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]]>(3-{[(2′-{(5S,8S,9S,10R,13S)-15-{6-amino-2- [(1S)-3-amino-1-{[(2S)-2,3-diamino-3-oxopropyl]amino}-3-oxopropyl] -5-methylpyrimidin-4-yl}-13-[{[(2R,3S,4S,5S,6S)-3- {[(2R,3S,4S,5R,6R)-4-(carbamoyloxy)-3,5-dihydroxy-6- (hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy} -4,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy} (1H-imidazol-5-yl)methyl]-9-hydroxy-5-[(1R)-1-hydroxyethyl]-8,10-dimethyl-4,7,12,15-tetraoxo-3,6,11,14-tetraazapentadec-1-yl}-2,4′-bi-1,3-thiazol-4-yl)carbonyl]amino}propyl)(dimethyl)sulfonium.
Bleomycin falls under the category of antibiotic Antineoplastic cytotoxic drug. [1]
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 1415.6 g/mol |
2 | Appearance | Yellow to colorless powder.
Can appear bluish if copper content is high. |
3 | Melting point | 200-204 °C |
4 | Solubility | Freely soluble in water |
5 | Presence of ring | Bithiazole ring system |
i. Bleomycin chelates metal ions and produces pseudoenzymes.
ii. The pseudoenzymes so formed reacts with Oxygen to produce hydroxide and superoxides free radicals.
iii. Cleaving of DNA by the free radicals.[2]
i. Erythro-/3-hydroxy-L-histidine was prepared by condesation of 4-formylimidazole and N-pyruvylideneglycinatocopper(II) by modification of Ishido’s method.
ii. Methyl ester of the above formed compound was treated with MeOH-HCl.
iii. It is then treated with Tert-butyl S-(4,6-dimethylpyrimidine-2-yl)thiocarbonate.
iv. Formed compound will be treated with tosylchloride-Na2CO3 in dioxane water to give tosyl derivative.
v. The compound will be then treated with alpha-bromide of peracetyl in CH2Cl2.
vi. All the protective groups except the Boc-group will be removed by mild alkaline treatemnet.
vii. Then the compound will be treated with DNFB to give N-DNP derivative, then purified using chromatography technique.
viii. The Boc-group is deprotected using trifloroacetic acid and the compound is then coupled with Boc-PBA by DCC-HOBt method in DMF.
ix. The formed compound is then purified using chromatography technique to get the yield of 83%.
x. All the protective groups are removed by using 0.1N NaOH to get the Bleomycin.[3]
Bleomycins are used for the treatment of:
Q.1 The term ‘Blenoxan’ is associated with which drug?
a) Prednisolone
b) Ethinylestradiol
c) Toremifene
d) Bleomycin
Q.2 Disaccharide moiety in drug Bleomycin is responsible for?
a) Cellular uptake
b) Cell recognition
c) Cytotoxicity
d) All of the above
Q.3 Which amongst the following are the correct side effects of the drug Bleomycin?
I. Hair loss
II. Arrhythmias
III. Hypertension
IV. Nail banding
a) I, III & IV
b) II, III& IV
c) I & IV
d) I, II & III
Q.4 The microbes required for the synthesis of drug Bleomycin is?
a) Streptomyces caespitosus
b) Streptomyces verticillus
c) Streptomyces peucetius
d) None of these
Q.5 Which pairs of drug and its classification are true
I. | Bleomycin | Antibiotic antineoplastic drug |
II. | Fosfestrol | Glucocorticoids |
III. | Topotecan | Taxanes |
IV. | Etoposide | Camptothecin analogues |
a) I & IV only
b) I, II & III only
c) III & IV only
d) I only
Q.6 Correct physical form in which the drug Bleomycin is found?
a) Yellow to colorless powder
b) Bluish when copper concentration is present
c) Red crystalline powder
d) Both a) and b)
Q.7 Match the following with respect to ring systems of the drug
i. Bleomycin | A. Dihydroxyanthraquinone ring system |
ii. Mitoxantrone | B. Bithiazole ring system |
iii. Daunorubicin | C. Anthraquinone ring system |
iv. Vincristine | D. Quinoline ring system |
a) i-D, ii-B, iii-A, iv-C
b) i-B, ii-D, iii-A, iv-C
c) i-B, ii-C, iii-A, iv-D
d) i-B, ii-A, iii-C, iv-D
1-d
2-d
3-a
4-b
5-d
6-d
7-c
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