Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation

Noor A. Waheed; Hashim J. Azeez; Faris T. Abachi

doi:doi:10.11648/j.jddmc.20160205.11

| Peer-Reviewed

Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation

Noor A. Waheed, Hashim J. Azeez, Faris T. Abachi

Published in Journal of Drug Design and Medicinal Chemistry (Volume 2, Issue 5)

Received: 27 August 2016 Accepted: 12 October 2016 Published: 14 October 2016

Views: Downloads:

Download PDF

Share This Article

Twitter
Linked In
Facebook

Abstract

The present work describes the preparation and evaluation of an ophthalmic eye drops of antibacterial agent. The active ingredients (mereopenem, fluoroquinolones & 1,3,4 oxadiazole -2-thione derivatives) have been used in the formulation as eye drops with different doses as broad spectrum antibiotics to minimize the emergence of resistance lesion such as conjunctivitis or corneal ulcers. The experimental effectiveness of single or combination ophthalmic preparation as eye drop is well documented against different types of bacteria e.g. P.aeruginosa and other G^(+)ve & G^(-)ve bacteria. Other parameters pH, sterility, particulates and contents were calculated. All solutions are sterile, clear, isotonic and pH (5.1-6.3). These solutions didn’t cause any eye irritation in rabbits after daily application for four consecutive days. The potential clinical significant of combination therapy over monotherapy for different types of bacteria has been a controversial subjects for many years especially for ophthalmic purposes. The mechanism of carbapenem and fluoroquinolones are well known, while oxadiazole derivative is expected to inhibit p-amino benzoic acid. The uses of combination drug is thought to minimize the emergence of resistance, safe, potent and increase their synergistic activities.

Published in	Journal of Drug Design and Medicinal Chemistry (Volume 2, Issue 5)
DOI	10.11648/j.jddmc.20160205.11
Page(s)	47-50
Creative Commons	This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.
Copyright	Copyright © The Author(s), 2016. Published by Science Publishing Group

Keywords

Carbapenem, Ciprofloxacin, Olfloxacin, Moxifloxacin, Conjunctivitis, Corneal Ulcers

References

[1]	Christopher M. Brackett, Roberta J. Melander, Il Hwan An, Aparna Krishnamurthy, Richele J. Thompson, John Cavanagh, and Christian Melander (2014). Small-Molecule Suppression of β-Lactam Resistance in Multidrug-Resistant Gram-Negative Pathogens. J. Med. Chem., 57 (17), pp 7450–7458.
[2]	Jin-Woong Kim, Hyeong Beom Park, Bong Young Chung, Jong Baek Lee, Jung-Hyuck Cho, and Chang-Hyun Oh (2006). Synthesis and Antibacterial Activity of 1β-Methyl-2-[5-(α, β-disubstituted ethyl) pyrrolidin-3-ylthio] carbapenem Derivatives. Part II. Bull. Korean Chem. Soc., Vol. 27, No. 8.
[3]	Nagaraj; Chaluvaraju, K. C.; Niranjan, M. S.; Kiran, S. (2011). 1,3,4-Oxadiazole: A potent drug candidate with various pharmacological activities. Int. J. Pharm. Pharm. Sci., 3, 9–16.
[4]	Amir M; Javed SA; Kumar H. (2007). Synthesis of some 1,3,4oxadiazole derivatives as potential anti-inflammatory agents. Indian J Chem. 46B: 1014–9.
[5]	Krisztina M. Papp-Wallace; Andrea Endimiani; Magdalena A. Taracila; and Robert A. Bonomo. (2011). Carbapenems: Past, Present, and Future. Antimicrobial agents & Chemotherapy., 55 (11): 4943–4960.
[6]	Franski R. (2005). Biological activities of the compounds bearing 1,3,4-oxa(thia) diazole ring. Asian J Chem. 17:2063–75.
[7]	Moshirfar M; Chew J; Werner L; Meyer J. J; Hunter B; Stevens S; Jensen M; Kleinmann G; Mamalis N. (2008). Comparison of the effects of fourth-generation fluoroquinolones on corneal re-epithelialization in rabbit eyes: Graefes Arch. Clin. Exp. Ophthalmol.. 246(10): 1455-61.
[8]	Plech, T.; Wujec, M.; Kosikowska, U.; Malm, A.; Rajtar, B.; Polz-Dacewicz, M. (2013). Synthesis and in vitro activity of 1,2,4-triazole-ciprofloxacin hybrids against drug-susceptible and drug-resistant bacteria. Eur. J. Med. Chem. 60: 128–134.
[9]	K. Drlica; M. Malik; R. J. Kerns and X. Zhao. (2008). “Quinolone mediated bacterial death. Antimicrobial Agents and Chemotherapy, 52 (2): 385–392.
[10]	Tomoo SAGA; Keizo YAMAGUCHI. (2009). History of Antimicrobial Agents and Resistant Bacteria. JMAJ. 52(2): 103–108.

Cite This Article

Plain Text BibTeX RIS

APA Style

Noor A. Waheed, Hashim J. Azeez, Faris T. Abachi. (2016). Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation. Journal of Drug Design and Medicinal Chemistry, 2(5), 47-50. https://doi.org/10.11648/j.jddmc.20160205.11

Copy | Download

ACS Style

Noor A. Waheed; Hashim J. Azeez; Faris T. Abachi. Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation. J. Drug Des. Med. Chem. 2016, 2(5), 47-50. doi: 10.11648/j.jddmc.20160205.11

Copy | Download

AMA Style

Noor A. Waheed, Hashim J. Azeez, Faris T. Abachi. Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation. J Drug Des Med Chem. 2016;2(5):47-50. doi: 10.11648/j.jddmc.20160205.11

Copy | Download

@article{10.11648/j.jddmc.20160205.11,
  author = {Noor A. Waheed and Hashim J. Azeez and Faris T. Abachi},
  title = {Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation},
  journal = {Journal of Drug Design and Medicinal Chemistry},
  volume = {2},
  number = {5},
  pages = {47-50},
  doi = {10.11648/j.jddmc.20160205.11},
  url = {https://doi.org/10.11648/j.jddmc.20160205.11},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.jddmc.20160205.11},
  abstract = {The present work describes the preparation and evaluation of an ophthalmic eye drops of antibacterial agent. The active ingredients (mereopenem, fluoroquinolones & 1,3,4 oxadiazole -2-thione derivatives) have been used in the formulation as eye drops with different doses as broad spectrum antibiotics to minimize the emergence of resistance lesion such as conjunctivitis or corneal ulcers. The experimental effectiveness of single or combination ophthalmic preparation as eye drop is well documented against different types of bacteria e.g. P.aeruginosa and other G(+)ve & G(-)ve bacteria. Other parameters pH, sterility, particulates and contents were calculated. All solutions are sterile, clear, isotonic and pH (5.1-6.3). These solutions didn’t cause any eye irritation in rabbits after daily application for four consecutive days. The potential clinical significant of combination therapy over monotherapy for different types of bacteria has been a controversial subjects for many years especially for ophthalmic purposes. The mechanism of carbapenem and fluoroquinolones are well known, while oxadiazole derivative is expected to inhibit p-amino benzoic acid. The uses of combination drug is thought to minimize the emergence of resistance, safe, potent and increase their synergistic activities.},
 year = {2016}
}

Copy | Download

TY - JOUR
T1 - Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation
AU - Noor A. Waheed
AU - Hashim J. Azeez
AU - Faris T. Abachi
Y1 - 2016/10/14
PY - 2016
N1 - https://doi.org/10.11648/j.jddmc.20160205.11
DO - 10.11648/j.jddmc.20160205.11
T2 - Journal of Drug Design and Medicinal Chemistry
JF - Journal of Drug Design and Medicinal Chemistry
JO - Journal of Drug Design and Medicinal Chemistry
SP - 47
EP - 50
PB - Science Publishing Group
SN - 2472-3576
UR - https://doi.org/10.11648/j.jddmc.20160205.11
AB - The present work describes the preparation and evaluation of an ophthalmic eye drops of antibacterial agent. The active ingredients (mereopenem, fluoroquinolones & 1,3,4 oxadiazole -2-thione derivatives) have been used in the formulation as eye drops with different doses as broad spectrum antibiotics to minimize the emergence of resistance lesion such as conjunctivitis or corneal ulcers. The experimental effectiveness of single or combination ophthalmic preparation as eye drop is well documented against different types of bacteria e.g. P.aeruginosa and other G(+)ve & G(-)ve bacteria. Other parameters pH, sterility, particulates and contents were calculated. All solutions are sterile, clear, isotonic and pH (5.1-6.3). These solutions didn’t cause any eye irritation in rabbits after daily application for four consecutive days. The potential clinical significant of combination therapy over monotherapy for different types of bacteria has been a controversial subjects for many years especially for ophthalmic purposes. The mechanism of carbapenem and fluoroquinolones are well known, while oxadiazole derivative is expected to inhibit p-amino benzoic acid. The uses of combination drug is thought to minimize the emergence of resistance, safe, potent and increase their synergistic activities.
VL - 2
IS - 5
ER -

Copy | Download

Author Information

Noor A. Waheed

Department of Pharmaceutical Chemistry, College of Pharmacy, University of Mosul, Mosul, Iraq
Hashim J. Azeez

Department of Chemistry, College of Education, University of Salahddin, Erbil, Iraq
Faris T. Abachi

Department of Pharmaceutical Chemistry, College of Pharmacy, University of Mosul, Mosul, Iraq

Download PDF

Sections

Plain Text BibTeX RIS

APA Style

Noor A. Waheed, Hashim J. Azeez, Faris T. Abachi. (2016). Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation. Journal of Drug Design and Medicinal Chemistry, 2(5), 47-50. https://doi.org/10.11648/j.jddmc.20160205.11

Copy | Download

ACS Style

Noor A. Waheed; Hashim J. Azeez; Faris T. Abachi. Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation. J. Drug Des. Med. Chem. 2016, 2(5), 47-50. doi: 10.11648/j.jddmc.20160205.11

Copy | Download

AMA Style

Noor A. Waheed, Hashim J. Azeez, Faris T. Abachi. Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation. J Drug Des Med Chem. 2016;2(5):47-50. doi: 10.11648/j.jddmc.20160205.11

Copy | Download

@article{10.11648/j.jddmc.20160205.11,
  author = {Noor A. Waheed and Hashim J. Azeez and Faris T. Abachi},
  title = {Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation},
  journal = {Journal of Drug Design and Medicinal Chemistry},
  volume = {2},
  number = {5},
  pages = {47-50},
  doi = {10.11648/j.jddmc.20160205.11},
  url = {https://doi.org/10.11648/j.jddmc.20160205.11},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.jddmc.20160205.11},
  abstract = {The present work describes the preparation and evaluation of an ophthalmic eye drops of antibacterial agent. The active ingredients (mereopenem, fluoroquinolones & 1,3,4 oxadiazole -2-thione derivatives) have been used in the formulation as eye drops with different doses as broad spectrum antibiotics to minimize the emergence of resistance lesion such as conjunctivitis or corneal ulcers. The experimental effectiveness of single or combination ophthalmic preparation as eye drop is well documented against different types of bacteria e.g. P.aeruginosa and other G(+)ve & G(-)ve bacteria. Other parameters pH, sterility, particulates and contents were calculated. All solutions are sterile, clear, isotonic and pH (5.1-6.3). These solutions didn’t cause any eye irritation in rabbits after daily application for four consecutive days. The potential clinical significant of combination therapy over monotherapy for different types of bacteria has been a controversial subjects for many years especially for ophthalmic purposes. The mechanism of carbapenem and fluoroquinolones are well known, while oxadiazole derivative is expected to inhibit p-amino benzoic acid. The uses of combination drug is thought to minimize the emergence of resistance, safe, potent and increase their synergistic activities.},
 year = {2016}
}

Copy | Download