ae a eo ae ont “ “oe 4 4 A branch of Chamispy fh Which er eee medical, Om'd Pho macest cal SD science ane studied fs termed a medicinal chamichnys tha or: Stucky of Invention, discovery AUWGh , jolent ficakion, and or boreboatton of biological active compoond Huta metabolism madlt of Acton at dro molecvlan lavel and Hu shnockwe. “SMS Achy oelationshth are alto convered onclen this bronehe y “Garr Medi ctrat chamist sy algo mvolves Stoding 4raexttting dnogs TEED tein blologtlal porwbeuiel and Quanlitalve stowehie — TERPS Activity Relation crib COSAR) athe mestictual cembomd axe EIB, bavteally Corgarte combourd Which mas meldale small terganic molecole, aval biobelymens ‘ History and _ Olaveltbmmack of m edfcnal Chemistoy | ~ ‘The hiStoouy of meclfelnal Chomistry convist of folea , Kehowleage z ad tool having advanced moolen knowlege there aro no a Cee plies fy tho Sumankable advance made fr thofixed af : medictal Chamishry TS Dawg of Ant quity!- AIS tho hed apevtic flat and mins are fy ve stnce tira Sq? ancient civilisahon of te chine fire htndvsthe- Moy au) Far oF combnal mentary and ter met Feuroncom bespler of ar a henge ai TSaEr? PY gone ays: = middlfe agai Dn 8 1b" ¢ eateries tha studies of Phyoice and Chamisiey Shi Ad Pro a ; mm &P1c0-creH Os fo. ae ambian allchomtsls ‘$n ahbelived trad chomi ca could cure ce | Aiseate b ano celsys ai 3° 4431S Floated anttmeny aad tf Salts te € | Pring i Menyand SHR a 1 JThe 1a cen tary AGE oF Lrwovalion avd chimttny '- “The Knowlealge OP fhemishy expaudled fe toa Re col Which algo exterctell tre brovioosly establisel Herbal anmocelads The Chumfcal amaly sis techniges wert advance Kolbe to 18UE syntretised QceHe acted and [3 orth clot ey - 18S Cynthtiged metrant qual togethur trwy bath exctabl is “tee Stage foo) cognate chamaitfary » The 26 ¢ ebony and tue brarmacertcal Bnclartiy = The synfute china bunaber Hed agext were foond to be effective ti borotoeal ed spidrockanlal oftake « Do meg i Stages that prowdesil cancune AS tae systemic qo posehuCoB bacterial ifichou ty hema and animals: q a A water-soluble bowsley ustth artfbactental potency higey tf $ toxicity lower than any know syndhadtfe Chemo on (OG eT UVAF maole dtm Flemivg Abs covercel Penicflith &% OF 124 and Florey Chain @ xomtzed! Hoth (ayy. ‘ ell Development fy tee 21 cout Nema cl als m e400 Manulotr such af!- fa vitken Hoechat. suallised thot trety ¢. He Was also Incpidad by his Colteagebxe who amen PUbeandhs 4, tmmntmolony Incleding Covis pastor Reb ert | CE kd ol, cn Femi] vo Behning ad cht baqbun kihuato- , fy dw 28 cadery ennlteh come op tuthy Hee SCE Arana wal this beconus Mhlunhal tomake vnduydeud now dawg > Upsteochomfcal probedlier & oolehion, Bioletaal Achou! - tha Blologteal Acting of Fegeted og molecole fr Leperalck J om TES physfeocumical charachenishes exenHally tre naboog + £ tube of Anchoal motels awl aljo fo Sprhal QWUViAnp sic > of such qetevh ty the molecule modlolakvy Ho Shruchixe of dro 3 Implies Inbrodecto, , eftmahin, om substilobien.of codaly ¥ gaorp of fra dlowgss ‘the bhystco chomical Poropercties | ~ 3D Ponistkion |- oftan fremont of a cng ane susbourible forit's bf0 log teal achuily th such cates nerere fh tonisakiog > cheque SHewngtime while Sometring He un dissocfaled molecole WU cerrboutib le foo tro came ty which fhouseth inonjteher, > ltgrue of active Compound hee sre actvity + Pka valvet~ ‘he cell membsauo of clomach, smal) Mecosa, amd newveots fiscUe ane Paschal Moxt oF te anus aro ettrer uy The degree of cfssociation Gt Pk) Hamel bateh eq.vatier, Bor ann act ol Intetting, fy Oibi?e Pnaloces eakly acid tc ax weakly bate Can be calevlated Ostng H endlordoy PH Pratleg Leniced! clnoy concwdnahion nS ontintsal day tone ad5 . PH Pleq ofdsuy tonised _ Io Paacendeye m4 it jor pkg XID Fon base t- y PH Peat toq > Unfonised davy cont Sonised dows ant Percendeye of dow4 fonitey -— pyPka~ PH ie rere 3 Solobet itty + woaten courtitoeudh thamajen poouien of living bodies “therelboee tue HANI IANANAN biochem foal seachiong occuntrg @ u9tth fy Q living bootyrely eltren on dune micro molemuled -| dispoued 4, tre phates a Polenelty No dswa mBlecolel fs comblelety mageluble every = molecvle it coluble fy bol ano BPO ond Hore aque «= UBEA combardnads of 4 cell Mow HOT Hire colvbt itty obegout tt i differcuct blw each compobmad » i ea D) Partition coe Mfcietd te cep tlibontom comer of clnag = cof ty tre two bhate is FOumed ay & Parti tier, cefPfete wy & We oletormined ink vibio Using y_ Scena] ay tne Itptd = Phare ond a PH 4 A4,L00U5 brosthate boffer os te usater a Pra beavee it's SHawolrdl ced meataromad tn tivi a Systems i difftcvlt Partition cofciet cry chad gw etbouned as t- & & Pro (dlovg) Iti [es wooly -; 2} Haag boucling {= P bod fh Which o hydregen ots wl 4 4wWo Of, cto togetluy th formed af hyroqen bowcly CHe bond) This formed Ehud electronegative @ Hydresen clond othe atom Which Can form H- bowls Carry at lente andl onchreral > Palin of election “the cutons foaming H- bond mosee extent adcy Cl oma Se hydrogen bonding fs Cfayifiel inte >) Latemolecvlan Hydrogen bond ts: -this H— bowding Occuws with th dra molecoles > O-Nikiobhanel 5 (pds motecuten hy dre gen bonding This H- baomeling occuns 5 with jf, the molecle coc 8 - Tem Long? Pe ntoobheny |. st. 5) protein binding i= Prog distntbotion eltmination ond its —z2 Pharmacological effects get efPectea by bindling oF deg of plasma hotefy doe 4 thet hte molecu fey wWelqnk They cannot bar ‘thorough capt) a thefoy fo [Ebf0! soli aise Oud lve fy Py hey Can yl OSE Fhe cell membranes | ging Can Oven thong), lenicvanol, woalt, tad J Plbvectn co mbsises nary 50% of Hretodap : : 9 Prwg Pototel n bi Hydrogen bind vey uaB» Platma prblein cael ais tra clowg bivlg fy tua laama +” 8) ChalaHont~ The voveuitble binging of tus cligand te chel Mo: eeeaae chalabivg 29 Gk « SLO IY Ag eck 06) comp [ening oa aget toa metal ten to Poo a chelate fs calted eh elabteus fa THistenmis moctiy wced for combleres havivy melel tons on bowled with hoo Or MOR Albom of Cheleltuy 0g ent vig on Combinakion ou ionic bendy - ; Chelatng agents — Ligawls hau hug yoda than Om election Sa denalivg~ gsoub ara called - Chelabiug agent the mot or cMechoe comblext agonk th ligands @2 amino and ( Conbory late low} U7 CH2 COOH en " ctncoou wn 7) Bio ee io Tha femal and =D Strwetoge cloorieg a SPR Stories and d i : Substttoonk ad Bndttocaf yao becombaned with tht Fe ; Fimilay biolegi cal acliyitiy OF compound havieg wl Biosostenism fs medicinal chemistry APPHACH Loy aot chong a Alevigning of rew chug aPblied wit, atead Compound Cie J = Using a borocets of molecolan modi Penton. = Ssotener and Psostenitin'’ - ul lowgmnvin pce Hot WO mang On molewle shold hoxgeny “J Strllen Chorattenistcs iP-touy eee idutteal i Pleckroy rp, Sal Awel RANI Cork aud Such feder of fons I ns ~~® Y -_ ® pfolsoteresi— The Combomal oor gaovp oP almoxt eg val molecviar ° BP Shape woloma and elect distribu and cimilay Physical Chay actOitic aro called bio foleud + clasificahioy of Bion hey :~ » 1) Cladgtoal Riots ree ~The volence elecknern conbiqun ~ , Hoy of Hue fonchiorgl qewobs ano stmilan: CX tay OH, ~cHy-, -cH= _¢- , _ i I Hey til . * . . D Men~ classical Biokteus- tro volerce electrsr con fiq~,. 2 sets of thong Ponctoval geoob an vot cfmilar. CH. OW x } oy Hyerroxy| groeh cay bohu| Qeroup a CooH -NH COM boxy! ‘ | aS o excl gorwep ele on ae a Ye ag Jeo a Thiovanea > oH a Pa Y Ha a 2 aI we 4 eae 2 | ev® OPHcal jgomanism $= A clowwy Jrunapevtic ond torte ¢ frect Can be undurstrad by the concebtys of Stereo Chamistoy enand (omens | ijn Ghxy - caymorehoy mal chidectiy amy ofowy is Said to be chinol 1f cHleat one fwe Rnoutiomony ObH cal (Omudtm ano tie Follousingy Super = ub Erantioney i into two foot, The Paior cornoy om th this 3p Anne still othey hence — A moleole beomes asym and exists ¢ fuoy ane liffout - }! al Heeger or chy a C)lacke acta = . cl With 400 Similan avy rmebifg La} t MWS = A compoun a ° : cosine ee Raid The ouNlon foo simian UyPmebr he Carbo atoms is thak ah os & cartbory] Joovp aro wesc Petco i a VLE | 4 Ho -¢ N ong COOH sou ant lactic actd LyCOOH cmH fo" } -c- 0H Ho-3—H Hemp Maereeee Hop eb ol HEE ow a CooH CooH cOoH ; 5 DCA} LCS meéjo ortante acted ertanic actdl te acid 9) Greemetnical comin ismt- The Phenomanen of g eomekrtea| tomato alse olettolu the achon of corktin clog + 0 cliaskeoromen occurs clue to Surtdricled wofakion around a sy TA A geometnt ea] isemenitm « et Alga nd 9 “Re CHS He chy a 7 ‘a aN H a, cis i Tr a Dnf uence of Greomektcal tsomoriem of Phanmacolegica | 7. fehivity t- a, Acomboond may get vanibly oliskytbsted in a livig, system doe to the olf Pere in Ht bhysteal pooperties of Icomou + “ara a Frysilost PH one of fia tsomeny may be highly’ . tonisedd seewtting th, © dfffocree | ; LT) membrane penthrakon- met in Surface qelsonblion andyy) a i } HO r oe dstoadi |) Cat ( Dows metabolicn \ ® a The chemical alteration of q clowy by tra body fs teed 24 oe chowg metatoliim algo known a4 biota Romatior a 7 Dowg metabolionr Poiinciblest- Live, Qo iaeleepetie Al ; metabolism of 4 no of a lovey + Thyw poroceld of metabolitm OCCUNS jy AO part Phare £ (Metabolicm /rie, -Synthelfe bros J THiS is fre Fx ite phate of metabolism Wheq dry enter OA | Te molecule Pom a vaactve site ov forctoual gowop = Such a3~ GOH, -sH, on -NHo} Which Pushy conjogedd with 7 Fre molecu! i Phase BD en 7 The molecule Libobhitictty Wike ond hy dobhilicity eryse oT to fouliate ffs excention: tr Powers of phate f’ metaholitny + Una Jo aay one of to follow Phase S me tabolitna» = Chilotdadion Reactou'- Civer celld fe hobathocytes Reon tue = move Common site Hn oxtdahinr of a dogs molecules with th St Tre hebatocyte mictosome & trrontt wrure eiclation, oceuses The dowy molesule may % MJ) MAjO pHoceda during a t Mixed function \- D's trengyme system calely.shg exh] of dwg mote lea- Y a Varig system components make vb Hae ehgymt ee . zuON ie 6 Cyto Chywms OX Tote engyme 1 FF iy gervrally 24 cyto chooma, . puso ( cyPyse) Db) NADPH I= St is anotun importa rember oF tuis axidabive > gustem and acts Q COPA YML + Rey NADPH cytochsiome Reductre!- SF is anole, eng yma Which > Ie chemically 4 Flevo proteins r 7 a (hy Hycbrolysts *- $y tris bowce tho dog molecule fs booker down in to stmilan molecules by talraedtios of water mateark ~ CH) gga llity Reduchou't- This sumacton fs avoctated with Hre imknoduchion a oF H ctoms e9'~ chlonambhenteal [¢ vadloced fo any! amina ¥ (Ww) Cycltgatou'- This broces ousulk fo te Mometion of 4 Sting 3 Stowetwore From comourel arranged tr a shnaight chain, %, > egi- Prroguant | ; WY Decyctisatton!~ fy tie Porocels the sting chrocture of que cyclic ows molecule oben ob egie Phonytotn % Phare I Csyntobte Reaction) *- The seeaction i choyactentted by tre Rommatio, oa conjugate Gilycureny) sol phate, methy) , acety}, glyceryl, and glu kuthione ane tre gerovps « ” Crimenly Imvalveds ti conjogte omabion ' i‘ 3 ReRehond oF brake ara tne bahay ousolhng fy oldeatftlong? ; He dovey «Tey Incluole , pal? ey niGombegption with Glocnonte actd- Of torah 4s +8) Glu Cun onte acid t obiind Mo commantty Brom D- ylvcae 35) 1) Glocononic aciel Ic eutly quakile foar combination with foncioval Gowop LIKE amines ,alechol, actds ete@© C) GlUcwonid 3 are commonly pooduced by all mammalss © UDP. albra ~ glucaunenicle brlucovaersh UDP ~glucunony| cforaws on Torah enare: Glvcveroniale C dow , Ui Conjugation with sulphale moi etia'~ this fer stontfeotsteh ‘nm tue melabolitm of hunvitc Combourd »sulprak cou} ogahion a fh atlco cuFemed 4o ay entiuneal culpable syntnunie a a . At MB Conjugation usitt Glycine moieties "This fs tre ma joy a bathusay involved fy tre biottowshrmatiog of soma doug * a CH in biota Pormehion of salicylates eer =~ uv) Conjugation with Acetulation'- This conjugate yielala - ob amice porodlucts just [tke red obtained 1% conjogetion wsith a albha- amine aofol i Pactoon qffertivg Dug melebarlism’ ~ a Tha followings factors Play a vrele ty modlfPying dawg metebl Qala i Br hibltoad \~ Some olawg trhibtt tha low metabelising san gs Pooction Gig e THe low “melaboligm «Ps o ouyoth tre cluniag, =o OF achon ase 5 LHAL ge Ppeailoon irs iii hget- Do infant ounel yourd ichildien ol%89 meteotim ) i engumes CU poosly cleveloped thu 4 dew9 [i poosly metabolism p . . . ath) $ext Dowg mekeboliting ability to females fe eH thas drat > tt malas “ww sbecieli- Some mebablttng engym cre prerest only fy q p> few mammatitns cbecies aud ose apsent tp homons+ ‘Thos A029 metabolized by trae Chaym4y borove to be toxic fo humank = While fry Ow noy- toxfe to otrury- >i) boneke'- Certain inolividvals may tnhot dows metabolism ~, eraymo ouFiciency e4- genskie oleFicienty of brlvcere 6~ Phosbiate Dehyebwog ensse ~ (6.-6~ PD) eng yme vurtult tr hoemolysis ay Administering botimaq.ulna’ 7 (uit Booly tempera s- Noibk th booly temp: enHancel dowy Metabolism while a elecnense ty hocly Femp+ rad ucer’ dows metabo | itm » 7 Sheneochumieg| Aspect} ¢ Dow metabolism §— Tyr Howt ouly tre Phys/olog fecal factooy, efPectvy yenebiot'c metabolism, some stebaboliti Ja 4 5+fretoer alco effect dows bie fray Romatin, He xenoblolte e metabplicm Sowa endogenous subchuce Which we chisel moleccles- a ‘The metabolic ctowochsmt cal CUachod aro as fillarsi- Q ard substaale ctorencelectivity !~ Bn this fae onadiomoy of @ chia! |G, Substrale ge! jelebolised at client gated 1- exansblel~ S52 Acanborylation of sx | = 4 aaa eleti, Poredoct Storenselectivily!-Br tis a ned crteal conve th ceouted edie molecole Cd one eidntiouens geht melabolism Example! = Recluetios of Keon to steneotsomunte A\conol + ots 1) cubstowte « porodoct- Stereo selectivity Bh tnis aq ned ceadaa oF a chisial molecule gets metabolised fr So ene of two Aiasteneo mor PXamblei- Reductten of Wanhamin enanttemens® et a eer as |i > didn ° \vxadeto Say eerPRRER Rt EtItt