UNIVERSITI MALAYA UNIVERSITY F MALAYA PEPERIKSAAN IJAZA SARJANA MUDA SAINS EXAMINATIN FR TE DEGREE F BACELR F SCIENCE SESI AKADEMIK 2015/2016 : SEMESTER 2 ACADEMIC SESSIN 2015/2016 : SEMESTER 2 SCES2323 : KIMIA UBATAN MEDICINAL CEMISTRY Jun 2016 June 2016 Masa : 2 jam Time : 2 hours ARAAN KEPADA CALN : INSTRUCTINS T CANDIDATES : Jawab SEMUA soalan. Answer ALL questions. (Kertas soalan ini mengandungi 7 soalan dalam 9 halaman yang dicetak) (This question paper consists of 7 questions on 9 printed pages)
1. Terangkan yang berikut Explain the following (a) Dadah yang bertindak ke atas lipid dan berikan satu contoh dan struktur kimianya Drug acting on lipid and give one example and the chemical structure (b) Kesepadanan terdorong dan tapak aktif. Induce fit and active site. (c) Perencat berbalik dan adakah penisilin perencat berbalik atau perencat tidak berbalik. Terangkan. Reversible inhibitors and is penicillin a reversible or irreversible inhibitor. Explain. (d) Keselektifan enzim dan mengapa ia penting untuk mencari dadah yang enzim dan iso enzim terpilih? Enzyme selectivity and why is it important to find drugs that are enzyme and iso enzyme selective? (e) Dadah yang bertindak ke atas DNA; pemotong rantai atau agen pengalkilan. Terangkan dan berikan salah satu contoh. Drugs acting on DNA; chain cutter or alkylating agent. Explain and give example of either one. (f) Apa itu farmakokinetik dan terangkan empat faktor utama yang dipertimbangkan dalam kajian farmakokinetik dadah. What is pharmacokinetic and describe the four main factors to be considered in the pharmacokinetic studies of a drug. 2/9
2. Cadangkan sekurang-kurangnya 6 laluan metabolisma bagi sebatian berikut, derivatif quinidin, yang melibatkan tindak balas fasa 1 dan fasa 2. Terangkan jawapan anda. Suggest at least 6 metabolism pathway of the following compound, a quinidine derivative, which includes phase 1 and phase 2 reaction. Explain your answer. (12 markah/marks) Derivatif quinidin Quinidine derivative 3. Apakah tindak balas fasa 1 dan fasa 2 dalam metabolisma dadah. What are phase 1 and phase 2 reactions in drug metabolism? (4 markah/marks) 4. Apakah kepentingan dadah untuk menjalani metabolisma? Apa yang akan berlaku jika kadar metabolisma sangat rendah bagi sesuatu dadah? 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) 3/9
5. Pewarnaan Gram merupakan kaedah pewarnaan yang penting untuk membezakan di antara bakteria Gram-positif dan Gram-negatif. The Gram staining is the most important staining procedure to differentiate between Grampositive and Gram-negative bacteria. (i) Jelaskan perbezaan struktur dinding cell di antara bakteria Gram-positif dan Gram-negatif. Explain the difference in the cell wall structure between Gram- positive and Gramnegative bacteria. (2 markah/marks) (ii) uraikan prinsip bagi teknik Pewarnaan Gram. Describe the principle of Gram staining technique. (6 markah/marks) (iii) Mengapa pewarnaan bakteria Gram-positif berwarna ungu? Why do Gram-positive bacteria give purple stain? (2 markah/marks) 6. Penisilin G adalah antibiotik pertama untuk melawan jangkitan. Struktur bagi antibiotik ini adalah seperti berikut: Penicillin G is the first antibiotic used to fight infections. The structure of this antibiotic is as follows: N N S Me Me C 2 Penisilin G Penicilin G (i) Nyatakan selektiviti penisilin G terhadap sel bakteria. State the selectivity of penicillin G against bacterial cells. (1 markah/marks) 4/9
(ii) Tunjukkan mekanisme tindakan penisilin G dalam mencegah pertumbuhan bakteria. Show the mechanism of action of penicillin G in preventing the growth of bacteria. (iii) Jelaskan mengapa penisilin G kurang diserap jika diambil secara oral. Explain why Penicilin G is poorly absorbed orally. (7 markah/marks) (iv) Cadangkan satu daripada analog penisilin yang terbukti berjaya untuk mengatasi masalah yang dinyatakan di (iii). uraikan jawapan anda. Suggest one of penicillin analogues which is successful in tackling the problems stated in (iii). Explain your answer. (v) Bincangkan dua kesan preskripsi berlebihan bagi penisilin ke atas manusia. Discuss two effects of over prescription of penicillin on humans. (2 markah/marks) 7. Berikut adalah struktur bagi morfina dan analognya. The following are the structure of morphine and its analogues. Ac NMe Ac NMe Ac NMe Morfina Morphine Analog 1 Analogue 1 Analog 2 Analogue 2 (i) Bincangkan bahagian pada molekul morfina yang penting untuk aktiviti analgesik. Discuss which parts of the morphine molecule that are important for analgesic activity. (6 markah/marks) 5/9
(ii) Lukiskan imej cermin bagi morfina. Nyatakan aktiviti analgesik bagi sebatian ini. Draw the mirror image of morphine. State the analgesic activity for this compound. (3 markah/marks) (iii) Susunkan aktiviti analgesik bagi morfina dan analongnya dalam turutan menaik. Terangkan jawapan anda. Arrange the potency of morphine and its analogues in increasing analgesic activity. Explain your answer. (8 markah/marks) (iv) Terdapat tiga jenis reseptor analgesik untuk morfina: μ, κ dan δ. Jelaskan aktiviti berkaitan dengan salah SATU dari reseptor ini. There are three types of analgesic receptor which are activated by morphine: μ, κ and δ. Explain the activities related to NE of these reseptors. (3 markah/marks) 6/9
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
Amino asid dengan kumpulan sisi hidrofilik. Amino acids with hydrophilic side groups. 8/9
TAMAT END 9/9