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https://hdl.handle.net/10316/26909
Title: | Novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one derivatives as potential inhibitors of chorismate mutase | Authors: | Rao, V. Mallikarjuna Kumar, P. Mahesh Rambabu, D. Kapavarapu, Ravikumar Rani, S. Shobha Misra, Parimal Pal, Manojit |
Keywords: | Pyrimidinone; Alkyne; Iodine; Palladium; Chorismate mutase | Issue Date: | Dec-2013 | Publisher: | Elsevier | Citation: | RAO, V. Mallikarjuna [et al.] - Novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one derivatives as potential inhibitors of chorismate mutase. "Bioorganic Chemistry". ISSN 0045-2068. Vol. 51 (2013) p. 48-53 | Serial title, monograph or event: | Bioorganic Chemistry | Volume: | 51 | Abstract: | A series of novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives were designed, synthesized and evaluated in vitro as potential inhibitors of chorismate mutase (CM). All these compounds were prepared via a multi-component reaction (MCR) involving sequential I2-mediated Biginelli reaction followed by Cu-free Sonogashira coupling. Some of them showed promising inhibitory activities when tested at 30 μM. One compound showed dose dependent inhibition of CM with IC50 value of 14.76 ± 0.54 μM indicating o-alkynylphenyl substituted DHPM as a new scaffold for the discovery of promising inhibitors of CM. | URI: | https://hdl.handle.net/10316/26909 | ISSN: | 0045-2068 | DOI: | 10.1016/j.bioorg.2013.08.002 | Rights: | openAccess |
Appears in Collections: | I&D CNC - Artigos em Revistas Internacionais |
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