Medicinal Chemistry Assignment-Answers

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Qn:

giv
etheI
UPACRULESFORNAMI
NGGAUNI
NEANDURACI
L?

Sur
e,Icanhel
pyouwi
tht
hat
!

Accor
dingt
oIUPACr
ules,
thenamesf
orguani
neandur
aci
lar
easf
oll
ows:

1.Guani
ne:
TheI
UPACnamef
orguani
nei
s2-
ami
no-
1H-
pur
in-
6(9H)
-one.

Expl
anat
ion:

-The"2-
amino"prefi
xindi
cat
est
hatt
her
eisanami
nogr
oupont
hesecondcar
bonat
om oft
he
puri
neri
ngstruct
ure.

-"
1H"meanst
hatt
her
eisahy
drogenat
om at
tachedt
othef
ir
stcar
bonat
om oft
hepur
iner
ing.

-"
puri
n"indi
cat
est
hetypeofhet
erocy
cli
cri
ngpr
esenti
nthest
ruct
ure,
whi
chcont
ainsaf
used
pyr
imi
dineandimi
dazol
eri
ng.

-"6(
9H)"speci
fiest
hatthecar
bonylgr
oupisattachedtothesi
xthcar
bonat
om oft
hepur
iner
ing
andthattheri
ngcontai
nsanitr
ogenatom atposit
ion9.

-Fi
nal
l
y,"
one"i
susedt
oindi
cat
ethatt
her
eisacar
bony
lgr
ouppr
esenti
nthest
ruct
ure.

2.Ur
aci
l
:TheI
UPACnamef
orur
aci
li
s2,
4-di
oxopy
rimi
dine.

Expl
anat
ion:

-The"
2,4-
dioxo"pr
efi
xindi
cat
esthatt
her
ear
etwocar
bony
lgr
oupspr
esenti
nthepy
rimi
dine
ri
ngst
ruct
ureatposit
ions2and4.

-"
pyri
midi
ne"i
ndi
cat
esthetypeofhet
erocy
cli
cri
ngpr
esenti
nthest
ruct
ure,
whi
chcont
ainst
wo
ni
tr
ogenatomsandfourcar
bonatoms.

Ihopet
hathel
ps!Letmeknowi
fyouhav
eanyf
urt
herquest
ions.
Thi
smessagehasbeengener
atedbyNov
a-downl
oadi
tforf
ree:

ht
tps:
//nov
aappai
.page.
li
nk/
y8wXkhqqzkPZMki
S7

Qn2:
giv
ethedi
ff
erencebet
weenal
l
ost
eri
candor
thost
eri
csi
te?

Sur
e,Icanhel
pyouwi
tht
hat
!

Themai
ndi
ff
erencesbet
weenal
l
ost
eri
candor
thost
eri
csi
tesar
easf
oll
ows:

1.Locat
ionoft
hebi
ndi
ngsi
te:

-Or
thost
eri
csi
tesar
el ocat
edattheacti
vesiteoft
het
argetenzy
meorr
ecept
orpr
otei
n,
wher
ethel
igandbi
ndstoi
nit
iateabiol
ogical
response.

-All
oster
icsi
tesarel
ocatedatadi
ff
erentr
egi
onont
hepr
otei
n,of
tendi
stantf
rom t
he
or
thost
eri
cal
lyboundli
gand-
bindi
ngsit
e.

2.Bi
ndi
ngaf
fi
nit
yandki
net
ics:

-Ligandsbindi
ngtotheort
host
ericsi
tet
ypi
cal
l
yhav
ehi
ghaf
fi
nit
y,hi
ghpot
encyanda
f
astassociat
ionanddissoci
ati
onki
net
ics.

-Ligandsbindi
ngt
otheall
ost
eri
csit
etypi
cal
l
yhav
eloweraf
fi
nit
y,l
owerpot
ency
,anda
sl
owerassociat
ionanddi
ssoci
ati
onki
neti
cs.

3.Mechani
sm ofact
ion:

-Li
gandsbindingtotheorthost
eri
csi
tety
pical
lyr
egul
atethet
argetprot
einbydi
rect
ly
bl
ocki
ngoracti
vati
ngt her
eceptororenzymeact
ivi
ty,
oft
enbyinduci
ngconformati
onal
changes
i
ntheprot
einst
ructur
e.

-Ligandsbindi
ngtotheal
lost
ericsit
ecommonl yinducechangesi
ntheconf
ormat
ionof
thepr
otein,therebymodul
ati
ngthebindingoracti
vi
tyofotherli
gandsatt
heort
host
eri
csi
te,
oft
enwi t
hmor esubtl
ebutpot
enti
all
yphy si
ologi
cal
lyr
elevantef
fects.
4.Ty
peofl
i
gands:

-Ort
host
eri
csitesoft
enbindsmal
l,
lowmolecul
arweightl
i
gandsthathavetr
adi
ti
onal
phar
macophor
efeatur
es,suchashydr
ophobi
candpolargr
oupsandioni
cinter
acti
ons.

-Al
loster
icsi
testypi
cal
lybindlargerormor ecomplexl
igands,suchasendogenous
modul
ator
s,metaboli
tes,
orall
ostericagentsthathavedi
ff
erentpharmacophorefeat
urest
han
t
heort
hoster
ical
lyboundsmallmol ecul
es.

Ihopet
hathel
psclar
if
ythediff
erencesbet
weenal
l
ost
eri
candor
thost
eri
csi
tes!Letmeknowi
f
youhav
eanyfurt
herquest
ions.

Thi
smessagehasbeengener
atedbyNov
a-downl
oadi
tforf
ree:

ht
tps:
//nov
aappai
.page.
li
nk/
y8wXkhqqzkPZMki
S7

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