• 제목/요약/키워드: Thiosemicarbazones

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Thiosemicarbazones의 몇 가지 코팔트(II) 및 니켈(II) 착물에 대한 합성, 항박테리아 및 항균 활성 (Synthesis, Antibacterial and Antifungal Activities of Some Cobalt(II) and Nickel(II) Complexes of Thiosemicarbazones)

  • Prasad, Surendra;Agarwal, Ram K.
    • 대한화학회지
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    • 제55권2호
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    • pp.189-198
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    • 2011
  • 두 가지 새로운 thiosemicarbazone으로, 예를 들면, 4[N-(4'-ethylbenzalidene)amino]antipyrine thiosemicarbazone(EBAAPTS) 및 4[N-(2',4'-dimethylbenzalidene)amino]antipyrine thiosemicarbazone(DMBAAPTS)를 합성하여 그 특성을 규명하였다. 이들 thiosemicarbazone(EBAAPTS 및 DMBAAPTS)의 코발트(II) 및 니켈(II)에 대한 착물화 특성을 조사하였다. EBAAPTS 및 DMBAAPTS와 코발트(II) 및 니켈(II) 염과의 반응을 뜨거운 에탄올 용액에서 수행한 결과, 일반적 조성으로 [$MX_2(L)H_2O$] (M=$Co^{2+}$ 또는 $Ni^{2+}$; X=$Cl^-$, $Br^-$, $NO_3^-$, $NCS^-$ 또는 $CH_3COO^-$; L=EBAAPTS 또는 DMBAAPTS)을 갖는 새로운 착물의 형성을 확인하였다. 새롭게 합성한 이들 착물에 대해 원소분석, 분자량, 몰전도도, 자기수자율, 적외선 및 자외선 분광학 등의 방법으로 특성을 규명하였다. 니트로벤젠 용액에서 이들 착물의 몰전도도를 측정한 결과, 비전해질 성질을 가짐을 알았다. 또한, 모든 착물은 높은-스핀 형태였다. 분광학적 연구로부터 [$MX_2(L)H_2O$] 형의 코발트(II) 및 니켈(II) 착물은 팔면체의 기하구조를 갖는 것으로 확인되었다. 이들 착물을 이용하여 항박테리아 및 항균 활성을 여러 종류의 병원균, 세균 및 박테리아에 대해 조사하여 생물학적 활성을 고찰하였다.

Synthesis of New 2-Thiouracil-5-Sulfonamide Derivatives with Biological Activity

  • Fathalla, O.A.;Zaghary, W.A.;Radwan, H.H.;Awad, S.M.;Mohamed, M.S.
    • Archives of Pharmacal Research
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    • 제25권3호
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    • pp.258-269
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    • 2002
  • 2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

Synthesis of Some Novel Thiazolyl - Azetidinone Hybrids

  • Ahn, Chuljin;Hegde, Hemant;Shetty, Nitinkumar S.
    • 대한화학회지
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    • 제60권2호
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    • pp.107-110
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    • 2016
  • A new series of hydrazino thiazolyl-2-azetidinone 4(a-i) derivatives were synthesized efficiently using benzylidene hydrazinyl thiazole derivatives 3(a-i). The precursors, benzylidene hydrazinyl thiazoles were prepared by reacting 4-fluoro phenacyl bromide with thiosemicarbazones 2(a-i). All the structures of the synthesized compounds were ascertained by IR, NMR and mass spectral analysis.

실험 항암제 2-Formylpyridine Thiosemicarbazone유도체의 철 및 동착물의 합성 (Synthesis of Iron and Copper Complexes of 2-Formylpyridine Thiosemicarbazone Derivatives, Potential Antitumor Agents)

  • 김종윤;최보길;우순형
    • 약학회지
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    • 제26권3호
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    • pp.181-184
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    • 1982
  • The iron and copper chelates of 4-dimethylamino-2-formylpyridine thiosemicarbazone, one of the amine substituted derivatives at 4-C of 2-formylpyridine thiosemicarbazones which are known as the more improved potential antitumor agents, have been synthesized to make them more effective than the ligand (denoted as HL) itself. Their ligand-to-metal ratios were 2:1 and 1:1 for the iron and copper chelates, and the data along with those of elemental analysis and IR spectroscopy showed that. the compositions are [$FeI_{2}{\times}2H_{2}SO_{4}$ and [CuL($H_{2}Cl$O)], respectively.

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Synthesis and Antimicrobial Activity of New Substituted Anili-nobenzimidazoles

  • Nofal, Z.M.;Fahmy, H.H.;Mohamed, H.S.
    • Archives of Pharmacal Research
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    • 제25권3호
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    • pp.250-257
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    • 2002
  • A series of benzimidazole derivatives carrying different heterocycles such as 1,2,3-thiadiazole, 1,3,4-thiadiazole, thiazolidine, 2,3-dihydro-thiazole, 1,3,4-oxadiazole, semicarbazone and substituted thiosemi-carbazones were synthesized. Also a series of 1-methylbenzimidazole carrying hydroxy ethyl-amide, substituted sulfonyl hydrazide and benzoyl hydrazide from aminobenzoyl group at position 2 of 1-methylbenzimidazole were synthesized. The antimicrobial evaluation of some of the new compounds was carried out.

Design and Synthesis of Pyrazolyl Thiosemicarbazones as New Anticonvulsants

  • Deng, Xian Qing;Song, Ming Xia
    • Bulletin of the Korean Chemical Society
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    • 제35권9호
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    • pp.2733-2737
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    • 2014
  • A series of pyrazolyl thiosemicarbazone derivatives were synthesized and evaluated for their anticonvulsant activity using the maximal electroshock (MES) method. Interestingly, all compounds prepared showed long duration of protection effect in the MES screens. Among them, compound 5b was considered as the most promising one with an $ED_{50}$ value of 47.3 mg/kg, and a PI value of 4.8, which was superior to phenobarbital and valproate in the aspect of safety. Furthermore, compound 5b showed protection against seizures induced by pentylenetetrazole suggesting that compound 5b may exert anticonvulsant activity through GABA-mediated mechanisms.

Synthesis and Antimicrobial Activity of Novel Tetrahydrobenzothienopyrimidines

  • Amal Abdel Haleem Mohamed Eissa;Ashraf Ahmed Moneer
    • Archives of Pharmacal Research
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    • 제27권9호
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    • pp.885-892
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    • 2004
  • Due to the rapidly growing number of resistant strains of bacteria, the search for antibacterial agents with new modes of action will always remain an important and challenging task. Thus, the reaction of 2-substituted or. unsubstituted-4-(4-acetylanilino)-5,6,7,8-terahydrobenzo[b] thieno[2,3-d]pyrimidine derivatives 1-3 with the hydrazine derivatives, semi and / or thiosemi-carbazides, provided the corresponding hydrazones 4-6 and semi and/or thiosemicarbazones 7-9. Claisen-Schmidt condensation of compounds 1 or 2 with the appropriate aldehyde yielded the chalcones 10, 11 which, when treated with hydroxylamine hydrochloride gave rise to the isoxazoline-containing compounds 12, 13. Furthermore, reacting the respective chalcones 10, 11 with different hydrazines, urea and/or thiourea, furnished compounds 14, 15, 16, and 17 respectively. Representative compounds were tested for their antimicrobial activity against Candida Albicans and certain gram-positive and gram-negative bacteria. Their MICs were then determined. Compound 15e, showed a broad spectrum of activity while most of the other com-pounds showed varying antimicrobial activity.

Cycloplatinated Complexes of Thiosemicarbazones. Synthesis and Crystal Structure of [$Ph_2PC_6H_4CHNNC(S)NHCH_3PtCl$]

  • 유동원;강상욱;고재정;최문근
    • Bulletin of the Korean Chemical Society
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    • 제18권3호
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    • pp.305-310
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    • 1997
  • The synthesis and characterization of the platinum heterocyclic carboxaldehyde thiosemicarbazone complexes [NC5H4CRNNC(S)NHR'PtCl] (R=H, R'=CH3(1); R=CH3, R'=CH3(2); R=CH3, R=H(3)) and diphenylphosphinophenyl carboxaldehyde thiosemicarbazone complexes [Ph2PC6H4CHNNC(S)NHRPtCl] (R=CH3(5); R=iC3H7(6); R=Ph(7)) are described. Compounds 1-3 were prepared by reaction of Pt(SEt2)2Cl2 with 2-acetylpyridine-4-alkylthiosemicarbazone in the presence of NEt3. Compounds 5-7 were prepared using Pt(SEt2)2Cl2 in toluene with diphenylphosphinophenyl carboxaldehyde alkylthiosemicarbazone. The compounds have been characterized by microanalysis, NMR (1H, 13C, 31P) spectroscopy, and single-crystal X-ray diffraction. X-ray single crystal diffraction analysis reveals that compound 5 is a mononuclear platinum compound with P,N,S-coordination mode.