend heavily on water in many different aspects. Water is present wherever there is hydrocarbon production. It is produced along with the hydrocarbons and helps in mobilizing them. It is also injected into the reservoirs to aid in mobilizing the hydrocarbons, maintain the pressure and increase the recovery of the development project. With water presence, some serious problems occur such as scaling. Scaling is a well-known problematic precipitation caused mainly due to mixing of two incompatible fluids, changes in temperature and pressure conditions and disturbance to thermodynamics and kinetics of reservoir fluids. They can be found at any point of the operations starting down at the formation up to the surface tanks. Scales are directly responsible for compromising the economics and safety of development projects. This review paper is going to include a recap of the importance of water in the oil and gas industry, then review the different types of scales as well as their properties including carbonate and sulfate scales. After that, famous scales from each type is going to be reviewed as well as their properties and precipitation conditions such as Calcium Carbonate CaCO3, Calcium Sulfate CaSO4, Barium Sulfate BaSO4 and Strontium Sulfate SrSO4. Moreover, common practices and precautions steps in the industry are going to be reviewed as well. Finally, the paper presents the common practices used by the operators for scale removal.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47806463","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Nucleosides 10: Synthesis of New Derivatives of Pyrimidine and Fused Pyrimidine Nucleosides of Expected Biological Activity 核苷10:具有预期生物活性的新型嘧啶衍生物和融合嘧啶核苷的合成
有机化学国际期刊(英文) Pub Date : 2019-07-10 DOI: 10.4236/IJOC.2019.93010
L. M. Break, M. A. Mohamed, Ohoud A. A. Al-Thubaiti, Fatma E. M. Eibaih
{"title":"Nucleosides 10: Synthesis of New Derivatives of Pyrimidine and Fused Pyrimidine Nucleosides of Expected Biological Activity","authors":"L. M. Break, M. A. Mohamed, Ohoud A. A. Al-Thubaiti, Fatma E. M. Eibaih","doi":"10.4236/IJOC.2019.93010","DOIUrl":"https://doi.org/10.4236/IJOC.2019.93010","url":null,"abstract":"Pyrimidines, such as 6-amino-2-thio and 2-methylthiouracils and fused pyrimidines, such as thienopyrimidines reacted with 1-O-acetyl-2,3,5-tri-O- benzoyl-β-D-ribofuranose to get new derivatives of the corresponding nucleosides. The obtained protected nucleosides were deprotected by methanolic sodium methoxide to get the corresponding free uracil and thienopyrimidine nucleosides. The new nucleosides formed were tested for biological activity against some of microorganism (some fungi and bacteria species). Some of the tested products showed moderate activity and the results were reported.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49103900","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
Progress toward the Synthesis of Pochonin J Pochonin J的合成研究进展
有机化学国际期刊(英文) Pub Date : 2019-06-11 DOI: 10.4236/IJOC.2019.92009
Sydney N Jackson, R. Pongdee
{"title":"Progress toward the Synthesis of Pochonin J","authors":"Sydney N Jackson, R. Pongdee","doi":"10.4236/IJOC.2019.92009","DOIUrl":"https://doi.org/10.4236/IJOC.2019.92009","url":null,"abstract":"The construction of the C(1) - C(5) fragment of the resorcylic acid lactone pochonin J is described. The synthesis is marked by the installation of the cis-1,3-diol moiety in a highly stereoselective manner using Evans’ intra-molecular base-catalyzed oxyconjugate addition of a hemiacetal-derived nucleophile. The synthetic route presented affords an efficient pathway to the preparation of this critical architectural feature that should facilitate the development of this secondary metabolite as a potential drug candidate.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42839192","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","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 Novel 4-Thiazolidinone and Bis-Thiazalidin-4-One Derivatives Derived from 4-Amino-Antipyrine and Evaluated as Inhibition of Purine Metabolism Enzymes by Bacteria 新型4-氨基安替比林衍生物的合成及对细菌嘌呤代谢酶的抑制作用
有机化学国际期刊(英文) Pub Date : 2019-06-11 DOI: 10.4236/IJOC.2019.92008
R. -Rahman, Abdulrahman S. Alharbi, N. A. Alshammari
{"title":"Synthesis of Novel 4-Thiazolidinone and Bis-Thiazalidin-4-One Derivatives Derived from 4-Amino-Antipyrine and Evaluated as Inhibition of Purine Metabolism Enzymes by Bacteria","authors":"R. -Rahman, Abdulrahman S. Alharbi, N. A. Alshammari","doi":"10.4236/IJOC.2019.92008","DOIUrl":"https://doi.org/10.4236/IJOC.2019.92008","url":null,"abstract":"Novel 4-thiazolidione and 1,4-bis-thiazolidinone derivatives bearing antipyrine moiety have been obtained from condensation of 4-aminoantipyrine 1 with aromatic/heteroaldehydes followed by cycloaddition with mercaptoacetic acid in nonpolar solvents. Structure of the products has been deduced upon their elemental analysis and spectral measurements. Most of the targets evaluated as enzymatic effect towards some bacteria (E. coli) in compare with Xanthine oxidase (from buttermilk) where the role of compounds is an inhibition of purine metabolism enzymes caused by E. coli.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48998369","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
Efficient Cross-Coupling Reaction of Aryltrifluoroborates and Aroyl Chlorides for the Synthesis of Fluorine Substituted Aromatic Ketones 三氟硼酸芳酯与芳酰氯高效交联反应合成氟取代芳酮
有机化学国际期刊(英文) Pub Date : 2019-03-18 DOI: 10.4236/IJOC.2019.91006
Mohammed Al-Masum, Tasfia Islam, Grady Clopton
{"title":"Efficient Cross-Coupling Reaction of Aryltrifluoroborates and Aroyl Chlorides for the Synthesis of Fluorine Substituted Aromatic Ketones","authors":"Mohammed Al-Masum, Tasfia Islam, Grady Clopton","doi":"10.4236/IJOC.2019.91006","DOIUrl":"https://doi.org/10.4236/IJOC.2019.91006","url":null,"abstract":"The direct aroylation of ArCOPdCl with potassium aryltrifluoroborates establishes a new cross-coupling synthetic tool for the synthesis of various fluorine substituted benzophenones. The new microwave irradiated process is very efficient and produce high yield benzophenone products within minutes.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44911101","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","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 Novel Heteropolycyclic Nitrogen Systems Bearing Fluorine Substituted Pyrazolo[3,4-d] Pyrimidine Derived from Polyfunctional π-Acceptor Compounds and Guanidine as Fungicidal Probes 含氟取代吡唑并[3,4-d]嘧啶的多功能π-受体化合物和胍的新型杂环氮体系的合成
有机化学国际期刊(英文) Pub Date : 2019-01-11 DOI: 10.4236/IJOC.2019.91007
D. Bakhotmah, Salwa Y. Al-Hazme
{"title":"Synthesis of Novel Heteropolycyclic Nitrogen Systems Bearing Fluorine Substituted Pyrazolo[3,4-d] Pyrimidine Derived from Polyfunctional π-Acceptor Compounds and Guanidine as Fungicidal Probes","authors":"D. Bakhotmah, Salwa Y. Al-Hazme","doi":"10.4236/IJOC.2019.91007","DOIUrl":"https://doi.org/10.4236/IJOC.2019.91007","url":null,"abstract":"Novel heteropolycyclic nitrogen systems bearing fluorine substituted pyrazolo[3,4-d] pyrimidine moiety have been synthesis by the interaction between N’-heteroaryl guanidine 4 with polyfunctional π-acceptors in different media and condition. The structures of the synthesis compounds were established by spectroscopic analysis and evaluated as antifungal probes in various concentration.","PeriodicalId":64796,"journal":{"name":"有机化学国际期刊(英文)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43537147","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
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