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DB00948 - Mezlocillin


Identification
Name Mezlocillin
Accession Number DB00948 (APRD01113)
Type small molecule
Description Semisynthetic ampicillin-derived acylureido penicillin. It has been proposed for infections with certain anaerobes and may be useful in inner ear, bile, and CNS infections. [PubChem]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 539.582
Groups approved
Monoisotopic Weight 539.114454181
Pharmacology
Indication Used to treat serious gram–negative infections of the lungs, urinary tract, and skin.
Mechanism of action By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, mezlocillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that mezlocillin interferes with an autolysin inhibitor.
Absorption Not Available
Protein binding 16-59%
Biotransformation Unlike many other penicillins, mezlocillin is either extensively metabolized or is subject to biliary excretion, as only about 50% of the dose was accounted for in normal urine.
Route of elimination Not Available
Toxicity Symptoms of overdose include rash, fever, chills, and peeling skin.
Affected organisms
  • Enteric bacteria and other eubacteria
Interactions
Drug Interactions
Drug Mechanism of interaction
Demeclocycline Possible antagonism of action
Doxycycline Possible antagonism of action
Ethinyl Estradiol This anti-infectious agent could decrease the effect of the oral contraceptive
Methotrexate The penicillin increases the effect and toxicity of methotrexate
Minocycline Possible antagonism of action
Tetracycline Possible antagonism of action
Food Interactions Not Available

Targets


Penicillin-binding proteins 1A/1B
Name Penicillin-binding proteins 1A/1B
Gene Name pbpA
Pharmacological action yes
Actions inhibitor
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Lei Y, Li JT: [Affinity of penicillin-binding proteins of Escherichia coli K-12 for furbenicillin and other beta-lactam antibiotics] Zhongguo Yao Li Xue Bao. 1989 Mar;10(2):177-80. - Pubmed
DTHybrid score 0.7972
Penicillin-binding protein 3
Name Penicillin-binding protein 3
Gene Name pbp3
Pharmacological action yes
Actions inhibitor
References
  • Lei Y, Li JT: [Affinity of penicillin-binding proteins of Escherichia coli K-12 for furbenicillin and other beta-lactam antibiotics] Zhongguo Yao Li Xue Bao. 1989 Mar;10(2):177-80. - Pubmed
  • Drugeon HB, Caillon J, Moinard D, Juvin ME, Pirault JL: [Bactericidal effect of piperacillin alone and combined] Presse Med. 1986 Dec 20;15(46):2297-302. - Pubmed
  • McCloskey RV, LeFrock JL, Smith BR, Aronoff GR: Microbiology, pharmacology, and clinical use of mezlocillin sodium. Pharmacotherapy. 1982 Nov-Dec;2(6):300-12. - Pubmed
DTHybrid score 0.0322
Penicillin-binding protein 2
Name Penicillin-binding protein 2
Gene Name mrdA
Pharmacological action unknown
Actions inhibitor
References
  • Lei Y, Li JT: [Affinity of penicillin-binding proteins of Escherichia coli K-12 for furbenicillin and other beta-lactam antibiotics] Zhongguo Yao Li Xue Bao. 1989 Mar;10(2):177-80. - Pubmed
DTHybrid score 0.0237

Predictions


Id Partner name Gene Name Score
1974 Oligopeptide transporter, kidney isoform SLC15A2 0.1282
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.1219
543 Penicillin-binding protein 1B mrcB 0.1186
6186 Penicillin-binding protein 1B ponB 0.1186
6822 Penicillin-binding protein 1b pbp1b 0.1186
6844 Penicillin-binding protein 1b pbp1b 0.1186
645 Penicillin-binding protein 1A mrcA 0.1167
5805 Penicillin-binding protein 1A ponA 0.1167
6185 Penicillin-binding protein 1A mrcA 0.1167
6799 Penicillin-binding protein 1A pbpA 0.1167
819 Penicillin-binding protein 4 dacB 0.0669
1729 Solute carrier family 22 member 6 SLC22A6 0.06
118 Organic cation/carnitine transporter 2 SLC22A5 0.0442
332 Beta-lactamase blaZ 0.0434
2478 Beta-lactamase ampC 0.0434
2613 Beta-lactamase ampC 0.0434
2635 Beta-lactamase ampC 0.0434
2700 Beta-lactamase penP 0.0434
5445 Beta-lactamase blaB 0.0434
6019 Beta-lactamase SHV-7 0.0434
6701 Beta-lactamase cphA 0.0434
867 Penicillin-binding protein 3 pbpC 0.0322
6119 Penicillin-binding protein 3 pbp3 0.0322
7157 Penicillin-binding protein 3 LMHCC_2184 0.0322
7162 Penicillin-binding protein 3 pbpB 0.0322
7172 Penicillin-binding protein 3 pbp3 0.0322
6184 D-alanyl-D-alanine carboxypeptidase dacC dacC 0.0305
587 Serum albumin ALB 0.0298
1024 Solute carrier family 22 member 11 SLC22A11 0.026
1 Peptidoglycan synthetase ftsI ftsI 0.026
4155 Peptidoglycan synthetase ftsI ftsI 0.026
115 Penicillin-binding protein 2 mrdA 0.0237
6118 Penicillin-binding protein 2 penA 0.0237
6187 Penicillin-binding protein 2 pbpA 0.0237
6686 Penicillin-binding protein 2 pbp2 0.0237
6939 Penicillin-binding protein 2 mrdA 0.0237
7163 Penicillin-binding protein 2 pbpA 0.0237
6142 Solute carrier family 22 member 8 SLC22A8 0.0222
1198 Serum paraoxonase/arylesterase 1 PON1 0.0183
6223 Penicillin-binding protein 1C pbpC 0.0183
6113 MecA PBP2' (penicillin binding protein 2') mecA 0.0182
2385 Penicillin acylase Not Available 0.0166
6067 Penicillin binding protein 2a mecA 0.0143
4512 Cytochrome P450 3A4 CYP3A4 0.014
1757 Myeloperoxidase MPO 0.0139
159 Penicillin-binding protein 2B penA 0.0126
6121 Penicillin-binding protein 2B penA 0.0126
4252 Penicillin-binding protein 5 dacA 0.0117
3760 Penicillin-binding protein 5 precursor dacA 0.0112
1405 Thiopurine S-methyltransferase TPMT 0.0108
6143 Solute carrier family 22 member 7 SLC22A7 0.0098
2164 Multidrug resistance-associated protein 4 ABCC4 0.0073
6016 Cytochrome P450 2C19 CYP2C19 0.0067
2461 D-alanyl-D-alanine carboxypeptidase Not Available 0.0045
5756 D-alanyl-D-alanine carboxypeptidase dac 0.0045
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