Mansoura Univeralty First Semester Exam. Faculty of Pharmacy Date: Jan, 23, 2010 Dept. of Med. Chem. All que: are to be attempted (QT G2 Marks) A- Complete the following table, write only the missing parts (17 marks) a) Generic name... oF Chemical mame «...-..++ (2) Possesses high pharmacokinetic character on due to... QO. ef See 1¢ forms mutual prodrug with the The drug target is. tiv used in combination with-—~(8)-——-— Hs (draw its structure} ad ‘hs put cnt 4d) Generic name......(19). Results in hormonul imbalance and 2 meno we ahnormat menses due t0...(11 )..... hs Jo ; ©) Generic same. It is metabolized by the enzymes... 10 afford...(14) A 13). Its pharmacokinetic properties could be improved by ...(16).. M1 is am analog of ...(17).B) Select the correct answer in each case of the followings 15 Morks) 1-N!.(2-Pyrimidinylsulfanilamide is the chemical name of : a) Salfadiaxine bb) Sulfapyridine ©) Sulfaisoxazole 4) Sulfamethoxazole 2-An example of antifungal agovt (hat inhibit sequalone epoxidaso is : a) Miconazole b) Ketoconazole ©) Flucytosine 4) Naftinine 3-The hepacotoxieity of INH is due «o the ix vivw formation of; 8) Tsonicotinic acid b) Nieatinie acid @)N-Acetylisoniazid —d) Acetylhydrazine 4 The mode of action of Oseluumivir depends on (he inbibition of: 3) DNA polymerase enzyme b) Neuramini 5-Pe G hana self destructive mechanism due to the presence of je enzyme ¢) Protease enzyme d) Protein synthesis *) Acylside chain 1) Reactive ftectam carbonyl! 6) «Carboxylic group wand by An example of urvidopenicillin is: a) Ticareillin by Pipera © Pivampicittin 7-An example of NARTI is: a) Rikavirie b) Niverapine ©) Zidovudine & Carbenicillin is a prodrug which is hydrolyzed in vivo with the formation of: a) Ampicillin b) Benzylpenicillin ©) Amorteiliin ‘9--The antifungal agent Nucylosine is converted én vivo o metaboli a) SFluorouracit h) S-Fluorothymidine —_c) $-Fluoropyrimidine 10-Aa example of beptaene andfun 3) Griseofulvin ——b) Nystatin Uibiotie is: 6-{3-Phenyl-S-methyl-isoxazolyll pe | name of a) Tiearcillin 1) Clexaeillin ©) Oxacillin 12-The targeted enzyme in cnse of ticonazale is: 8) Ma-lanostcrol demethytase b) Amideoc ——_c) Cytoaine deaminase 13- The skeleton of penicillin moleeuleis derived frow the amino acids: a) Cysteioe and valine 1h) Alaniaeand valine —_c) Lysine and alanioe 14-The substituents on pyrimidine ring of sulphadonine ure: a) 5.6-dimethoxy b) 2,6-dimethoxy ¢)4,6-dimethoxy 15- Ribavirin action attributed (0 its siructural similarity with a) Cytidine b) Guanosine ©) Deoxyadeno: d) Acyclovir ¢) Aglvcillin 4) $-Fluoropyridine d) Flueytosine a) Carbencillin 4) DNA polymermse d) Cysteine and alanice d) 2,5-dimethoxy d) Thymidine 2 4) CarbencillinCa ‘O11 GI Marks) 1) From the following drug pairs, encircle the letter (A or B) corresponding to the drug ‘thot fulfills the mentioned statement, then give reason for your choice nae (12 morks) 4. Stable to gastric acidity oo, 2. Less CNS side effects ne eo neon ~ Gn A B ‘3. Con be administered orally Mote OFS, A 4. More stable in acid medium 2) Explain why this drug should nol be administered during the first; %,, we — trimester of pregnancy [OW (ilusirate your answer with chemical structure) @.5 marks) ne pos : ‘ the enzymatic bacterial inactivation (Give the generic name of the obtained drug) (25 marks) “az!4) Encircle only the letter/or letters of the WRONG statement{s) describing the provided drugs (1-4). (4 marks) ‘inhibits bacterial DNA gyrase. 1 Ny i b. Fourth generation quinolone derivative. l . | ©. ILis 1, S:caphihyridin-4-one-3-carboxylic JD {J acid derivative. d. Should be administered with mincral supplements, 2. ‘a, Can not be administered orally. 8 s b. Wis B-lactamase resistant, Napa c. is inetabolically stable. door : No PN 4. Contains anti-oxime i och? 00git; 8-60-61, Se * 7 ‘a. Active against Pseudomonas aeruginosa ak «ew, b. Nanural agent 2 W “Tr ¢. Azetidin-2-one derivative 9 Dn. . | & feLactamase resistant Ss, na netics ut f + a. is 6 Prmetlylepimer is more three times as ative as its a-methwiepimer. b. Causes teeth diseoleration in children, ¢. Iis absoxplion is impaired in presence of milk 4, Binds to 20 $ ribosomal subunits 5) Use the provided to answer the following question: (10 marks) A) Bithionol Bj Chloramphenicol C] Cilastatin D)Dilexanide furoate —_E) Eflominhine F) Erythromycin G) Flubendazole Hy Hexamine 2) Lincomyein T) Niclosfide kK) Nifutimex L) Phenazepyridine M)Praziquantal NN) Scenidazale 0) Suramnin For each of the following statements, Select the ONE lettered option (drug A-O} that is most closely associated with the description. (Each drug may be used once, more than ‘once or nat at oll), 1) TWhinds co che heleainth protein tubulin preventing wbulin polymerization to microtubules. 2) tis a niteosalicylanilide derivative used as potent taeniacide. 3) Increases cell membrane penneability of worms resulting in loss of extraceliular ealeiuin. 4) tis 4-methyl sulphonyl analog is quite potent and hes nol Deen associated wilk aplastic ane:nia, 5) Its 7-chlama-7-deoxy derivative is more bioactive with better oral abscrption. 6) I possesses local analgesic effec: on the mucosa of the vrinary act. 7) Wis an acetanilide derivative used [or treatment of luminal amebiasis. 8) Iisa thiomorpholing derivative used for treatmenic of acute Chagas’ disease. 9) inhibins reval dehydropeptidase-t. 16) Its light induced hycrotytic reaction product in solution is 2-amina-1-(4-nitrophenyT] propane I,3-dial 4‘QUT (18 Marks) 1) Examine the chemical structures of the following drugs and fill in the blank the required information (write only the missing parts in your poper’) (15 marks) we a) IN is the aetive form af . po b) Its targeted enzyme A , @ | a) Generie — neon Her b) At is not suitable for oral adi j (4). ‘e 8) Medicinal us b) Tron chelators antagonize is pharmacological action because .......6).. jolie activation results in (be formation of 2) His am interealating drug containing a planar sereeee(IO)as 1b) The positively charged amino group forms sessseu(LDossesbond Wb .0(12)-.. in DNAL nocleus. a) The fluorine atom decreases the susceplibility of the dog t0 (13)... ¥vhile the phosphate group ia important for «os sndl4) a) Allopurinol inereases ils loxicity due (0 18).2) Match each ontitumor drug with the mest appropriate clinical use and give reasons for your choice (write only the letters with the matched eumbers in your paper) (3 marks) ~ (2) Brain mor (2) Breast cancer (3) Immunosuppressive agent z 2 (4) Prostate cancer yey oH T 5) Pancreatic islet-cell carcinoma b © ; (© Multiple myeloma ce Nee fof ¢ Mad ADE seg gad Mie cae 6 ge clase yy + AT A ye sake cl oh pe UE le Ua an Alsy Gia aa Ce AT Na ay pal Gey hy A BaD ba Da iy fyi base La gd Dead ey pal Sih gpl 5 a iy Splat gd Vag ei AS Ua cata I gpa yl ll ay i caiay SL Lie Span aly Fle yp ARAL plat gh YN UF ed pad ght bata Las = (chant y GI tn GRR MeL a (EUG) coe ISN) ¢ AAD gal te Fan (CAAA pin ay GEN Zeta AM 100) co MT} = AES ly Casey Gly gpl GLa Fall le papell SY ogg © Chay aly al ean pad Bal gil yl pe uw