- Synthesis antimicrobial and anticancer activity of N′- arylmethylidene-piperazine-1-carbothiohydrazide
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Ten newly synthesized thiosemicarbazones of piperazine (3a-3j) were evaluated for their antibacterial and antifungal activity against non-pathogenic strains of Escherichia coli (NCIM 2068), Klebsiella pneumonia (NCIM 2957), Staphylococcus aureus (NCIM 2079), and Bacillus subtilis (NCIM 2921); pathogenic strains of Vibrio cholerae, protease, Candida albicans and Aspergillus niger. All the 10 compounds (3a-3j) were found to be better than Ciprofloxacin against B. subtilis and four molecules (3c, 3d, 3e, and 3h) against S. aureus. Compound 3j, a derivative of benzophenone, has been identified as a potent and promising candidate against C. albicans. The compounds were also evaluated for their anticancer activity against HBL-100 and HL60 cell lines. Compound 3a, a p-hydroxy benzaldehyde derivative, has been identified as a potent and promising candidate.
- Kulandaivelu, Umasankar,Shireesha, Boyapati,Mahesh, Chidara,Vidyasagar, Jannu Vincent,Rao, Tadikonda Rama,Jayaveera,Saiko, Philipp,Graser, Geraldine,Szekeres, Thomas,Jayaprakash, Venkatesan
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p. 2802 - 2808
(2013/07/26)
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- Synthesis, antimicrobial and anticancer activity of new thiosemicarbazone derivatives
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Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Vibrio cholerae, and Bacillus subtilis with IC50 value of about 1 aμM. Compound 4f showed potent antifungal activity against Candida albicans (IC50a=a1.29 aμM) and compound 4h showed potent anticancer activity (IC50a=a0.07 aμM). Hydroxamate derivatives 4a-4l were found to show better antimicrobial and anticancer activity in compariosn with their acid counterparts 3a-3l. Copyright
- Kulandaivelu, Umasankar,Padmini, Valisakka Gari,Suneetha, Kyatham,Shireesha, Boyapati,Vidyasagar, Jannu Vincent,Rao, Tadikonda Rama,Jayaveera,Basu, Arijit,Jayaprakash, Venkatesan
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experimental part
p. 84 - 90
(2011/09/21)
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- Synthesis and anticancer activity of thiosemicarbazones
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Twenty-six thiosemicarbazones (III-1-III-26) were synthesized via three steps starting from hydrazine hydrate and carbon disulfide. The testing of anticancer activity of these compounds in vitro against P-388, A-549, and SGC-7901 shows that compounds III-15 and III-16 possess a higher inhibitory ability for P-388 and SGC-7901. Further testing shows that the value of IC 50 of compound III-16 against SGC-7901 reaches to 0.032 μM.
- Hu, Wei-Xiao,Zhou, Wei,Xia, Chun-Nian,Wen, Xi
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p. 2213 - 2218
(2007/10/03)
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- A Pummerer-Type Novel Ring Fission of 2-Methylsulfinyl-5,6-dihydro-4H-1,3,4-thiadiazine Derivatives: A Homologation of Aldehydes and Ketones
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Aldehydes and ketones were converted into 2-methylsulfinyl-5,6-dihydro-4H-1,3,4-thiadiazines via the formation and base-induced ring-closure of N-alkylidene-N′-bis(alkylthio)methylenehydrazines followed by mCPBA oxidation. The subsequent Pummerer-type ring fission of the rings was performed by treating with trifluoroacetic anhydride or trifluoromethanesulfonic anhydride at -78°C to give α,β-unsaturated esters and ketones in modest yields. Thus, this reaction sequence was regarded as being a new method for the two-carbon homologation of aldehydes and ketones.
- Shimada, Kazuaki,Otaki, Akihiro,Yanakawa, Masaki,Mabuchi, Shosuke,Yamakado, Naoya,Shimoguchi, Takeshi,Inoue, Kazuya,Kagawa, Takashi,Shoji, Kazutoshi,Takikawa, Yuji
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p. 1043 - 1054
(2007/10/03)
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- A Homologation of Aldehydes and Ketones via the Formation and the Subsequent Pummerer-type Ring Fission of 2-Methylsulfinyl-5,6-dihydro-4H-1,3,4-thiadiazine Derivatives
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A two-carbon homologation of aldehydes and ketones was achieved by using a sequence involving the formation and the subsequent Pummerer-type ring fission of 5,6-dihydro-4H-1,3,4-thiadiazine rings possessing methylsulfinyl functionality at C-2.
- Shimada, Kazuaki,Otaki, Akihiro,Yanakawa, Masaki,Mabuchi, Shosuke,Yamakado, Naoya,et al.
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p. 925 - 926
(2007/10/03)
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- A Facile Synthesis of Unsymmetrical Heterocyclic Azines by Cyclodesulfurization: Reaction of Methyl Arylalkylidenehydrazinecarbodithioates with Diamines
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A new and facile synthesis of unsymmetrical heterocyclic azines is described.Methyl arylalkylidenehydrazinecarbodithioates, prepared by the condensation of ketones or aldehydes with methyl hydrazinecarbodithioate, were heated under reflux with various dia
- Lin, Ai Jeng,Klayman, Daniel L.
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