145622-52-2Relevant academic research and scientific papers
Novel 50-norcarbocyclic pyrimidine derivatives as antibacterial agents
Khandazhinskaya, Anastasia L.,Alexandrova, Liudmila A.,Matyugina, Elena S.,Solyev, Pavel N.,Leonova, Olga G.,Popenko, Vladimir I.,Kochetkov, Sergey N.,Efremenkova, Olga V.,Buckheit, Karen W.,Wilkinson, Maggie,Buckheit, Robert W.,Chernousova, Larisa N.,Smirnova, Tatiana G.,Andreevskaya, Sofya N.,Seley-Radtke, Katherine L.
, (2018)
A series of novel 50-norcarbocyclic derivatives of 5-alkoxymethyl or 5-alkyltriazolyl-methyl uracil were synthesized and the activity of the compounds evaluated against both Gram-positive and Gram-negative bacteria. The growth of Mycobacterium smegmatis was completely inhibited by the most active compounds at a MIC99 of 67 μg/mL (mc2155) and a MIC99 of 6.7–67 μg/mL (VKPM Ac 1339). Several compounds also showed the ability to inhibit the growth of attenuated strains of Mycobacterium tuberculosis ATCC 25177 (MIC99 28–61 μg/mL) and Mycobacterium bovis ATCC 35737 (MIC99 50–60 μg/mL), as well as two virulent strains of M. tuberculosis; a laboratory strain H37Rv (MIC99 20–50 μg/mL) and a clinical strain with multiple drug resistance MS-115 (MIC99 20–50 μg/mL). Transmission electron microscopy (TEM) evaluation of M. tuberculosis H37Rv bacterial cells treated with one of the compounds demonstrated destruction of the bacterial cell wall, suggesting that the mechanism of action for these compounds may be related to their interactions with bacteria cell walls.
The Potential of Carbocyclic Nucleosides for the Treatment of Aids: Synthesis of Some Diphosphorylphosphonates Possessing Potent Activity Against HIV-Coded Reverse Transcriptase
Coe, Diane M.,Roberts, Stanley M.,Storer, Richard
, p. 2695 - 2704 (2007/10/02)
The phosphonates 19, 20, 24, 27 and the diphosphorylphosphonates 10 and 11 have been prepared as mimics of nucleoside-phosphates and -triphosphates respectively.The compounds 10 and 11 were found to be potent inhibitors of human immunodeficiency virus rev
Preparation of Nucleotide Mimics with Potent Inhibitory Activity Against HIV Reverse Transcriptase
Coe, Diane M.,Orr, David C.,Roberts, Stanley M.,Storer, Richard
, p. 3378 - 3379 (2007/10/02)
The triphosphate 11 has been synthesised in eight steps from 6-oxabicyclohex-2-ene 6 and has been shown to inhibit the enzyme, human immunodeficiency virus reverse transcriptase (HIV-rt).
