Created by yousef mohamed
over 5 years ago
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Question | Answer |
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 |
Image:
1 (binary/octet-stream)
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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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