Heterocycles - Synthesis and Biological Activities最新文献

One-Pot-Condensation Reaction of Heterocyclic Amine, 1,3-Diketone and Aldehydes Using In Situ Generated Superoxide Ion: A Rapid Synthesis of Structurally Diverse Drug-Like Complex Heterocycles 利用原位生成的超氧离子进行杂环胺、1,3-二酮和醛的一锅缩合反应:快速合成结构多样的类药物杂环复合物

Heterocycles - Synthesis and Biological Activities Pub Date : 2020-06-10 DOI: 10.5772/intechopen.81146

Sundaram Singh, S. Kumari

{"title":"One-Pot-Condensation Reaction of Heterocyclic Amine, 1,3-Diketone and Aldehydes Using In Situ Generated Superoxide Ion: A Rapid Synthesis of Structurally Diverse Drug-Like Complex Heterocycles","authors":"Sundaram Singh, S. Kumari","doi":"10.5772/intechopen.81146","DOIUrl":"https://doi.org/10.5772/intechopen.81146","url":null,"abstract":"A novel, convenient one-pot multicomponent synthesis of tetraheterocy-clicbenzimidazolo/benzothiazolo quinazolin-1-one derivatives has been reported in the presence of tetraethylammonium superoxide under non-aqueous condition. The superoxide induced three-component reaction of various aromatic aldehydes, 2-aminobenzimadazole/2-aminobenzothiazole and dimedone/1,3- cyclohexane-dione produced tetraheterocyclicbenzimidazolo/benzothiazolo quinazolin-1-one derivatives at room temperature under the mild reaction conditions. The tetraethylammonium superoxide has been generated by phase transfer reaction of potassium superoxide and tetraethylammonium bromide in dry DMF at room temperature. The present study extended the applicability of tetraethylammonium bromide as a phase transfer catalyst for the efficient use of superoxide ion in multi-component synthesis of structurally diverse drug-like complex heterocycles (quinazolines). role of O 2 • − in living cells. Since the investigation has been performed at an ambient temperature in the presence of in situ generated O 2• − , the results may be easily correlated with those occurring at physiological temperatures in more complex biological counterparts. A novel synthetic route has been developed for the synthesis of tetraheterocyclic benzimidazolo/benzothiazolo quinazolin-1-one ring systems using tetraethylammonium superoxide under non aqueous condition at room temperature (mild reaction condition) within 6 h. The yield of the products was obtained up to 88% without using any tedious purification process. The applicability of tetraethylammonium bromide as an inexpensive alternative to 18-crown-6 for superoxide ion generation has been extended in present report.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"126136482","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

Introductory Chapter: Synthesis and Antimicrobial Activities of Dihydroazeto[2′,3′:4,5]seleno[2,3-b]quinolines 导论:二氢偶氮[2 '，3 ':4,5]硒[2,3-b]喹啉的合成及其抗菌活性

Heterocycles - Synthesis and Biological Activities Pub Date : 2020-06-10 DOI: 10.5772/intechopen.92030

B. Nandeshwarappa, G. Prakash, S. Sadashiv

引用次数: 0

Potent Antibacterial Profile of 5-Oxo-Imidazolines in the New Millennium 新千年5-氧-咪唑类药物的有效抗菌谱

Heterocycles - Synthesis and Biological Activities Pub Date : 2020-06-10 DOI: 10.5772/intechopen.81269

Roshan D. Nasare, M. Idrees, Satish S. Kola, Rajendra S. Dongre

{"title":"Potent Antibacterial Profile of 5-Oxo-Imidazolines in the New Millennium","authors":"Roshan D. Nasare, M. Idrees, Satish S. Kola, Rajendra S. Dongre","doi":"10.5772/intechopen.81269","DOIUrl":"https://doi.org/10.5772/intechopen.81269","url":null,"abstract":"Pharmaceutics and therapeutics industries enforced chemists to seek/discover antibacterial novel heterocycles owing specific bioactivity and innate characteristics significance. This chapter summarized potent antibacterial profile of 5-oxoimidazolines in the new millennium as an antibacterial against Gram-positive and Gram-negative bacteria viz. B. thuringiensis, S. aureus, E. coli, and E. aerogenes is presented in this chapter. 5-(H/Br benzofuran-2-yl)-1-phenyl 1H-pyrazole-3carbohydrazides are condensed with 4-(arylidene)-2 phenyloxazol-5(4H)-one in acetic acid at elevated temperature to yield product 5-(H/Br benzofuran-2-yl)-N(4-arylidene-5-oxo-2-phenyl-4,5-dihydroimidazol-1-yl)-1-phenyl-1H-pyrazole-3carboxamides. Different substrates like 4-(arylidene)-2-phenyloxazol-5(4H)-one allowed to react with benzaldehyde hippuric acid to yield 5-oxo-imidazolines/ 5-oxo-4,5-dihydroimidazole. All synthesized 5-oxo-imidazolines were characterized via elemental analysis and FT-IR, H-NMR and mass spectra techniques. All 5-oxo-imidazolines assayed in vitro for inherent antimicrobial activity at different concentration against stated bacterial strains and compared with standard chloramphenicol. 5-Oxo-imidazolines (3a and 3c) with 125 μg/mL concentration showed excellent antibacterial profile against Gram-positive bacteria, B. thuringiensis, while other derivatives at different concentrations showed moderate antibacterial activity against Gram-positive bacteria, S. aureus and B. thuringiensis. Gram-negative bacteria like E. coli and E. aerogenes are tested at higher concentration (1000, 500, and 125 μg/mL) and found good-to-moderate antibacterial activity. Tested products found non-active against E. aerogenes for 125, 61, and 31 μg/mL concentration also inactive at conc. 31 μg/mL against E. coli.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128997549","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

Recent Developments of Target-Based Benzimidazole Derivatives as Potential Anticancer Agents

Heterocycles - Synthesis and Biological Activities Pub Date : 2020-01-02 DOI: 10.5772/intechopen.90758

N. S. Goud, Pardeep Kumar, R. Bharath

引用次数: 11

Amidoxime Derivatives with Local Anesthetic, Antitubercular, and Antidiabetic Activity 偕胺肟衍生物与局部麻醉，抗结核和抗糖尿病活性

Heterocycles - Synthesis and Biological Activities Pub Date : 2019-12-17 DOI: 10.5772/intechopen.90002

L. Kayukova, U. Jussipbekov, K. Praliyev

{"title":"Amidoxime Derivatives with Local Anesthetic, Antitubercular, and Antidiabetic Activity","authors":"L. Kayukova, U. Jussipbekov, K. Praliyev","doi":"10.5772/intechopen.90002","DOIUrl":"https://doi.org/10.5772/intechopen.90002","url":null,"abstract":"О ur task in the field of new derivatives of amidoximes was the elaboration for new medication with increased activity and lower toxicity than medications used in practice. Here are the results of the search for new painkillers and antitubercular and antidiabetic drugs in the class of amidoxime derivatives. Nitrous derivatives of α -chloro- α -isonitrosoacetone, O -aroyl- β -aminopropioamidoximes, and 3-[ β -(piper-idine-1-yl)]ethyl-5-aryl-1,2,4-oxadiazoles were tested for conduction, infiltration, and terminal anesthesia. Among them hit compounds were discovered. The search for new anti-TB drugs is executed in the world. Salts and bases of O -aroylation products of β -(thiomorpholin-1-yl) and β -(4-methylpiperazin-1-yl) propioamidoximes during in vitro antitubercular screening for DS, DR, and MDR strains of M. tuberculosis manifest themselves as highly active competitive compounds. In the series of the derivatives of β -aminopropioamidoximes, a search for new antidiabetic drugs was done. The compounds with pronounced antidiabetic properties were revealed. The obtained data of the most promising samples with a preliminary assessment of their average toxic dose in animals can be used in further in vivo testing of infiltration anesthesia conditions, of antidiabetic properties, and at the development of doses and new treatment regimens for TB.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114527790","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

Azoles as Potent Antimicrobial Agents 氮唑类强效抗菌剂

Heterocycles - Synthesis and Biological Activities Pub Date : 2019-08-07 DOI: 10.5772/INTECHOPEN.88547

Rohit Singh, S. Ganguly

引用次数: 2

Phenacyl Bromide: An Organic Intermediate for Synthesis of Five- and Six-Membered Bioactive Heterocycles 苯那基溴:合成五元和六元生物活性杂环的有机中间体

Heterocycles - Synthesis and Biological Activities Pub Date : 2019-07-29 DOI: 10.5772/INTECHOPEN.88243

D. Jangid, Dr. Surbhi Dhadda

引用次数: 1

Synthesis and Anticancer Evaluation of Benzenesulfonamide Derivatives 苯磺酰胺衍生物的合成及抗癌评价

Heterocycles - Synthesis and Biological Activities Pub Date : 2019-07-17 DOI: 10.5772/INTECHOPEN.88139

Dattatraya N. Pansare, Rohini N. Shelke

引用次数: 0

The Oxygen-Containing Fused Heterocyclic Compounds 含氧熔融杂环化合物

Heterocycles - Synthesis and Biological Activities Pub Date : 2019-07-12 DOI: 10.5772/INTECHOPEN.88026

H. Venkatachalam, N. V. Kumar

引用次数: 2

Synthesis and Biological Evaluation of Novel Phosphonyl Thiazolo Pyrazoles 新型膦基噻唑类吡唑的合成及生物学评价

Heterocycles - Synthesis and Biological Activities Pub Date : 2019-06-24 DOI: 10.5772/INTECHOPEN.86977

A. Srinivas

引用次数: 0