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4th sem medicinal chemistry paper B. Pharm

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mc1 Ppr+imp

4th sem medicinal chemistry paper B. Pharm

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tomerkailash12
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© © All Rights Reserved
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7 ·
I' '
'ilibj,•et

... -~-
J
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Total ,1/ark.\; 75
Tir.:,: _; lll'U~

:i-,.· 011:: 1_ .-\:rc:r.~?t ~u Sc:czions. ffn:quirc any rn,isSing data; then choose suitably.

•• .. .. ..-r 10 X 2 = 20
H
1. Attempt all questious in brief.
· ~efi nc metabolism.
~ t o~t the role of panition coefficient in relation to biological action of drug?

~
-- - '
~esc noe the synthesis of Tolazoline.
~ v e structure and uses of Phenylephrine.

~
: • iscuss cholinergic receptors and their distribution.
~~iffer ~nt,:-. te ::t.nticho linervi~ ,inn :mtidml in~t~nt~ ~ .
:~~p. ..-e the basic ring structures and W\;ntion us~ of barbir,lratc and ber:zodiucpinc.
.m
: .,- ! u1ve .J:.e :MOA and structure of chlorpromazine.
1
::,
Dis~~ the synthesis of drug that causes disso~ e .anaesthesia.
~

-~

~

. . " ,..._---= :---- ------ - - ~ ~
_;/_ .: '.~.::;:-..A7lc g:n; s,rucrureE or any !'No na~c~'tl~)i:::tago •.1sts.

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. ,,- . ' ,_/

• 2. Attemp t any two parts o ~ following;

...t '
'. a ! Summarize about various pbysicochemical parameters that affect
~ Classify sedative and hypnotics. Outline the synthesis, mechatti~
I l diazepam. •v
~! Classify NSAIDs. Give the synthesis of Ibup~ien. ~r- _r-:;• ·•

; . .. _t,:>~
;~ .~-f~-~ IO~
3. ~ . .
Attempt &JD'Ji~ parts~--;;,t, ·· ,:. ·-. _ . ......., _ ~ 7 X 5 - 35
. , • , · ·. _ - , . .

i' ,. ~ ~m~r~!riasc ! and pha:.e n rn~~·~~EliJJ.l&l-ii


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i~i.ii~~:~-affe.ctino.
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• • " ._: -.• ,:,"''.
"lffilO
/ ~:-;-;--:_c,,
1--
.:, ---·-
• I ~ - - ~-

- OutJine 1he classification and SA~'ctsymJ"lthomimetics.• -. ~.::..:·-· --~- --.-· ' · ·


~

• ' Uustrate the MOA, synlhes · · , . :achol. .
_. ,. - i~·Carb
es of(i)'Dicyclomine hy~ocli•l~~~~ 1·
· i
(

I Classify anticonvulsants and give synthesis of phenytoin. . _ •

I
- Explain the biosynthesis and cataboiism of a&Cebulamines.
Give synthesis of propranolol and discuss SAcrt;R.o~fibeta;;;"~bli;:oc::ik;.:ers=.:-_ _ _ _ _ _ __J

·'
https://www.aktuonline.com
Sub Cm.
,,
.....
Printed Pa ce ~l_ of_ l~~ --, . ..... . ....~-.. ~
Paper Id: [ 910 027 ]
Roll No: [[ J[ J: J: J: J: J: J: J: JI :T _
R PHARM NATION 20 19
"i
(SEM-IV) THEORVLEC~HAEMM -20
• MEDICI NA IISTRY - I
-•

Tim~: .3 Ho urs Total Marks: 75


Note: l. Attempt all Sec tio ns. . . d t
Tf_req?ire a~Y. m1ssmg a a,. then cho ose suitably.
2. Any spe cia l pap er spc ctf ic
mstru ctmn.
SECTION A
1. Attempt all questions in brief. 10 x l = 20
... D~firi~ &v!ub:!;t;• .
b. Wh at is rin g c~ iva lcn t bioiso
stcrism.
c. Wr ite the mo de of act ion of me
thyl dop a.
d. Wr ite the syn the tic Toute of Phe
nyl eph rin e.
e. De fin e par asy mp ath oly ticc age nts
r1'3~ca,, ('l~n11ru=-cti::ar?5e 1nl, 1h:1 tnrc .
f. -· -··J :.
g. Wh at are the ide al cha rac teri stic .
of sed ativ es and hyp not ics .
h. Dr aw the che mic al stru ctu re of
Clo naz epa m and wr ite mo de
i. Wr ite the syn the tic rou te of of act ion
hal oth ane.
j. Wr ite the mo de of act ion of Ult
ra sho rt act ing bar bit utr ate
s.

SE CT IO NB
2. Attempt any two pa rts of the
following:
a. Ex pla in in det ail ab ou
t iso ste ris m an d bio iso ste ris m
b. Dn,cm,~ the SA R bet.a blo wi th sui tab le ex am ple s.
cker an d wr ite the mo de of ad.
c. Wr iti. the chemical structure iun ~y nih ~i~ of pru pa no io i.
, mo de of action, syn the sis an
procyclidine. d use of car ba ch ol an d

SE CT IO NC
3. Attempt any fiv e parts of the
fol low ing :
a. Discuss the SA R of barbitura 7 X 5= 35
te wi th suitable ex am ple s.
b. Classify ant i-in fla mm ato ry age
synthesis of ibu pro fen . . nts. Di scu ss the ch em ica l str
uc tur e mo de of act ion an d
c:, Desrrjhe grometric:a1 iS<lme:ri~
m in Tt".lr'ti(ln t<' affr.f:t bi<'l<'gk
d. Di scu ss in detail ab ou t indire al a~ tiv ity.
ct acting sym pa tho mi mc tic ag
e. Cla ssi fy ant ico nv uls ant drugs en ts.
an d Ex pla in SA R of suc cin im
action an d synthesis of eth osu ide . Wr ite the me ch an ism of
cci mi de.
f. Discuss the SA R of mo rph ine
fentanyl. ana log ues . Wr ite the me ch an
ism of act ion an d syn the sis
of
g. Wr ite a sho rt no te on dissociat
ive ana est het ics .
Printed Pages: 01 Nub C:,Hie: IW402'f'

11.PIIAHM
(SEMESEll-lV) TIU~Ol(Y •:XAMINA'l'ION 201H-l'J

Tl•t: J ffp11,s
MEDICINAL c1n:MISTR\'-I
To111I M,,,h~ 1,
Note: Attempt all Sections. If you require any mi:.:.;ing data, cho,,:ic auil;.ibly,
s1-:cnoN A
Attempt all questions In brief.
i ~- Define pa,rtitiofil.Q_~tlicicnt and give its applications.
t b.. Explain role of ionization towards biological action ,,f drug.
2... c. Explain in short biosynthcsis of cholincrgic ne,•1m,tran1,mittcn;.
d. Write chemical structures of phcnytoin and Et.holoin.
e. Write ch.f'!"1ir~I st.n.1ct•1rl.:.' and uo;r-; 0f Kct;1mirn~hy1Jr1)d,lnri 1k
f. Write diffc.cnccs between Narcotic and non-narcoti c analgesics.
g. Compare benzodiazcpincs and barbiturates.
e
0 h. Write synthesis ofEthosuximidc.
0

-~
-a0 J. Define ulb·a-sho1t actini barbiturate!> with cxamr+lcs.
~ SECTJONB
l 2. Attempt any twtJ pam of the following ; 2 1 10 • 20
i a. Define biotr:msformation. Eiplain principles of drug metabolism including pha.:;e I and
phase II pathways .

• 1 b. . Write classification, mechanism of action and structure-activity relationship of


antipsychotics with suitable examples.
Exph!!n.Bjoj~oc.tr.ri~m>typr.'- ~•,d t.h.ei.r r.nl.r. _in ,ln1g, <1.ic.r.ov<'ry wit.b ~ Ji1l4hlr P-Y~mpl<',

• SECTION C
3. Attempt any five parts of the following: 5 x7 = 35
a. Stereochemistry contributes towards biological action of drug. Explain with examples.
b. Write synthesis, mechanism of action and uses of -
i) lpratropium bromide, ii) Tolazoline.
c. Write a note on medicinal chemistry of barbiturates.
d. Define adrenergic blockers. Explain structure-activity relationship studies and uses of
beta blockers.
e. Write classification of parasympathomimetics with examples and chemical structures.
Write synthcs~ .,f Carb-adrol. ·
f. Write syntheliis, mechanism of action and uses of -
(i) Chlorpromazine hydrochloride, (ii) Carbamazepine.
g. Write chemical structures, uses of - i) Indomethacin, ii) Valproic acid, iii) Phenacetin,
iv) Meperidine hydrochloride, v) Sulindac. ·

http://www.aktuontine.com
Printed Pages:01 Sub Code: BP 402T
Paper Id: ,,..~23..,..80_77_....,
Roll No. I I I I I I I

B.PHARM
(SEM IV) THEORY EXAMINATION 2022-23
MEDICINAL CHEML~TRY-1
Time: 3 Hours Total Marks: 75
Note: 1. Attempt aH Sections. if require any missing data; then choose suitably.
SECTION A
1. Attempt all questions in brief. l0x 2= 20

(a) Define Bioisosterism. Give examples.


(b) Give name and structures of two narcotic antagonists.
(c) Discuss mechanism of Methohexital sodium.
(d) What is Cholinesterase reactivator? Write its example and use.
(e) Write synthesis of Phenytoin.
(f) Give uses ofTolazoline and Dicyclomine hydrochloride.
(g) Mention the significance of Ionization and solu~'!:S)in relation to biological action. ('\~
(h) Enumerate Adrenergic receptors and their di~bL1ion. · V
(i)
V
Differentiate Phase I and Phase II reactirv.~etions. 1'~S0·
G) From which category chlorpromazjtf~ug belongs? Give its structure. ~ •

.
0,;:(/
~CTIONB
.
~~" '
2. Attempt any twoparts ~following, ,.___C:)- 2 x 10 = 20

(a) Wh:tt are Sedatives and Hypnotics? Classify them. Give SA~~~enzodiazepines,
ang. synthesis of Diazepam. • tx""O
(b) Classify Narcotic analgesics. Write SAR of Morphine an~es in detail.

(c) Explain Physicochemical properties in relation to biolwric~tion in detail.


f"'i , ..
~ «.I
SECTIONr>-,.,
3. Attempt any fiveparts of the following:R')'l,; 7 x 5 = 35

(a) Give uses, mechanism and s~~of any two: Carbachol / Neostigmine
/Salbutamol. ~
(b) What are Sympathomimet~jts? Classify them.
(c) '°(g;nts. Discuss the mode of action and synthesis of
Classify anti-inflammat~
ibuprofen..
(d) Write short note on Adrenergic Antagonists.
(e) Discuss SAR of Phenothiazines.
(f) Write short note on Cholinesterase inhibitors
(g) Elaborate Drug metabolism principles of Phase I and Phase II.

QP23EP2_229 I ~-08-202313:33:48 I 103.211.190.27


BP402T. MEDICINAL CHEMIST RY - I (Theory)
45 Hours

Course Content:
"ti ti
Study of the development of the following classes of drugs, ClassI ica_ ~n,
mechanism of action, uses of drugs mentioned in the course, Structure activity
relationship of selective class of d~gs as specified in the course and synthesis of
drugs superscript ed (*). o 0

0
10 Hours
. Unit-I
Introduction to Medicinal Chemistry
History and development of medi_cinal chemistry
Physicochemical properties in relation to biological action
Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein binding, Chelation,
Bioisosterism, Optical and Geometrical isomerism.
Drug metabolism
Drug metabolism principles- Phase I and Phase II.
1
Factors affecting drug metabolism including stereo chemical aspects.

Unit-JI llHeurs
Drugs acting on Autonomic Nervous System
,. Adrenergic Neurotransmitters:
Bios ynthesis and catabolism of catecholamine.
Adrenergic receptors (Alpha & Beta) and their distribution .
Sympatbomimetic agen ts : SAR of sympatliomimetic agents
Pirect acting: Nor-epinep hrine, Epinephrine, Phenylephrine*, Dopamine, Methyldop a,
Clonidine, Dobutamin e, Jsoproterenol, Terbutaline, Salbutamol*, Bitolterol, Naphazolin e,
Oxymetazo line and Xyfometazoline.
Jndirect acting agents: H)tlroxyam phetamine, Pseudoephedrine, Propyfhexe drine.
Agents with mixed mechanism : Ephedrine, Metaramino l.
Adrenergic Antagonists:
Alpha adrenergic blockers: Tola29!ine*, Phentolami ne, Phenox}b enz~e, Prazosin,
Dih)tlroerg otamine, Methysergide.
Reta adrenergic blockers: SAR of beta blockers, Prouranolo l*, Metipranol ol ,
Atenolol, Be~olol, Bisoprolol, Esmolol, Metoprolol , ~betolol, Carvedilol.

Evaluation Scheme Bachelor of Pharmacy I, Il, III & N Year syllabus 2019-2020 Page63
UBiMII __ 10 Houn
Cholinergic neurotransmitters:
Biosynthesis and catabolism of acetylcholine.
Cholinergic receptors (Muscarinic & Nicotinic) and their distribution.
Parasympathomimetic agents: SAR of Parasympathomimetic agents
Direct acting agents: Ac;ylcholine, Carbachol*, Bethanechol, Methacholine,
Pilocatpine.
Indirect acting/ Cholinesterase inhibitors (Reversible & Irreversible): Phy.;ostigmine,
Neostigmine•, Pyridostigmine, Edrophonium chloride, Tacrine hydrochloride,
Ambenonium chloride, Isofluorphate, Echothiophate iodide, Parathion, Malathion .
.Cholinesterase reactivator: Pralidoxime chloride.
-'Cholinergic Blocking agents: SAR of cholinolytic agents
Solanaceous alkaloids and- analogues: Atropine .sulphate, Hyoscyamine sulphate,
Scopolamine hydrobromide, Homatropine hydrobromide, Ipratropium bromide*.
Synthetic cholinergic blocking agents: ~opicamide, Cyclopentolate hydrochloride,
Clidinium bromide, Dicyclominc hydrochlor~ e*, Glycopyrrolate, Methantheline bromide,
Propanthcline bromide, Benztropine mes yfate, Orphenadrine citrate, Bipe1i din e
hydrochloride, Procyclidine hydrochloride* , Tridihexethyl chloride, Isopropamide

-
iodide, Ethopropazine hydrochloride .
.

Unit-IV 08 Hours
Drugs acting on Central Nervous System
A. Sedatives and Hypnotics:
Benzodiazepines: SAR of Bcnzodiazepincs, Chlordiazepoxide, Diazepam*, Oxazepam,
Chlorazepate, Lora~pam, Alprazolam, Zolpidem
Barbiturates : :;iAR ot barbiturates, Barbital*, Phenobarbital, Mephobarbital,
Amobarbital, Butabarbital, Pentobarbital, Secobarb ital.
iscellaneous: Amides & imides: Glutethimide. .- - - - - - -
'/-
G lcohol & their carbamatc derivatives: Meprobamate, Ethchlorvynol.
ldchydc & th eir derivatives: Triclofos sodium, Paraldch-.c:;_
B. Antipsychotics
de::.:·- - -

Phenothiazines: SAR of Phenoth iazines- Promazine hydrochloride, gi1orpromazine_


hydrochloride*, Triflupromazine, Thioridazine hydrochloride, Piperacetazine
hydrochloride, Prochlorperazine maleate, Trifluoperazine hydrochloride.
Ring Analogues of Phenothiazines: Chlorprothixene, Thiothixene, Loxapine succinate,
Clozapine.
)Ci Fluoro buterophenones: Haloperidol, Droperidol, Risperidone.
)0 Beta amino ketones: Molindone hydrochloride.
')6 Ben1.amides: Sulpiride.

Evaluation Scheme Bachelor ofPhannacy L Il, III & N Year syllabus 2019-2020 Page64
·•

C. Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant action.


Barbiturates: Phenobarbitone, Metharbital.
Hydantoins: Phen)toin *, Mcphenytoin, Ethotoin.
,x Oxazolidine diones: Trimcthadionc, Pammcthadionc.
Succinimides: Phensuximide, Methsuximide, ~hosuxim ide. *
Urea and monoacylureas: Phenacemide, c..arbamazepine. *
Benzodiazepines: Clonazepam.
Miscellaneous: Primidon e, Valproic acid, Gabapentin, Felbamate.

Unit-V 07 Hours
· Drugs acting on Central Nervous System
~ General anesthetics: ·
Inhalatio n anesthetics: Halothan e*, Methoxyf lurane, Enflurane, Sevoflurane, Jsoflurane ,
Desfluran e.
Ultra-sho rt \ , acting barbitutrates: Methohex ital sodium*, Thiamylal sodium,
Thiopental sodium.
Dissociat ive anestheti cs: Ketamine hydrochlo ride. *
~ Narcotic and non-narc otic analgesic s ·J
~7 - Morphin e and related drugs: SAR of Morphine analo~es , Mmphine sulphate, Codeine,
Meperidi ne hydrochlo ride, Anileridin e hydrochlo ride, Diphenox ylate hydrochlo ride,
Loperam ide hydrochl oride, Fent@_)'L citrate*, Methadon e hydrochlo ride*, Propoxyp hene
hydrochl oride, Pentazoc ine, Levmpha nol tartrate .
Narcotic antagoni sts: Nalorpbin e hydrochlo ride, Levallorphan tartrate, Naloxone
hydrochl oride.
~ nti-infla mmatory agents: Sodium salicylate , . A~n, Mefenami_s, acid*,
Meclofen amate, Indometh acin, Sulindac, Tolmetin , Zomepira c, Diclofena c, Ketorolac ,
. --- Acetamin ophen, Antipyrin e,
fuupro~ *, Naproxen , Piroxicam , Phenacet in,
v
Phenylbu tazone.

Evaluation Scheme Bachelor of Pharmacy I, II, III & N Year syllabus 2019-2020 Page65
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