NOVEL N 4 -ALKYLCYTIDINES AS PROMISING ANTIMICROBIAL AGENTS L.A. Alexandrova a , M.V. Jasko a , D.A. Makarov a , I.A. Oskolsky a , I.L. Karpenko a , O.V. Efremenkova b
,
B.F. Vasilieva b
, D.A. Avdanina c
, G.K. Nuraeva c
, A.A. Ermolyuk c
, A.A. Zhgun c
, S.N. Kochetkov a
a Engelhardt Institute of Molecular Biology RAS, 32 Vavilova St., 119991 Moscow, Russia. b Gause Institute of New Antibiotics, 11 Bol'shaya Pirogovskaya St., 119021 Moscow, Russia. c Research Center of Biotechnology RAS, 33 Leninsky Ave, 119071 Moscow, Russia. The emergence of drug-resistant strains of pathogenic microorganisms necessitates
the creation of new drugs.
In order to find new inhibitors
of pathogenic bacteria and fungi,
we synthesized
a set of
N
4
-
derivatives of (2’-deoxy)cytidine,
bearing extended N
4
-alkyl and
N
4
-
phenylalkyl
groups
1-3 1
as well as
3′-modified derivatives of N
4
-alkyl
-5-methyl-2′,3′-dideoxycytidines
4 2
. The derivatives
1-3 demonstrated activity
against
Mycobacterium smegmatis and some Gram-positive bacteria,
including
Staphylococcus aureus (MIC=
50 – 200
mM),
comparable with the activities of a
number of antibiotics
in medical use.
The most promising are low toxic nucleosides
