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FlashCards sobre get, criado por yousef mohamed em 10-06-2019.
yousef mohamed
FlashCards por yousef mohamed, atualizado more than 1 year ago
yousef mohamed
Criado por yousef mohamed aproximadamente 5 anos atrás
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Resumo de Recurso

Questão Responda
benzyl.penicillin penicillin G
phenoxy-methyl penicillin penicillin V
fused B-lactam + thiazolidine bicyclic structure Penicillin
6-APA 6-aminopenicillanic acid
4-Thia-1-azabicyclo [3,2,0] heptane 1- Penam
6-phenyl.acetamido-2,2-dimethyl-penam-3-carboxylic acid. penicillin G
(4-Thia-1-azabicyclo13.2.0] hept-2-ene) 7-one Penem
(1-Azabicyclo (3.2.0) hept-2-ene)-7-one Carbapenem
(5-Thla-1-azabicyclo. [4.2.0]oct-2-ene)-8-one Cefem
1-Azacyclobutan-4-one Monobactam
2,6-dimethoxy-benzamido penicillanic acid methicillin
5-thia-1-azabicyclo [4, 2,0] octanes Cephalosporins
B-lactam + dihydro.thiazine Cephalosporins
3,3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylate 4,4- dioxide. Sulbactam
(2S,5R,6R)-6-[(R)-2-amino-2-phenylacetamido ] -3,3 dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2 carboxylate. Ampicillin
Have weak activity comparable to 6- APA Clavulanic acid
fused B-Lactam + oxazolidine ring Oxapenems
contain one ring [azetidine Monobactams
pKa values between 6.0 and 9.0. Macrolide
2,3,6-trihydroxy -3- methoxy-3-C-methyl-L-ribo-hexose Cladinose
6-methyl ether of erythromycin Clarithromycin
prototype of a series of nitrogen-containing, 15-membered ring known as azalides. Azithromycin
2,2-Dichroro-N-[(IR,2R)-2-hydroxy-1- hydroxy-methyl-2-(4-nitrophenyl) ethyl acetamide. Chloramphenicol
1945 Tetracyclines
1960 1- First generation cephalosporins:
late 1970s 2- Second generation cephalosporins:
1980s 3- Third generation
oral bioavailability good, (40%) Azithromycin
Effective concentrations achieved in bone for staphylococcal osteomyelitis but not in cerebrospinal fluid for meningitis Clindamycin
below Pka 10.4 Sulfonamides
protect against, cure, streptococcal in mice Sulfonamides
aniline-substituted sulfanilamides
2. Prodrugs react to generate active sulfanilamides sulfasalazine, Prontosil
3. Non-aniline sulfonamides mafenide acetate
Synthesis: 1. Reaction p-nitrobenzenesulfonyl-chloride + amine  the intermediate + reduction leads directly sulifon-amide
a. Short-acting sulfonamides: 1. Sulfa-merazine, 2. sulfamethazine (sulfadimidine), 3. sulfa-methizole, 4. sulfa-pyridine, 5. sulfathiazole 6. sulfi-soxazole.
b. Intermediate-acting sulfonamides: 1. sulfa-diazine 2. sulfa-methoxazole, 3. sulfa-phenazole 4. sulfa-symazine
c-Long-acting sulfonamides: 1.sulfa-doxine 2. sulfa-methoxy-pyridazine 3. sulfa-moxole 4.sulfa-metomidine.
For: cholera, leprosy and malaria. c-Long-acting sulfonamides:
4-amino-N- (4,6-dimeth yl-2 - pyrimidinyl) benzene surfonamide. Sulfamethazine (sulfadimidine)
4-amino-N-(-2-pyrimidinyl) benzene sulfonamide. Sulfadiazine
4- amino-N- (5, 6-dimethoxy-4pyrimidinyl) benzene sulfonamide. Sulfadoxine
4-amino-N-(6-methoxypyridazin-3-yl) benzene sulfonamide Sulfa-methoxy-pyridazine
Intestinal sulfonamides 1. pthaly-sulfathiazole 2. Succinyl-sulfathiazole, 3. Sulfa-guanidine 4. Sulfa-salazine
2-hydroxy-5- [ [(4- [2pyridinyl.amino) sulfonyl]-phenyl] Azo] benzoic acid. Sulfasalazine (oral nonabsorbable
Urinary sulfonamides 1. Sulfa-cytine, 2.sulfadiazine, 3.sulfa-methoxine 4.sulfisoxazole. The preferred one is a. sulfacytine, b.sulfa-methizole c.sulfi-soxazole,
Ophthalmic sulfonamides: as sulfacetamide+ its sodium salt
Burn therapy sulfonamides: a. Mafenide (sulfa-mylon) b. silver sulfadiazine and c. sulfa-thiourea
4-amino-N-(3,4-dimethylisoxazol-5yl) benzene sulfonamide Sulfi-soxazole
N-[(4-aminophenyl) sulfonyl) acetamide Sulfacetamide
4- (Amino methyl) benzene sulfonamide. Mafenide
5- [ (3,4,5-trimethoxy phenyl) methyl] pyrimidine-2,4-diamine Trimethoprim
sulfamethoxazole- trimethoprim (Co-trimoxazole) (septazole, sutrim), to prevent resistance of bacteria to sulfa drugs. for acute or complicated or recurrent urinary tract infections / upper respiratory infections / pneumocystis pneumonia / toxoplasmosis / salmonella infections / prostatitis.
N'-alkylated-3-carboxypyrid-4-one ring Quinolones Antimicrobial
(1997-1999). Third generation: Sparfloxacin, Levofloxacin, Gatifloxacin and Moxifloxacin
(1965 First generation: Nalidixic acid
I-Ethyl-1,4-dihyro-7-methyl-4-oxo- 1,8-naphthyridine-3-carboxylic Nalidixic Acid:
1-Cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline-3-carboxylic acid Ciprofloxacin
(+/-) 6-Fluoro-7-piperazinyl quinolone with methyl substituted oxazine ring Ofloxacin
acute bacterial sinusitis chronic bronchitis Third Generation Quinolones
tri-fluoro.naphthyridine derivative with aza-bicyclo group at C-7 and formulated as hydrochloride or mesylate salt. Fourth Generation: Trovafloxacin
3- Alkyl substitution at position 1 is essential  di-fluoro-phenyl group may cause hepatotoxicity Trovafloxacin
4- Substitution C-5 with amino group improves both Gram +ve and Gram -ve.  This improved dependent on C-8 and is most active when substituent fluorine, Sparfloxacin
6- Addition of piperazine group at C-7 provides antipseudomonal activity.  Alkyl substitution of piperazine improves activity against gram +ve bacteria +  increase drug's half-life.  Lipophilic aza-bicyclo modification C-7 increases activity Gram +ve Sparfloxacin, Levofloxacin, Gatifloxacin and Moxifloxacin)
7- Addition second fluorine group at C-8 increases absorption and longer half-life & increases phototoxicity Lemofloxacin and Sparfloxacin).
Iso-nicotinic Acid Hydrazide, INH). Isoniazid
(+) N, N-bis-(1-hydroxy-2-butyl) ethylene-diamine Ethambutol
pyrazine-carboxamide Pyrazinamide (PZA)
2-Ethyl-thio-iso-nicotin-amide Ethionamide
fluoro.deoxy.uridine.monophosphate 5-Fluorocytosine (5-FC)
8S,9R-6 -Methoxy.cinchonane-9-ol Quinine
7-Chloro-4 { [ 4-(diethyl.amino)-1 methyl.butyl ) amino } quinoline. Chloroquine
7-Chloro-4 { { 3- (diethyl.amino.methyl) -4-hydroxy.phenyl] amino } quinolone amodiaquine
8- [ ( 4-Amino-1-methyl-butyl) amino ] -6-methoxy.quinoline. Primaquine
1-(4-chlorophenyl) -5- isopropyl.biguanide Biguanides, Proguanil (Chloroguanide): Cycloguanil pamoate
5- (4-Chlorophenyl) -6-ethyl-2,4 pyrimidine.diamine Pyrimethamine
2-14-(4,6-diamino-1, 3,5-triazin-2-yl-amino) phenyl-1,3,2-dithia.rsolane-4-methanol Melarsoprol: arsenic compound
Alpha.-Difluoromethylornithine, OR DFMO' Eflornithine (Ornidyl):
4-[5-nitrofurfurylidene)amino]-3 methylthiomorpholine1,1-dioxide 1- Nifurtimox
N-Benzyl-2-nitroimidazole-1-acetamide 2- Benzindazole:
2-(2-Methyl-5-nitroimidazolyl)ethanol Metronidazole
5,7-Di.iodo-8-hydroxy.quinoline Diodo.quinol
2-furoate ester of : 2,2-dichloro-4'-hydroxy-N-methyl.acetamide b- Di.chloro.acetamides: Di.loxanid furoate
5 -chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy. benzamide Niclosamide
N.N-diethyl -4-methyl-1-piperazine carboxamide. Diethylcarbamazine Citrate ( Hetrazan ) (nowadays only used)
S)-2,3,5,6-tetahydro-6-phenyl.imidazo-(2,1-b) thiazole hydrochloride b) Levamisole Hcl:
Mebendazole 5-benzoyl-IH-benzimidazole-2-yl) carbamic acid, methyl ester
2-(4-thiazolyl)-1H-benzimidazole Thiabendazole
E-1, 4, 5, 6- tetrahydro-1-methyl-2-[2-(2-thienyl) ethenyl-pyrimidine. Pyrantel pamoate (combantrin
Pyrantel pamoate (combantrin
2-cyclo.hexyl.carbonyl)-1,2,3,6,7,1.I.b-hexa.hydro-4H-pyrazino[2,1-a] iso.quinolin-4-one. Praziquantel (Biltricide):
Tri sod phosphono formate Foscarnet sodium (Foscavir)®
ethyl (3R,4R,5S)-4-acetamido-5-amino-3-(pentan-3-yloxy)-cyclohex-1-ene-1-carboxylate Oseltamivir
Bis (2-chloroethyl) methylamine HCl Mustine HCl= Mechlorethamine HCl (mustargen®)
4-[bis(2 chlorethyl) amino] benzenebutanoic acid Chlorambucil (Leukeran)®
2,4,6-Tris(aziridin-1-yl)-1,3,5-triazine Triethylene melamine (TEM)=tretamine
1,4-Bis(methanesulfonyloxy)butane Sulphonic acid esters: Busulfan (Busulfex®)
6-[(1-Methyl-4-nitro-1H-imidazol-5-yl)sulfanyl]-7H-purine Azathioprine (Imuran®)
5-Methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methanesulfinyl]-1H-benzimidazole Omeprazole (Omez ®)
N-Ethyl-N-(2-methylphenyl)but-2-enamide Crotamiton (Eurax®)
P-hydroxy benzoic acid derivatives Parabens

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