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      KCI등재 SCIE SCOPUS

      Synthesis, Anti-inflammatory, Analgesic, and Antibacterial Activities of Some Triazole, Triazolothiadiazole, and Triazolothiadiazine Derivatives

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      https://www.riss.kr/link?id=A104665130

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      다국어 초록 (Multilingual Abstract)

      This study is concerned with the synthesis of new 1,2,4-triazoles, 1,3,4-thiadiazoles, and 1,3,4-thiadiazines derivatives. Derivatives 3a-i were obtained by condensation of 4-amino-3-(4-pyridine)-5-mercapto-1,2,4-triazole 1 with the appropriate aldehy...

      This study is concerned with the synthesis of new 1,2,4-triazoles, 1,3,4-thiadiazoles, and 1,3,4-thiadiazines derivatives. Derivatives 3a-i were obtained by condensation of 4-amino-3-(4-pyridine)-5-mercapto-1,2,4-triazole 1 with the appropriate aldehyde. Compounds 4a-i were synthesized in a one pot reaction involving compounds 3a-i, formaldehyde, and morpholine. Condensation of compound 1 with the appropriate acids or 4-substituted phenacyl bromide gave compounds 6a-d and 8a-f respectively. The chemical structures of the newly synthesized derivatives were elucidated using different spectral and elemental methods of analysis. All compounds were evaluated for their anti-inflammatory activity and the most potent derivatives were tested for their analgesic activity using indomethacin as a reference drug. In addition, ulcerogenicity and LD_50 for the most active compounds were evaluated. Moreover, the antibacterial activities of the newly synthesized derivatives were investigated.

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      참고문헌 (Reference)

      1 O’Neil, M. J., "The Merck Index 13th ed" Merck Research laboratories 892-, 2001

      2 Holla, B. S., "Synthesis, characterization and antimicrobial activity of some substituted 1,2,3-triazoles" 40 : 1173-1178, 2005

      3 Khanmohammadi, H., "Synthesis, biological and computational study of new Schiff base hydrazones bearing 3-(4-pyridine)- 5-mercapto-1,2,4-triazole moiety" 71 : 1474-1480, 2008

      4 Malinka, W., "Synthesis, analgesic activity and computational study of new isothiazolopyridines of Mannich base type" 60 : 961-968, 2005

      5 Raafat, M. S., "Synthesis of polyfunctionally substituted benzo[5,6]chromeno[4,3,2-de][1,6]naphthyridines and 5Hbenzo[ 5,6]chromeno[3,4-c]pyridines" 14 : 59-67, 2006

      6 Hamdy, M. A. R., "Synthesis of p-hydroxypropionic acid derivatives as potential anti-inflammatory and analgesic and antimicrobial agents" 378 : 339-378, 2006

      7 Shivarama Holla, B., "Synthesis characterization and anticancer activity studies on some Mannich bases derived from 1,2,4-triazoles" 38 : 759-767, 2003

      8 Shivarama Holla, B., "Synthesis and studies on some new fluorine containing triazolothiadiazines as possible antibacterial, antifungal and anticancer agents" 41 : 657-663, 2006

      9 Berk, B., "Synthesis and pharmacological activities of some new 2-[1-(6-methoxy- 2-naphthyl)ethyl]-6-(substituted)benzylidene thiazolo[3, 2-b]-1,2,4-triazole-5(6H)-one derivatives" 56 : 613-616, 2001

      10 Karthikeyan, M. S., "Synthesis and biological activity of Schiff and Mannich bases bearing 2,4-dichloro-5-fluorophenyl moiety" 14 : 7482-7489, 2006

      1 O’Neil, M. J., "The Merck Index 13th ed" Merck Research laboratories 892-, 2001

      2 Holla, B. S., "Synthesis, characterization and antimicrobial activity of some substituted 1,2,3-triazoles" 40 : 1173-1178, 2005

      3 Khanmohammadi, H., "Synthesis, biological and computational study of new Schiff base hydrazones bearing 3-(4-pyridine)- 5-mercapto-1,2,4-triazole moiety" 71 : 1474-1480, 2008

      4 Malinka, W., "Synthesis, analgesic activity and computational study of new isothiazolopyridines of Mannich base type" 60 : 961-968, 2005

      5 Raafat, M. S., "Synthesis of polyfunctionally substituted benzo[5,6]chromeno[4,3,2-de][1,6]naphthyridines and 5Hbenzo[ 5,6]chromeno[3,4-c]pyridines" 14 : 59-67, 2006

      6 Hamdy, M. A. R., "Synthesis of p-hydroxypropionic acid derivatives as potential anti-inflammatory and analgesic and antimicrobial agents" 378 : 339-378, 2006

      7 Shivarama Holla, B., "Synthesis characterization and anticancer activity studies on some Mannich bases derived from 1,2,4-triazoles" 38 : 759-767, 2003

      8 Shivarama Holla, B., "Synthesis and studies on some new fluorine containing triazolothiadiazines as possible antibacterial, antifungal and anticancer agents" 41 : 657-663, 2006

      9 Berk, B., "Synthesis and pharmacological activities of some new 2-[1-(6-methoxy- 2-naphthyl)ethyl]-6-(substituted)benzylidene thiazolo[3, 2-b]-1,2,4-triazole-5(6H)-one derivatives" 56 : 613-616, 2001

      10 Karthikeyan, M. S., "Synthesis and biological activity of Schiff and Mannich bases bearing 2,4-dichloro-5-fluorophenyl moiety" 14 : 7482-7489, 2006

      11 Kritsanida, M., "Synthesis and antiviral activity evaluation of some new 6-substituted 3-(1-adamantyl)- 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles" 57 : 253-257, 2002

      12 Walczak, K., "Synthesis and anti-tuberculosis activity of N-aryl-C-nitroazoles" 39 : 849-853, 2004

      13 Amir, M., "Synthesis and anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities of some new 2-[(2,6-dichloroanilino) phenyl]acetic acid derivatives" 35 : 535-545, 2004

      14 Bahaa Gamal Mohamed, "Synthesis and Antimicrobial Activity of Some New 1-Alkyl-2-alkylthio-1,2,4-triazolobenzimidazole Derivatives" 대한약학회 29 (29): 26-33, 2006

      15 Stillings, M. R., "Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives" 29 : 2280-2284, 1986

      16 Raafat, M. S., "Recent trends in the chemistry of 4-amino-1,2,4-triazole-3-thiones" 18 : 2577-2613, 2006

      17 Tan, B., "National Advisory Committee For Laboratory Animal, in Guidelines on the care and use of animals for scientific purposes" 2004

      18 William, H., "Microbiological assay, An introduction to quantitative principles and evaluation" Academic press 17-68, 1977

      19 Ferlin, M. G., "Mannich bases of 3H-pyrrolo[3,2-f]quinoline having vasorelaxing activity" 37 : 427-434, 2002

      20 Joshi, S., "In vitro study of some medicinally important Mannich bases derived from antitubercular agent" 12 : 571-576, 2004

      21 Nargund, L. V., "Anti-inflammatory activity of substituted 1,3,4-oxadiazoles" 83 : 246-248, 1994

      22 Francisca, L., "Amidomethylation of amodiaquine: antimalarial N-Mannich base derivatives" 45 : 7663-7666, 2004

      23 Raafat, M. S., "5-Aminouracil as a Building Block in Heterocyclic Synthesis: Part I. One-pot Synthesis of Pyrimido[5,4-b]quinolin-2,4,9-triones under Microwave Irradiation without Catalyst" 63 : 1431-1437, 2008

      24 Kane, J. M., "2,4-Dihydro-3H-1,2,4-triazole-3-thiones as potential antidepressant agents" 31 : 1253-1258, 1988

      25 Boyle, E. A., "-Aroyl- 2,3-dihydrobenzo[b]furan-3-carboxylic acids and 7-benzoyl- 2,3-dihydrobenzo[b]thiophene-3-carboxylic acids as analgesic agents" 29 : 894-898, 1986

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      2020-01-01 평가 등재학술지 유지 (해외등재 학술지 평가) KCI등재
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      학술지 인용정보
      기준연도 WOS-KCI 통합IF(2년) KCIF(2년) KCIF(3년)
      2016 1.96 0.2 1.44
      KCIF(4년) KCIF(5년) 중심성지수(3년) 즉시성지수
      1.07 0.87 0.439 0.05
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