Synthesis and in vitro microbiological evaluation of an array of biolabile 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides

被引：48
作者：
Kanagarajan, V. [1 ]
Thanusu, J. [1 ]
Gopalakrishnan, M. [1 ]
机构：
[1] Annamalai Univ, Dept Chem, Synthet Organ Chem Lab, Annamalainagar 608002, Tamil Nadu, India
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 04期
关键词：
2-Amino-4,6-diarylpyrimidines; Morpholine; Acetamide; Chloroacetyl chloride; Antibacterial activity; Antifungal activity; ONE-POT SYNTHESIS; BIOLOGICAL EVALUATION; DESIGN; DERIVATIVES; INHIBITORS;
D O I：
10.1016/j.ejmech.2009.12.068
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Biolabile 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides 34-42 have been synthesized and evaluated for their in vitro antibacterial and antifungal activities. The minimum inhibitory concentration tested for the same compounds against the same set of bacterial and fungal strains shows that the compounds 36 and 38 against beta-Heamolytic streptococcus and Klebsiella pneumonia, 40 against Escherichia coli and Pseudomonas, have excellent antibacterial activity. Compounds 36, 38 and 42 show inhibition against Aspergillus flavus, compound 41 against Microsporum gypsuem, 42 against Mucor, and compounds 39 and 40 against Rhizopus. (c) 2010 Elsevier Masson SAS. All rights reserved.
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页码：1583 / 1589
页数：7
相关论文
共 29 条
  • [1] AGARWAL R, 1984, J CHEM SOC PAKISTAN, V6, P308
  • [2] Avramova P, 1998, ARCH PHARM, V331, P342, DOI 10.1002/(SICI)1521-4184(199811)331:11<342::AID-ARDP342>3.0.CO
  • [3] 2-6
  • [4] Synthesis and biological evaluation of some 5-ethoxycarbonyl-6-isopropylamino-4-(substitutedphenyl)aminopyrimidines as potent analgesic and anti-inflammatory agents
    Chhabria, Mahesh T.
    Bhatt, Hardik G.
    Raval, Hitesh G.
    Oza, Pratik M.
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (04) : 1022 - 1024
  • [5] DHAR ML, 1968, INDIAN J EXP BIOL, V6, P232
  • [6] Dorn CP, 1997, US Patent, Patent No. [5691336:82, 569133682]
  • [7] Fisher MH, 1991, US Patent, Patent No. [5077290:10, 507729010]
  • [8] Substituted benzyl-pyrimidines targeting thymidine monophosphate kinase of Mycobacterium tuberculosis:: Synthesis and in vitro anti-mycobacterial activity
    Gasse, Cecile
    Douguet, Dominique
    Huteau, Valerie
    Marchal, Gilles
    Munier-Lehmann, Helene
    Pochet, Sylvie
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (11) : 6075 - 6085
  • [9] Gopalakrishnan M, 2008, J ENZYM INHIB MED CH, V23, P347, DOI [10.1080/14756360701611498, 10.1080/14756360701611498 ]
  • [10] Synthesis and biological evaluation of 5,7-diaryl-4,4-dimethyl-4,5,6,7-tetrahydropyridino[3,4-d]-1,2,3-thiadiazoles
    Gopalakrishnan, M.
    Thanusu, J.
    Kanagarajan, V.
    [J]. MEDICINAL CHEMISTRY RESEARCH, 2007, 16 (7-9) : 392 - 401
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