Medicinal Chemistry lectures contents:

Reference: - An Introduction to Medicinal Chemistry. By: Graham L. Patrick

Dru Desi n L!C"#R! $ 1- Finding a lead: 2- Isolation and purification 3- Structure determination 4- Herbal medicine

L!C"#R! % Optimizing target interaction: a. Structure acti it! relations"ip b. Identification of a p"armacop"ore c. #rug optimization d. $ase stud!

L!C"#R! & Optimizing access to t"e target: a. Impro ing absorption b. %a&ing drugs more resistant to c"emical and enz!matic degradation c. %a&ing drugs less resistant to drug metabolism d. 'argeting drugs e. (educing to)icit! f. *rodrugs

L!C"#R! ' +uantitati e Structure acti it! relations"ip: a. ,rap"s and e-uations b. *"!sicoc"emical properties

c. Hansc" e-uation d. $raig plot e. 'opliss sc"eme f. .ioisosteres g. Free / 0ilson approac" ". *lanning a +S1( stud! i. $ase stud!.

Anti(iotics L!C"#R! ) Penicillins and ce*halos*orins 1- ,eneral definition 2- 2ses 3- Side effects 4- %ode of action 3- $lassification 4- 5-6actam antibiotics a. $lassification b. Structure and nomenclature of penicillin7s c. %O18 classification and sources d. ,eneral preparation of semi s!nt"etic penicillin e. S1( f. *enicillin , and its problems and ampicillin:

g. 1cid resistance 9*enicillin

". 5-6actamase resistance 9o)acillin8 clo)acillin and fluclo)acillin: i. ;. .road spectrum9ampicillin8 amo)icillin and carbenicillin: $lass II 9'icarcillin:

L!C"#R! + 1- *rodrugs 9pi ampicillin: 2- 5-6actamase in"ibitors 9sulbactam8 cla ulanic acid and imipenem : and %O1 3- 6atent penicillin 9penicillin , procaine: 4- $ep"alosporin structure and nomenclature 3- $ep"alosporin $ and its S1( 4- $lassification of cep"alosporin <- 1st ,eneration 9cep"ale)in and cep"adro)il: =- 2nd ,eneration 9cefaclor:

>- 3rd ,eneration 9cefota)ime and cefi)ime: 1?- 4t" ,eneration 9cefepime: 11- $ep"am!cin 9cefo)itin:

L!C"#R! , !rythromycin- macrolide and amino lycoside 1- @r!t"rom!cin S1( and c"emical stabilit! 2- 1zit"rom!cin and its S1(8 %O18 action and uses 3- 'etrac!cline8 its %O18 metabolism and side effects 4- $"emistr! of tetrac!cline7s and S1( 3Sanac!cline8 o)!tetrac!cline and rolitetrac!cline

4- $"loramp"enicol8 mec"anism8 S1(8 prodrug and side effects <- 1minogl!coside8 %O18 properties8 application and side effects. =- #rug interaction Ait" 5 -lactam L!C"#R! . /uinolone - fluoro0uinolone and nitrofuran 1- Balidi)ic acid8 metabolism uses and side effects 2- 1st generation8 roso)acin 3- 2nd generation8 its ad antage8 norflo)acin and its s!nt"esis 4- Oflo)acin8 le oflo)acin and ciproflo)acin 3- 3rd generation and 4t" generation 9lomeflo)acin8gatiflo)acin: 4- S1(8 mec"anism of action and incompatibilit!. <Bitrofurantoin and nifuro)azide

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2ul*honamides and antimyco(acterial 1- ,eneral structure and nomenclature of sulp"onamides 2- #isco er! and %O1 3- $lassification and S1(

4- Sulp"acetamide and its s!nt"esis8 uses 3- Sulp"adiazine and s!nt"esis 4- Sulp"amet"o)azole and trimet"oprim combination 9%O1 and uses: <- Intestinal sulp"onamide 9Salazop!rine: and topical sulp"a 9sil er sulp"adiazine: ='uberculosis and classification of anti '... drugs

>- IBH and its S1( 1?- @t"ambutol and its S1( 11- (ifampin and streptom!cin 12- @t"ionamide8 aminosaic!lic acid andc!closerine 9%1O8 S1(8 uses and side effects:

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Anti-Infecti4e 1- $lassification of anti-infecti e agents 2- .ioc"emical targets of anti-infecti e 3- 1lco"ols8 %O1 and S1( 4- *"enols8 %O1 and S1( 9p"enol8 c"lorocresol and dettol: 3- 1lde"!desls8 %O1 and uses8 impurit! and bacterial resistance 9formalde"!de 8"e)amine: 4- 1cids8 uses and s!nt"esis 9benzoic and salic!lic: <- Iodine containing compounds8 %O1 and uses 9'r. Iodi and betadine: =- $"lorine containing compounds8 %O1 and uses 9c"loramine: >- O)idizing agents 9H!drogen pero)ide and benzo!l pero)ide: 1?- $ationic surfactants 9benzal&onium c"loride and cet!l p!ridinium c"loride: 9%O18 uses8 ad antage and disad antage: 11- Organic mercurial7s 9merbromine: %O18 ad antage 12- %edicinal d!e 9,entian iolet: S1(8%O18 uses

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Anti-ame(ic and anti- malarial 1- $lassification of amebicides 2- #ilo)anide furroate 9%O18 uses: 3- Iodo-uinol 9%O18 uses8 side effects8 S1(: 4- %etronidazole 9S!nt"esis8 uses: 3- 'inidazole and secnidazole 9%O18 uses: 4- 1ntimalarial8 species of malaria8 life cucle and classification of antimalarials <- +uinine8 c"loro-uine8 S1( and general s!nt"esis of 4- amino-uinoline =- *rima-uine 8S1( 8 resistance and %O1 of +uinoline >- %eflo-uine8 %O1 1?- 1ntifolate8 t!pe 18 t!pe 28 di"!drofolate reductase in"ibitors and its properties 11- *roguanil and its S1( 12- *!remet"amine and its S1(

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Anthelmintic and Anti-fun al 1- $lassification of ant"elmintic 2- *iperazine citrate 9%O18 uses: 3- $arbamazine citrate 9%O18 uses8 s!nt"esis: 4- *!rental pamoate 9%O18 uses: 3- 6i a misole 9&atara): 9%O18 uses: 4- %ebendazole 9%O18 uses8 metabolism: <- 1lbendazole9uses8 metabolism: =- '"iabendazole 9%O18 uses8 S1(: >- Biclosamide 9%O18 uses: 1?- .razi-uantel 9%O18 uses: 11- I ermectin 9%O18 uses:

12- $lassification of anti-fungal drugs 13- 1ntibiotic antifungal 9%O18 uses and side effects: 14- ,riso al in 9%O18 uses 8S1(: 13- $lotrimazole8miconazol8 &etonazole and &etoconazole 14- Fluconazole 9S1(: 1<- Fluc!tosine 9%O18 uses: 1='olnaftate C

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Anti4iral and anti-5I6 1- Cirus classification8 structure and life c!cle 2- $lassification of anti iral 3- 1mantadine 9%O18 uses: 4- 1c!clo ir 9%O1: 3- Ido)uridine 9%O18 uses: 4- Oseltami ir 9tamiflu: 9%O18 uses: <- 1nti-HIC classification8 Sidu udine 8 sta udine8 ni irapine and Sa-uina ie 9%O18 uses:.