Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid in the C2-methyl series

…, R Kimbell, BM O'Connor, AH Calvert…

Index: Marsham; Jackman; Barker; Boyle; Pegg; Wardleworth; Kimbell; O'Connor; Calvert; Hughes Journal of Medicinal Chemistry, 1995 , vol. 38, # 6 p. 994 - 1004

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Citation Number: 36

Abstract

[N-[(3, 4-dihydro-2-methyl-4-oxo-6-quinazolinyl~ methy11-N-prop-2-yny1amino1benzoy11- ~-g1utam-ic acid (IC1 198583, 1) is described in which the glutamic acid residue has been replaced by other a-amino acids. Most of these analogues were prepared by coupling of tert- butyl-4-(prop-2-yny1amino) benzoate (37) with 6-(bromomethyl)-3, 4-dihydro-2-methyl-4- oxoquinazoline (34) followed by deprotection of the tert-butyl ester to the acid and azide- ...

~99%

Novel oxazolidinone–quinolone hybrid antimicrobials

[Gordeev, Mikhail F.; Hackbarth, Corinne; Barbachyn, Michael R.; Banitt, Lee S.; Gage, James R.; Luehr, Gary W.; Gomez, Marcela; Trias, Joaquim; Morin, Sara E.; Zurenko, Gary E.; Parker, Christian N.; Evans, Jonathan M.; White, Richard J.; Patel, Dinesh V. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 23 p. 4213 - 4216]