(Kertas soalan ini mengandungi 8 soalan dalam 9 halaman yang dicetak) (This question paper consists of 8 questions on 9 printed pages)
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1 UIVERITI MALAYA UIVERITY F MALAYA PEPERIKAA IJAZA ARJAA MUDA AI EXAMIATI FR TE DEGREE F BACELR F CIECE EI AKADEMIK 2014/2015 : EMETER 2 ACADEMIC EI 2014/2015 : EMETER 2 CE2323 : KIMIA UBATA MEDICIAL CEMITRY Jun 2015 June 2015 MAA : 2 jam TIME : 2 hours ARAA KEPADA CAL : ITRUCTI T CADIDATE : Jawab EMUA soalan. Answer ALL questions. (Kertas soalan ini mengandungi 8 soalan dalam 9 halaman yang dicetak) (This question paper consists of 8 questions on 9 printed pages)
2 1. Terangkan yang berikut Explain the following (i) Drug yang bertindak ke atas lipid. Berikan satu contoh dan struktur kimianya. Drug acting on lipid. Give one example with the chemical structure. (ii) Kepadanan terdorong dan tapak aktif. Induced fit and active site. (iii) Perencat berbalik dan adakah penisilin perencat berbalik atau perencat tidak berbalik. Terangkan. Reversible inhibitors and is penicillin a reversible or irreversible inhibitor. Explain. (iv) elektiviti enzim dan mengapa ia penting untuk mencari drug yang enzim dan iso enzim terpilih? Enzyme selectivity and why is it important to find drugs that are enzyme and iso enzyme selective? (v) Drug yang bertindak ke atas DA; pemotong rantai atau agen pengalkilan. Terangkan dan berikan salah satu contoh. Drugs acting on DA; chain cutter or alkylating agent. Explain and give example of either one. (vi) Apakah itu farmakokinetik? Terangkan empat faktor utama yang dipertimbangkan dalam kajian farmakokinetik drug. What is pharmacokinetic? Describe the four main factors to be considered in the pharmacokinetic studies of a drug. 2/9
3 2. Cadangkan sekurang-kurangnya 6 laluan metabolisme bagi sebatian berikut, terbitan quinidin, yang melibatkan tindak balas fasa 1 dan fasa 2. Terangkan jawapan anda, (sila lihat apendiks 2). uggest at least 6 metabolism pathways of the following compound, a quinidine derivative, which includes phase 1 and phase 2 reactions. Explain your answer, (refer to appendix 2). (12 markah/marks) Terbitan quinidin Quinidine derivative 3. Apakah tindak balas fasa 1 dan fasa 2 dalam metabolisme drug. What are phase 1 and phase 2 reactions in drug metabolism? (4 markah/marks) 4. Apakah kepentingan drug untuk menjalani metabolisme? Apa yang akan berlaku jika kadar metabolisme sangat rendah bagi sesuatu drug? Why is it important for drugs to undergo metabolism? What will happen if the rate of metabolism of a certain drug is very low? (4 markah/marks) 5. (a) Terangkan mana-mana dua (2) daripada terma-terma yang berikut: Explain any two (2) of the following terms: (i) Pro-drug Pro-drug 3/9
4 (ii) (iii) Perhubungan struktur-aktiviti tructure-activity relationship Bakteriostatik Bacteriostatic (6 markah/marks) (b) Bincangkan selektiviti agen anti-bakteria terhadap sel bakteria dan bukannya sel manusia. Explain the selectivity of anti-bacterial agents against bacterial cells and not human cells. (4 markah/marks) 6. Jelaskan mekanisme tindakan sulfonamida dalam menghalang pembentukan asid folik dalam sel bakteria dengan menggunakan persamaan kimia yang sesuai. eterusnya, nyatakan cara bagaimana bakteria dapat menghasilkan rintangan terhadap sulfonamida. Explain the mechanism of sulphonamides in inhibiting the formation of folic acid in bacteria cells by using suitable chemical equations. ubsequently, state how bacteria can acquire resistance towards sulphonamides. (6 markah/marks) 7. Tunjukkan langkah penyediaan drug yang berikut dengan menuliskan persamaan kimia bagi tindak balas yang terlibat. how the preparation steps for the following drugs by writing the chemical equations for all reactions involved. (a) C Ac 2 C C Ac 4/9
5 (b) 2 C 3 C 3 C 2 C 3 C 3 C (10 markah/marks) 8. (a) alah satu faktor yang mempengaruhi ciri analgesik adalah stereokimia drug. Bincang dan lakarkan gambarajah yang sesuai untuk menjelaskan faktor tersebut. eterusnya, berikan satu strategi untuk meningkatkan ciri analgesik. ne of the factor affecting the analgesic property is stereochemistry of the drug. Discuss and sketch a suitable drawing to explain that factor. ubsequently, state a strategy that can be used to improve the analgesic property. (6 markah/marks) (b) yatakan strategi yang digunakan untuk pembentukan analog morfina Q. Bincangkan kebaikan yang boleh diperolehi melalui strategi tersebut. Tunjukkan skema tindak balas bagi sintesisnya dari bahan pemula yang sesuai. tate the strategies used in the development of morphine analogue Q. Discuss the advantages of the strategies. how a reaction scheme for its synthesis from suitable precursor. Me Me Me 3 C 2 C 2 C Q (9 markah/marks) 5/9
6 (c) Bandingkan analog morfina X dan Y yang berikut. Berikan keaktifan analgesik dalam tertib menaik. Berikan penjelasan kepada jawapan anda. ekiranya (C 3 ) dalam X diubah kepada, ramalkan dan terangkan kesan ke atas aktiviti analgesik. Compare the following morphine analogues X and Y. Give the analgesic activity in ascending sequence. Explain on your answer. Deduce and explain the effect on analgesic activity if (C 3 ) in X is converted to. Ac C 3 Ac C 3 Ac C 3 X Y Z (9 markah/marks) 6/9
7 Appendiks 1 Appendix 1 Amino asid dengan kumpulan sisi di antara hidrofobik dan hidrofilik. Amino acids that are in between hydrophobic and hydrophilic side groups. Amino asid dengan kumpulan sisi hidrofobik. Amino acids with hydrophobic side groups. 7/9
8 Amino asid dengan kumpulan sisi hidrofilik. Amino acids with hydrophilic side groups. 8/9
9 Appendiks 2 Appendix 2 Molekul berkonjugat Conjugates molecules TAMAT ED 9/9
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