17821-34-0Relevant academic research and scientific papers
Synthesis of novel pyrido[2,1-b]benzothiazole and N-substituted 2-pyridylbenzothiazole derivatives showing remarkable fluorescence and biological activities
Azzam, Rasha A.,Elgemeie, Galal H.,Osman, Rokia R.
, (2019/10/22)
The synthesis of novel pyrido[2,1-b]benzothiazole and pyrido[2,1-b]benzoimidazole derivatives was achieved via the reaction of N-aryl-2-cyano-3,3-bis(methylthio)acrylamide with benzothiazoleylacetonitrile and benzoimidazoleylacetonitrile, respectively, while N-substituted 2-pyridylbenzothiazole derivatives were synthesized by reacting 2-(benzo[d]thiazol-2-yl)-3-(dimethylamino)acrylonitrile with either cyanoacetamide, aryl cyanoacetamides or 2-cyano-N’-(4-substituted benzylidene)acetohydrazide. Based on the steady state fluorescence measurements, the newly synthesized N-substituted 2-pyridylbenzothiazole derivatives exhibited remarkable fluorescence properties with considerably high quantum yields (0.25–0.29). In addition, the antimicrobial and antiviral activities were evaluated for all the newly synthesized derivatives. The antimicrobial examination revealed that triazolo-pyridone 21a had the highest potency among all tested compounds against Escherichia coli, Klebsiella pneumonia and Staphylococcus aureus while pyrido[2,1-b]benzoimidazole derivatives 9a and 9b had the highest potency over other compounds against Candida albicans fungus.
Structure-based design, synthesis and biological evaluation of a newer series of pyrazolo[1,5-a]pyrimidine analogues as potential anti-tubercular agents
Modi, Palmi,Patel, Shivani,Chhabria, Mahesh
, p. 240 - 251 (2019/03/26)
In-depth study of structure-based drug designing can provide vital leads for the development of novel, clinically active molecules. In this present study, twenty six novel pyrazolo[1,5-a]pyrimidine analogues (6a-6z) were designed using molecular docking studies. The designed molecules were synthesized in good yields. Structural elucidation of the synthesized molecules was carried out using IR, MS, 1H NMR and 13C NMR spectroscopy. All the synthesized compounds were evaluated for their in-vitro anti-tubercular activity against H37Rv strain by Alamar Blue assay method. Most of the synthesized compounds displayed potent anti-tubercular activities. Amongst all the tested compounds 6p, 6g, 6n and 6h exhibited promising anti-tubercular activity. Further, these potent compounds were gauged for MDR-TB, XDR-TB and cytotoxic study. None of these compounds exhibited potent cytotoxicity. Stability of protein ligand complex was further evaluated by molecular dynamics simulation for 10 ns. All these results indicate that the synthesized compounds could be potential leads for further development of new potent anti-tubercular agents.
Synthesis and insecticidal activities of novel neonicotinoid analogs bearing an amide moiety
Wu, Jian,Yang, Song,Song, Bao-An,Bhadury, Pinaki S.,Hu, De-Yu,Zeng, Song,Xie, Hua-Peng
, p. 901 - 906 (2011/10/02)
Figure represented. A series of novel neonicotinoid analogs containing an amide moiety were synthesized, characterized, and subsequently evaluated for their insecticidal activity. According to the preliminary bioassay, the compounds 6c, 6e, 6f, 6j, 6n, and 6r exhibited > 50% activity against Nilaparvata lugens at 100 mg/L. Amongst the active compounds, 6f and 6r revealed insecticidal activities similar to that displayed by standard buprofezin. J. Heterocyclic Chem., (2011)
A new general method for substituted 4-alkylthio-N-arylsulphonyl-amino-2-pyridones: Reaction of ketene-ss-acetals with arylsulphonylhydrazides
Elgemeie, Galal H.,Ali, Hosny A.,Elghandour, Ahmed H.,Abdel-Aziz, Hassan M.
, p. 171 - 179 (2007/10/03)
A novel and efficient method for the synthesis of substituted 4-alkylthio-N-arylsulphonylamino-2-pyridones via the reaction of ketene-SS-acetals with N-cyanoacetoarylsulfonyl-hydrazides has been investigated. 1-Arylsulfonylamino-pyrazolo[3,4-c]pyridine-2(1H)-ones have also been prepared from the reaction of 4-alkylthio-N-arylsulfonylamino-2-pyridones with hydrazines.
Synthesis of some novel α-cyanoketene S,S-acetals and their use in heterocyclic synthesis
Elgemeie, Galal H.,Elghandour, Ahmed H.,Elzanate, Ali M.,Ahmed, Sayed A.
, p. 3285 - 3289 (2007/10/03)
A variety of novel α-cyanoketene S,S-acetals, readily prepared by the reaction of cyanoacetanilides or cyanothioacetamide with carbon disulfide, followed by alkylation, react smoothly with nucleophiles to afford variously substituted methylthio derivatives of pyrrole, pyrazole, pyridine and pyrimidine. Copyright 1997 by the Royal Society of Chemistry.
