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Wonder DrugsSuly V. Gonzalez and Eric J. Marsh
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Background
Ancient cultures and societies used “wonder drugs
!uinine
"ro# $inchona trees in South A#erica
%reats "e&ers and is an anti#alarial
'o(glo&e
$ontains digitalis )su*stance that sti#ulates heart #uscles+
,sed "or heart ail#ents in Western Euro-e
s still -rescri*ed as heart sti#ulant
Seed ca-sules o" a -o--y -lant
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Historically not many things were successfully usedbacterial infections.
● Small cuts and wounds would be life
threatening if infected
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As-irin and Dyes
Bayer and $o#-any
/riginally a dye co#-any
nterested in che#ical -roduction o" #edication 0 es-ecially as-irin
'eli( 1o"#ann 0 $he#ist
n&estigated -ro-erties o" co#-ounds o" salicylic acid
Bark o" trees o" the willow genus
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As-irin 0 Salicin
Breaks u- into two -arts
Glucose
Salicyl alcohol
" o(idized -roduces salicylic acid
● Salicylic Acid reduces "e&er2 relie&es -ains2 and acts as anti0in3a##atory
4 1ar#"ul to sto#ach lining4 5educed #edicinal &alue
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As-irin 0 Acetyl Salicylic Acid
1o6#an took 1 o" the -henol grou- and re-laced it with acetyl grou
1o-ed this would re#o&e har#"ul e6ect *ut kee- anti0in3a##atory -ro-erty
8henol grou- is what #akes it corrosi&e
Note: this was already done by another German chemist 40 years before
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As-irin 0 n the End
1o"#ann9s e(-eri#ents -aid o6 0 "or *oth his -o-s )had rheu#atoid
the Bayer co#-any
:;
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%he Saga o" Sul"a 0 %he 1istory
Dr. 8aul Ehrilch 0 no training in e(-eri#ental che#istry or a--lied t
=oted coal tar dyes would stain so#e tissue and so#e #icroorganis#others.
$a#e u- reasoning o" how to kill tissue with this
“Magic *ullet a--roach
Magic *ullet > dye that targeting the tissue it stained
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'irst Success
%ry-an red dye
,sed against try-anoso#es 0 -rotozoic -arasite0 in la* #ice
Although worked in the #ice it did not work "or the hu#an disease )slee-ing sickness+.
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Sy-hilis
Ehrlich looked "or “#agic *ullet "or sy-hilis
At the ti#e sy-hilis treated with #ercury 0 not &ery good "or the -atients
'ound “=u#*er ?@? 0 arsenic containing aro#atic co#-ound
$o#-ared to #ercury treat#ent it was good
1ad so#e to(ic side e6ects
Didn9t always cure -atients with sy-hilis
Ehrlich ca#e u- with “che#othera-y
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E(-eri#enting on Daughters
Dr. Gerhard Dog#ak decided to use a dye called prontosil redi to tr
daughter
1ad already *een e(-eri#enting with it *ut hadn9t "ound any acti&it*acteria
Ga&e to his daughter orally2 her reco&ery was "ast
5eco&ery wasn9t *ecause o" dye *ut how it *roke down in hu#an *ody
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Structure of Different Sulfa Drugs
Sulfanilamide is a result of the breaking down of prontosil red in
bodyProntosil red
Sulfanilamide
Minor Changes in Sulfa Drugstructures are capable ofchanging what the are able todeal with
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Sulfapyridine-Pneumonia
Sulfacetamide-Urinary tractinfection
SulfatGastrinfect
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ow the Sulfas kill bacteria
!acteria need "olic #cid
Similarity between Sulfa
Drugs and Folic Acid p-
aminobenoic acid molecules
!acteria confuse the Sulfa molecule and "olic acid p-aminobenzoic acid and die frMalnutrition
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Penicillins-the earliest true antibiotics
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=ota*le Scientists
ouis 8asteur :;0
'irst to show one #icroorganis# could *e used to kill another when heco##on *acteria could -re&ent a strain o" anthra( in urine
Jose-h ister
$ured a*scesses in -atients with 8enicilliu# #old e(tract
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Ale(ander 'le#ing
:
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Early %rials
nected in #ice without to(ic e6ects0a--lied directly to in"ected tissue
Ani#al $ell Me#*ranes Vs. $ell Walls
1u#an trials
Short li&ed success in adults
More relia*le success in children
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$he structure of penicillin was disco%ered in &'() and synthesize
first time in &'*+
!eta-,actam ing
ing Strain and .nstability
Structure
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1ow 8enicillin works
Beta0acta# 5ings o-en in the -resence o" the enzy#e that creates *a
An /1 grou- on the *acterial enzy#e is acylated
0Acyl Grou-
0Deacti&ation
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Strains o"
8enicillins
Di6erent strains o" 8enicillins are #ostly identical e(ce-t "or areas tha
"ro# strain to strain
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!en" G Amo#"
Ampi"
!eni $" %lo#"