k) have been synthesized from the intermediate 4-(4-acetyl-phenylamino)-chromen-2-one (4). Cyclization reaction of chalcone (5a-strong class="a-plus-plus">k) with hydrazine hydrate, guanidine nitrate, and malononitrile gives the corresponding 4-[4-(1-acetyl-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)-phenylamino]-chromen-2-one (6a-strong class="a-plus-plus">k), 4-[4-(2-amino-6-phenyl-pyrimidin-4-yl)-phenylamino]-chromen-2-one (7a-strong class="a-plus-plus">k), and 2-amino-6-[4-(2-oxo-2H-chromen-4-ylamino)-phenyl]-4-phenyl-nicotinonitrile (8a-strong class="a-plus-plus">k) derivatives were synthesized. The newly synthesized compounds were evaluated for their antimycobacterial activity and antimicrobial activity against eight bacteria (S. aureus, B. cereus, E. coli, P. aeruginosa, K. pneumoniae, S. typhi, P. vulgaris, and S. flexneri) and four fungi (A. niger, C. albicans, A. fumigatus, and A. clavatus)." />
In vitro antimicrobial and antimycobacterial activity of some chalcones and their derivatives
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  • 作者：Divyesh Patel (1)
    Premlata Kumari (1)
    Navin B. Patel (2)
  • 关键词：Coumarin ; Chalcone and their derivatives ; Antimicrobial activity ; Antimycobacterial activity ; Structure activity relationship
  • 刊名：Medicinal Chemistry Research
  • 出版年：2013
  • 出版时间：February 2013
  • 年：2013
  • 卷：22
  • 期：2
  • 页码：726-744
  • 全文大小：402KB
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  • 作者单位：Divyesh Patel (1)
    Premlata Kumari (1)
    Navin B. Patel (2)

    1. Department of Applied Chemistry, S.V. National Institute of Technology, Surat, 395007, India
    2. Department of Chemistry, V.N. South Gujarat University, Surat, 395007, India
文摘
In this study, novel series of chalcone derivatives, namely, 4-[4-(3-phenyl-acryloyl)-phenylamino]-chromen-2-one (5a-strong class="a-plus-plus">k) have been synthesized from the intermediate 4-(4-acetyl-phenylamino)-chromen-2-one (4). Cyclization reaction of chalcone (5a-strong class="a-plus-plus">k) with hydrazine hydrate, guanidine nitrate, and malononitrile gives the corresponding 4-[4-(1-acetyl-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)-phenylamino]-chromen-2-one (6a-strong class="a-plus-plus">k), 4-[4-(2-amino-6-phenyl-pyrimidin-4-yl)-phenylamino]-chromen-2-one (7a-strong class="a-plus-plus">k), and 2-amino-6-[4-(2-oxo-2H-chromen-4-ylamino)-phenyl]-4-phenyl-nicotinonitrile (8a-strong class="a-plus-plus">k) derivatives were synthesized. The newly synthesized compounds were evaluated for their antimycobacterial activity and antimicrobial activity against eight bacteria (S. aureus, B. cereus, E. coli, P. aeruginosa, K. pneumoniae, S. typhi, P. vulgaris, and S. flexneri) and four fungi (A. niger, C. albicans, A. fumigatus, and A. clavatus).

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