The study of the antimicrobial activity of 6-sulfonyl derivatives of 4-methyl-1,2- dihydroquinoline-2-one
Ключові слова:
1, 2-dihydroquinoline-2-one, sulfones, amides, antimicrobial activity, "structure - activity" relationship.Анотація
Experimental study of the antimicrobial activity of the nineteen new 6-R-sulfonyl derivatives of 4-methyl-1,2- dihydroquinolin-2-one has been carried out using the
wells method and the serial dilution method in liquid medium. The experiment has shown that 6-alkylsulfonyl- 4-methyl-1,2-dihydroquinoline-2-ones have weak activity but 4-methyl-2-oxo-1,2-dihydroquinolin-6-sulfonic acid amides exhibit pronounced antibacterial activity, especially against strains of S. aureus and E. coli. The important structural feature of 4-methyl-2-oxo-1,2- dihydroquinolin-6-sulfonic acid anilides that increases this activity is the presence of the substituent in the orthoposition of the benzene ring of the amide residue.
Посилання
Mandell G.L., Sande M.A. Antimicrobial agents: drugs used in the chemotherapy of tuberculosis and leprosy. In:
Goodman Gilman A., Rall T.W., Nies A. S., Taylor P., etc. Goolman and Gilman`s The Pharmacological Basis of
Therapeutics. - New-York: Pergamon Press; 1990. – 1146 pp. Chapter 49.
Synthesis and antibacterial activity of certain quinoline derivatives / M. A. Abd-Alla, A.-H. N. Ahmed, M. F. El-
Zollry, F. A. Omar // Collect. Czech. Chem. Commun. – 1992. – Vol. 57, № 7. – P. 1547–1552.
US Pat. 2005119257, C 07 D 279/12. Cyclic sulfone containing retroviral protease inhibitors / Bertenshaw D. E.,
Getman D., Heintz R. M., Talley J. J., Reed K. L., Chrusciel R. A., Clare M. ; Pharmacia Corporation. – №
; 02.09.04 ; 02.06.05.
Synthesis and promising in vitro antiproliferative activity of sulfones of a 5-nitrothiazole series / Cohen A., Crozet M.
D., Rathelot P. et al. // Molecules. – 2012. – Vol. 21, №18(1). – P. 97-113.
Synthesis, in vitro and in vivo antimalarial assessment of sulfide, sulfone and vinyl amide-substituted 1,2,4-trioxanes
prepared via thiol-olefin co-oxygenation (TOCO) of allylic alcohols / Amewu R., Gibbons P., Mukhtar A. et al. // Org.
Biomolec. Chem. - 2010. - №8 (9). - Р. 2068-2077.
Discovery of small-molecule inhibitors of the ATPase activity of human papillomavirus E1 helicase / A.-M. Faucher,
P. W. White, C. Brochu et al. // J. Med. Chem. – 2004. – Vol. 47, № 1. – P. 18–21.
Synthesis and SAR of α-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors / Yue-Mei Zhang,
Xiaodong Fana, Bangping Xianga et al. // Bioorg. Med. Chem. Letters. – 2006. – Vol. 16, № 12. – P. 3096–3100.
Synthesis of (4-methyl-2-oxo-1,2-dihydroquinoline-6-sulfonyl)acetanilides and their effect on blood coagulation
system / V. A. Zubkov, T. A. Tsapko, I. S. Gritsenko and L. N. Maloshtan // Rus. Chem. Bull. – 2011. –V. 59, №2.
– P. 2329-2332.
Zubkov V.O. Synthesis and some peculiar properties of reactivity of 6-alkylsulfonyl-4-methyl-1,2-dihydroquinolin-2-
ones / V.O. Zubkov, I.S. Grytsenko, T.O. Tsapko // J. Org. Pharm. Chem. – 2009. – Vol. 7, № 3(27). – Р. 30-34.
##submission.downloads##
Як цитувати
Номер
Розділ
Ліцензія
Авторське право (c) 2020 Annals of Mechnikov's Institute
Ця робота ліцензованаІз Зазначенням Авторства – Некомерційна – Без Похідних 3.0 Міжнародна.
