It's honor to me to contact you Prof. Giovina Ruberti.
My name is Ahmed Mohsen Kamal, I'm a demonstrator at medicinal chemistry department-faculty of pharmacy-Assiut university-Egypt
I'm working on synthesis new norfloxacin derivatives with possible antibacterial, antimycobacterial and anticancer activity. My new compounds were exposed to in-silico studies through molecular modelling and showed promising activity on histone deacetylase enzyme more than norfloxacin and SAHA. I wonder if there's any possibility to cooperate with you prof and make screening for my new compounds to determine their anticancer activity and their inhibitory effect on histone deacetylase enzyme.
I have attached an excel spreadsheet with the results so far. We have all MICs against E. coli. There are several compounds with quite a good MIC, two with an MIC comparable to Nor, and one with an even better MIC. We have tested all compounds against P. aeruginosa. Less of them are active, but we have at least three with an MIC ≤ 1, which we will test again together with Nor and Cip.
We have done mode of action confirmation for gyrase in E. coli, where we selected the best compounds of each series, 19 in total. 18 of those show a phenotype consistent with gyrase inhibition. We have tested off-target activity on the inner membrane of E. coli and none of the 19 tested compounds showed any effects.
Next week, we plan to test outer membrane activity in E. coli with the best representative of each series. M. tuberculosis is still growing slowly. We will wait until the cultures are ready to complete the MIC assays (and we do not have 96-well plates at the moment because Covid testing has depleted the supply in Sweden, so we have to wait for that, too). Once Mtb is in log phase and we have the plates, we will test MICs against Mtb, test lower concentrations of the three best compounds against P. aeruginosa, and test S. aureus as well.
After that, we will test the best compounds against quinolone-resistant P. aeruginosa and S. aureus. Then we will test effects on peptidoglycan synthesis in Gram-positives with the compounds that are most active against S. aureus. So that is the plan. Unfortunately, I cannot tell you exactly when Mtb will be ready and when we will have plates again, but I made an estimate in the excel file. I will send you updated versions of the spreadsheet when results come in.
It's honor to me to contact you Prof.
Giovina
Ruberti
.
My name
is Ahmed
Mohsen
Kamal, I'm a demonstrator at medicinal chemistry department-faculty of
pharmacy-Assiut
university-Egypt
I'm working on synthesis new
norfloxacin
derivatives with possible antibacterial,
antimycobacterial
and anticancer
activity
. My new compounds
were exposed
to
in-silico
studies through molecular modelling and
showed
promising
activity
on histone
deacetylase
enzyme more than
norfloxacin
and
SAHA
. I wonder if there's any possibility to cooperate with you prof and
make
screening for my new compounds to determine their anticancer
activity
and their inhibitory effect on histone
deacetylase
enzyme.
I have attached an
excel
spreadsheet with the results
so
far. We have all
MICs
against E. coli. There are several compounds with quite a
good
MIC, two with an MIC comparable to Nor, and one with an even better MIC. We have
tested
all compounds against P.
aeruginosa
. Less of them are active,
but
we have at least three with an MIC ≤ 1, which we will
test
again together with Nor and
Cip
.
We have done mode of action confirmation for
gyrase
in E. coli, where we selected the
best
compounds of each series, 19 in total. 18 of those
show
a phenotype consistent with
gyrase
inhibition. We have
tested
off-target
activity
on the inner membrane of E. coli and none of the 19
tested
compounds
showed
any effects.
Next
week, we plan to
test
outer membrane
activity
in E. coli with the
best
representative of each series. M. tuberculosis is
still
growing
slowly
. We will wait until the cultures are ready to complete the MIC assays (and we do not have 96-well plates at the moment
because
Covid
testing has depleted the supply in Sweden,
so
we
have to
wait for that, too). Once
Mtb
is in log
phase and
we have the plates, we will
test
MICs
against
Mtb
,
test
lower concentrations of the three
best
compounds against P.
aeruginosa
, and
test
S. aureus
as well
.
After that, we will
test
the
best
compounds against
quinolone-resistant
P.
aeruginosa
and S. aureus. Then we will
test
effects on peptidoglycan synthesis in Gram-positives with the compounds that are most active against S. aureus.
So
that is
the plan. Unfortunately, I cannot
tell
you exactly when
Mtb
will be ready and when we will have plates again,
but
I made an estimate in the
excel
file. I will
send
you updated versions of the spreadsheet when results
come
in.