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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#"