Tiyazol-fenilasetik asit bileşiklerinin dual antibakteriyel-COX enzim inhibitörleri olarak sentezleri
Amaç: Bu çalışmanın amacı inflamasyon ve enfeksiyon geçiren hastalara önerilebilecek çift etkili potansiyel ilaçlar sunmak olup bu bağlamda tiyazol fenilasetik asit türevlerinin antienflamatuvar ve antibakteriyal aktiviteleri araştırmaktır.
Synthesis of thiazole-phenylacetic acid compounds as dual antibacterial-COX enzymes inhibitors
Purpose: Present a new potential dual drug for patient suffering both inflammation and infection was aim of this study therefore investigation of anti-inflammatory and antimicrobial activity of new thiazole-phenylacetic acid compounds derivatives as a potential dual drug was carried out.
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- 1. Cekici A, Kantarcı A, Hastürk H, Dyke TEV.
Inflammatory and immune pathways in the
pathogenesis of periodontal disease. Peridontol.
2000. 2014;64:57-60.
- 2. Coussens LM, Werb Z. Inflammation and cancer.
Nature. 2002;420:860-7.
3. Amor S, Puentes F, Baker D, Valk P. Inflammation
in neurodegenerative diseases. Immunology.
2010;129:154-69.
- 4. Libby P. Inflammation and cardiovascular disease.
Am J Clin Nutr. 2006;83:456-60S.
- 5. Gordon S, Taylor PR. Monocyte and macrophage
heterogeneity. Nat Rev Immunol. 2005;5:953-64.
- 6. Medzhitov R. Inflammation 2010: new adventures of
an old flame. Cell. 2010;140:771-6.
- 7. Ricciotti E, FitzGerald GA. Prostaglandins and
inflammation. Arterioscler Thromb Vasc Biol.
2011;31:986-1000.
- 8. Ong CKS, Lirk P, Tan CH, Seymour RA. An
evidence-based update on nonsteroidal antiinflammatory
drugs. Clin Med Res. 2007;5:19-34.
- 9. Zaghi A, Arfaei S. Selective COX-2 Inhibitors: A
review of their structure-activity relationship. Iran J
Pharm Res. 2011;10:655-83.
- 10. Claria J. Cyclooxygenase-2 biolog. Curr Pharm Des.
2003;3:2177-90.
- 11. Bekhit AA, Abdel-Azeim T. Design, synthesis and
biological evaluation of some pyrazole derivatives as
anti-inflammatory-antimicrobial agents. Bioorg Med
Chem. 2004;12:1935–45.
- 12. Ahmadi F, Ghayahbashi MR, Sharifzadeh M,
Alipoiur E, Ostad SN, Vosooghi M, et al.. Synthesis
and evaluation of anti-inflammatory and analgesic
activities of new 1,2,4-triazole derivatives. Med
Chem. 2015;11:69-76.
- 13. Bekhit AA, El-Sayed OA. Aboulmagd E, Park JY.
Tetrazolo[1,5-a]quinoline as a potential promising
new scaffold for the synthesis of novel antiinflammatory
and antibacterial agents. Eur J Med
Chem. 2004;39:249-55.
- 14. Moneer AA, Mohammed KO, El-Nassan HB.
Synthesis of novel substituted thiourea and
benzimidazole derivatives containing a pyrazolone
ring as anti-inflammatory agents. Chem Biol Drug
Des. 2016;87:784-93.
- 15. Paramashivappa R, Phani Kumar P, Subba Rao PV,
Srinivasa Rao A. Design, synthesis and biological
evaluation of benzimidazole/benzothiazole and
benzoxazole derivatives as cyclooxygenase inhibitors.
Bioorg Med Chem Lett. 2003;13:657-60.
- 16. Eswaran S, Adhikari AV, Shetty NS. Synthesis and
antimicrobial activities of novel quinoline derivatives
carrying 1,2,4-triazole moiety. Eur J Med Chem.
2009;44:4637–47.
- 17. Bekhit AA, Ashour HM, Abdel Ghany YS, Bekhit
AD, Baraka A. Synthesis and biological evaluation of
some thiazolyl and thiadiazole derivatives of 1Hpyrazole
as anti-inflammatory antimicrobial agents.
Eur J Med Chem. 2008;43:456-63.
- 18. [K548]Cyclooxygenase-1(COX-1) Inhibitor
screening kit (Fluorometric)
http://www.biovision.com/cyclooxygenase-1-cox-1-
inhibitor-screening-kit-fluorometric.html (accessed
Feb 2017).
- 19. [K547]Cyclooxygenase-2 (COX-2) Fluorescent
Inhibitor Screening Kit (Fluorometric)
http://www.biovision.com/cox-2-inhibitorscreening-
kit-fluorometric.html (accessed Feb 2017).
- 20. Clinical and Laboratory Standards Institute. Methods
for Dilution Antimicrobial Susceptibility Tests for
Bacteria That Grow Aerobically; Approved
Standard-Ninth Edition. CLSI document M07-A9.
- 21. Sanchez-Borges M. Clinical management of
nonsteroidal anti-inflammatory drug hypersensitivity.
World Allergy Organ J. 2008;1:29-33.