• Title/Summary/Keyword: Mannich base

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Synthesis of Mannich Bases of Antineoplaston A10 and their Antitumor Activity

  • Choi, Bo-Gil;Seo, Hee-Kyoung;Chung, Byung-Ho;Choi, Sang-Un;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.17 no.6
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    • pp.467-469
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    • 1994
  • Some Mannich bases of Antineoplaston A10 which is antitumor agent under chlinical investigation were synthesized and tested fro cytotoxicity. The tested compounds (2a, 2b, 2d) showed good activity comparable to that of carboplatin.

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Intramolecular Oxa-Mannich Reaction of 1,3-Dihydro-2-benzofuran-1-ol for Efficient Synthesis of 1-Aminophthalan Derivatives

  • Kim, Heebum;Kim, Sung-Gon
    • Journal of the Korean Chemical Society
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    • v.66 no.1
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    • pp.9-14
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    • 2022
  • An efficient method for the synthesis of 1-aminophthalans has been developed. The intramolecular oxa-Mannich reaction of 1,3-dihydro-2-benzofuran-1-ols with p-toluenesulfonylamine in the presence of Cs2CO3 as a base, without using any catalyst, provided the desired 1-aminophthalans in moderate to good yields.

Synthesis, spectral, thermal, structural study and theoretical treatment of new complexes of mannich base with Ni(II) and study of cytotoxicity effect on (Hepa-2) cell line and antimicrobial activity

  • Omar H. Al-Obaidi
    • Analytical Science and Technology
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    • v.36 no.2
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    • pp.70-79
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    • 2023
  • The synthesis of the Mannich base as a ligand (L) N-(morpholino (phenyl) methyl) acetamide is the subject of this study. Elemental analyses, FT-IR spectra, UV-vis, 1H-NMR, and magnetic measurements were used to confirm the synthesis of the [Ni(L)2]Cl2 complex, thermal analysis (TG/DTG), atomic absorption, and scanning, and structurally explained as electron microscopy (SEM), and X-ray powder diffraction (XRD) methods. The melting point of the complex and its molar conductivity were also measured. The suggested geometries of the complexes formed have a tetrahedral structure, according to the data acquired using various techniques. Theoretical approaches to the complex formation have been investigated. For molecular mechanics and semi-empirical calculations, the HYPERCHEM6 program had been used. The effect of the novel Ni(II) complex on the cancer cell Hepa-2 (human hepatocellular ademocarcinoma), that is the human laryngeal cancer, was studied. It has been found that these ligand and complex have potent effects on the cancer cell. The antibacterial activity of the free ligand and its complex was evaluated against two kinds of human pathogenic bacteria. The first category is Gram-positive (Staphylococcus aureas, epiderimids), whereas the second group is Gram-negative (Psedamonas aeruginosa, Escherichia coli) (from the diffusion method). Finally, it was discovered that various chemicals had varied growth-inhibiting effects on bacteria.

Synthesis and Antitumor Activity of Antineoplaston A10 Analogs as Potential Antineoplastic Agents (항암제 안티네오플라스톤 A10의 동족체합성 및 항암 활성)

  • Choi, Bo-Gil;Seo, Hee-Kyoung;Kim, Ok-Young;Chung, Bung-Ho;Oh, In-Jun;Cho, Won-Jea;Cheon, Seung-Hoon;Park, Min-Soo;Choi, Sang-Un;Lee, Chong-Ock
    • YAKHAK HOEJI
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    • v.41 no.3
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    • pp.283-293
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    • 1997
  • Some analogs and their Mannich bases of Antineoplaston A10 (A10) were synthesized. Chemical yield for the 2-(or 3-)thienyl, benzol, and phenylpropionyl analogs were high but 1-naphthyl analog was synthesized in low yield. The Mannich bases formation of these analogs with morpholine went verywell compared to other bases. 1-Naphthyl, 4-nitrobenzoyl, and phenylpropionyl analogs of A10 showed weak in vitro activity but the other A10 analogs showed weaker or no activity at 10-1000mcg/ml. But their Mannich bases containing A10analogs showed good in vitro activity compared to simple A10 analogs.

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Synthesis of Mannich Base of Benzoxazolin-2-thione and Alkyl Ester of PAS and Their Antimicrobial Activities (Benzoxazolin-2-thione과 PAS의 Alkyl Ester과의 Mannich Base 합성 및 항균력에 관한 연구)

  • 정원근;정상헌;정필근;윤원영;이남복
    • YAKHAK HOEJI
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    • v.18 no.4
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    • pp.243-248
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    • 1974
  • Nine benzoxazolin-2-thione derivatives were sunthesized as the potential antimicrobial substances. These compounds were tested for the antimicrobial activities using Staphylococcus aureus and Escherichia coli by way of tube dilution method. The three compounds of I, II and VII omjoboted the growth of S.aureus at the concentration of 1${\mu}$g/ml, and III,VI,VIII and IX exhibited considerable antimicrobial activities against S. aureus at the concentration of 10.m.u.g/ml. As to the growth of E. Coli, VII VII and VIII inhibited at the concentration of 1${\mu}$g/,l. II,III and IV exhibited considerable antimicrobial activities against E. coli at the concentration of 10${\mu}$g/ml.

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Studies on Nitroaniline derivative of 2, 2'-methylene-bis-(3, 4, 6-trichloroacetoxy benzene by Mannich reaction Part I. Synthesis and Antimicrobial activity (2, 2'-methylene-bis-(3, 4, 6-trichloroacetoxy benzene)의 nitroaniline 계 mannich bases에 관한 연구 I. 합성 및 항균성)

  • Yu, Ju-Hyun;Kim, Yu-Sam;Kim, Jong-Ho;Yang, Ryung
    • Korean Journal of Food Science and Technology
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    • v.6 no.1
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    • pp.6-11
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    • 1974
  • Four new compounds; 2,2'-methylene-bis [3, 4, 6-trichloro ${{\beta}-(o-nitroanilino)$ propionoxy} benzene]; m.p. $200{\sim}202^{\circ}C,\;C_{31}H_{22}O_8N_4Cl_6$ 2,2'-methylene-bis [3, 4, 6-trichloro ${{\beta}-(p-nitroanilino)$ propionoxy} benzene]; m.p. $168-170^{\circ}C,\;C_{31}H_{22}O_8N_4Cl_6$ : 2,2'-Methylene-bis [3, 4, 6-trichloro ${{\beta}-(o-chloro-p-nitroanilino)$ propionoxy} benzene]; m.p. $170.5-172.5^{\circ}C,\;C_{31}H_{20}O_8N_4Cl_8$ : 2,2'-Methylene-bis [3, 4, 6-trichloro ${{\beta}-(c-methyl-p-nitroanilino)$ propionoxy} benzene]; m.p. $163-164^{\circ}C,\;C_{33}H_{26}O_8N_4Cl_6$-were synthesized by Mannich reaction from 2,2'-Methylene-bis (3, 4, 6-trichloroacetoxy benzene) and their antimicrobial activities against the microorganisms Staphylococcus aureus, Escherichia coli, Bacillus subtilis Natto, Brevibacterium ammoniagenes, Candida tropicalis, Rhodotorula glutinis, Pseudomonas ovalis, Aspergillus candidus Link, Aspergillus awamori Nakazawa. Aspergillus niger var. Tieghem, Aspergillus usami Sakakuchi, Penicillium notatum-were tested. 2,2'-methylene-bis [3, 4, 6-trichloro ${{\beta}-(o-nitroanilino)$ propionoxy} benzene] showed a strong antimicrobial activity against Bacilus subtilis Natto and Brevibacterium ammoniagenes.

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Synthesis of 2,5Bis(2'-piperidymethyl)piperidine and Related Compounds

  • Hammouda, Metwally;Kandeel, Ex-el-Din;Hamama, Wafaa;Afsah, Elsayed
    • Archives of Pharmacal Research
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    • v.16 no.1
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    • pp.68-70
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    • 1993
  • The triketones 3-6 were obtained by alkylation of cyclopentanone or cyclohexanone with the appropriate cycloalkanone bis-mannich base (1) or (2). Schmidt reaction of the tricketones 3-6 afforded the corresponding trcyclic lactames 7-10 respectively. reduction of 7 and 9 gave compounds 11 and 12 respectively.

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Synthesis of 2,6-Diaromatic Substituted Pyridine Derivatives and Their Antitumor Activities

  • Moon, Yoon-Soo;Lim, Hyun-Tae;Zhao, Long-Xuan;Basnet-Arjun;Lee, Eung-Seok
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.345.1-345.1
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    • 2002
  • ${\alpha}$-terthienyl the first isolated from natural products shows potent antitumor activity, which encouraged us to study terpyridine and its biological properties. Terpyridine has also been reported as having carcinogenicity, and it's erivatives showed high cytotoxic activities against several human cancer cell lines and topoisomerase I inhibitory ctivity. Mannich free base from condensation reaction was allowed to react with pyridinum salts to give activity. (omitted)

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