POTANSİYEL FAAH İNHİBİTÖRÜ OLARAK BAZI ARİLHİDRAZON TÜREVİ BİLEŞİKLERİN TASARIMI VE SENTEZİ

Amaç: FAAH enziminin inhibisyonu amacıyla bir seri arilhidrazon türevi bileşiğin tasarımı, sentezi ve enzim aktif bölgesinde olası etkileşimlerinin incelenmesidir.

DESIGN AND SYNTHESIS OF SOME ARYLHYDRAZONE DERIVATIVES AS POTENTIAL FAAH INHIBITORS

Objective: The aim was to design, synthesis and investigation of possible interactions in the enzyme active site of a series of arylhydrazone derivatives for the inhibition of the FAAH enzyme.”

___

  • 1. Van Egmond, N., Straub, V.M., van der Stelt, M. (2021). Targeting Endocannabinoid Signaling: FAAH and MAG Lipase Inhibitors. Annual Review of Pharmacology and Toxicology, 61, 441-463. [CrossRef]
  • 2. Mechoulam, R., Parker, L. A. (2013). The Endocannabinoid System and the Annual Review of Psychology, 64(1), 21-47. [CrossRef]
  • 3. Lutz, B., Marsicano, G., Maldonado, R., Hillard, C.J. (2015). The endocannabinoid system in guarding against fear, anxiety and stress. Nature Reviews Neuroscience, 16(12), 705-718. [CrossRef]
  • 4. Tuo, W., Leleu-Chavain, N., Spencer, J., Sansook, S., Millet, R., Chavatte, P. (2017). Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors. Journal of Medicinal Chemistry, 60(1), 4-46. [CrossRef]
  • 5. Sachs, J., McGlade, E., Yurgelun-Todd, D. (2015). Safety and Toxicology of Cannabinoids. Neurotherapeutics, 12(4), 735-746. [CrossRef]
  • 6. Bajaj, S., Jain, S., Vyas, P., Bawa, S., Vohora, D. (2021). The role of endocannabinoid pathway in the neuropathology of Alzheimer's disease: Can the inhibitors of MAGL and FAAH prove to be potential therapeutic targets against the cognitive impairment associated with Alzheimer's disease? Brain Research Bulletin, 174, 305-322. [CrossRef]
  • 7. Bonifácio, M.J., Sousa, F., Aires, C., Loureiro, A.I., Fernandes-Lopes, C., Pires, N.M., Palma, P.N., Moser, P., Soares-da-Silva, P. (2020). Preclinical pharmacological evaluation of the fatty acid amide hydrolase inhibitor BIA 10-2474. British Journal of Pharmacology, 177(9), 2123-2142. [CrossRef]
  • 8. Ahn, K., Smith, S.E., Liimatta, M.B., Beidler, D., Sadagopan, N., Dudley, D.T., Young, T., Wren, P., Zhang, Y., Swaney, S., Van Becelaere, K., Blankman, J.L., Nomura, D.K., Bhattachar, S.N., Stiff, C., Nomanbhoy, T.K., Weerapana, E., Johnson, D.S., Cravatt, B.F. (2011). Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain. The Journal of Pharmacology and Experimental Therapeutics, 338(1), 114-124. [CrossRef]
  • 9. Ahn, K., Johnson, D.S., Mileni, M., Beidler, D., Long, J.Z., McKinney, M.K., Weerapana, E., Sadagopan, N., Liimatta, M., Smith, S. E., Lazerwith, S., Stiff, C., Kamtekar, S., Bhattacharya, K., Zhang, Y., Swaney, S., Van Becelaere, K., Stevens, R.C., Cravatt, B.F. (2009). Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chemistry & Biology, 16(4), 411-420. [CrossRef]
  • 10. Rocha, J.F., Santos, A., Gama, H., Moser, P., Falcao, A., Pressman, P., Wallace Hayes, A., Soares-da-Silva, P. (2022). Safety, Tolerability, and Pharmacokinetics of FAAH Inhibitor BIA 10-2474: A Double-Blind, Randomized, Placebo-Controlled Study in Healthy Volunteers. Clinical Pharmacology & Therapeutics, 111(2), 391-403. [CrossRef]
  • 11. Tripathi, R.K.P. (2020). A perspective review on fatty acid amide hydrolase (FAAH) inhibitors as potential therapeutic agents. European Journal of Medicinal Chemistry, 188, 111953. [CrossRef]
  • 12. Fazio, D., Criscuolo, E., Piccoli, A., Barboni, B., Fezza, F., Maccarrone, M. (2020). Advances in the discovery of fatty acid amide hydrolase inhibitors: what does the future hold? Expert Opinion on Drug Discovery, 15(7), 765-778. [CrossRef]
  • 13. Shang, Y., Hao, Q., Jiang, K., He, M., Wang, J. (2020). Discovery of heterocyclic carbohydrazide derivatives as novel selective fatty acid amide hydrolase inhibitors: design, synthesis and anti-neuroinflammatory evaluation. Bioorganic Medicinal Chemistry Letters, 30(10), 127118. [CrossRef]
  • 14. Jaiswal, S., Ayyannan, S.R. (2022). Discovery of Isatin-Based Carbohydrazones as Potential Dual Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase. ChemMedChem, 17(1), e202100559. [CrossRef]
  • 15. Freitas, R., Barbosa, J.M.C., Bernardino, P., Sueth-Santiago, V., Wardell, S., Wardell, J.L., Decote-Ricardo, D., Melo, T. G., da Silva, E.F., Salomao, K., Fraga, C.A.M. (2020). Synthesis and trypanocidal activity of novel pyridinyl-1,3,4-thiadiazole derivatives. Biomedicine & Pharmacotherapy, 127, 110162. [CrossRef]
  • 16. Fugard, A.J., Thompson, B.K., Slawin, A.M., Taylor, J.E., Smith, A.D. (2015). Organocatalytic Synthesis of Fused Bicyclic 2,3-Dihydro-1,3,4-oxadiazoles through an Intramolecular Cascade Cyclization. Organic Letters, 17(23), 5824-5827. [CrossRef]
  • 17. Sarıgöl, D., Yüksel, D., Okay, G., Uzgören-Baran, A. (2015). Synthesis and structural studies of acyl hydrazone derivatives having tetrahydrocarbazole moiety. Journal of Molecular Structure, 1086, 146-152. [CrossRef]
  • 18. Syakaev, V.V., Podyachev, S.N., Buzykin, B.I., Latypov, S.K., Habicher, W.D., Konovalov, A.I. (2006). NMR study of conformation and isomerization of aryl- and heteroarylaldehyde 4-tert-butylphenoxyacetylhydrazones. Journal of Molecular Structure, 788(1-3), 55-62. [CrossRef]
  • 19. Alp, A.S., Kilcigil, G., Ozdamar, E.D., Coban, T., Eke, B. (2005). Synthesis and evaluation of antioxidant activities of novel 1,3,4-oxadiazole and imine containing 1H-benzimidazoles. Turkish Journal of Chemistry, 39, 42-53. [CrossRef]
  • 20. Munir, R., Javid, N., Zia-Ur-Rehman, M., Zaheer, M., Huma, R., Roohi, A., Athar, M.M. (2021). Synthesis of Novel N-Acylhydrazones and Their C-N/N-N Bond Conformational Characterization by NMR Spectroscopy. Molecules, 26(16). [CrossRef]
Ankara Üniversitesi Eczacılık Fakültesi Dergisi-Cover
  • ISSN: 1015-3918
  • Yayın Aralığı: Yılda 3 Sayı
  • Başlangıç: 2016
  • Yayıncı: Ankara Üniversitesi Eczacılık Fakültesi
Sayıdaki Diğer Makaleler

REBOKSETİN’İN DİYABETİK SIÇANLARDA BOZULMUŞ DAVRANIŞ PARAMETRELERİ ÜZERİNDEKİ YARARLI ETKİLERİ

Nazlı TURAN YÜCEL, Ümmühan KANDEMİR, Umut İrfan ÜÇEL, Özgür Devrim CAN, Ümide DEMİR ÖZKAY

ENTEGRE BİYOİNFORMATİK ANALİZ İLE KRONİK LENFOSİTİK LÖSEMİDE HEDEF GENLERİN VE YOLAKLARIN BELİRLENMESİ

Buket ALTINOK GÜNEŞ

CLINOPODIUM PAMPHYLICUM SUBSP. DAVISII (CONTANDR. & QUÉZEL) GOVAERTS TOPRAK ÜSTÜ KISIMLARININ ANTİOKSİDAN, ENZİM İNHİBİSYON POTANSİYELİ VE FENOLİK PROFİLİNİN İNCELENMESİ

Nuraniye ERUYGUR, Fatma AYAZ

MOLEKÜLER YERLEŞTİRME YÖNTEMİYLE ZERUMBONUN EGFR TİROZİN KİNAZ İNHİBİTÖRÜ OLARAK DEĞERLENDİRİLMESİ

Dilek YONAR, Burcu BABA, Arzu KARAYEL

ANTİVİRAL İLAÇLARIN HASTANE ENFEKSİYON ETKENİ PSEUDOMONAS AERUGINOSA ÜZERİNDE SİNERJİSTİK ETKİSİNİN ARAŞTIRILMASI

Şükran ÖZTÜRK

ACUTODESMUS DIMORPHUS (TURPIN) P.M. TSARENKO (SCENEDESMACEAE, CHLOROPHYTA)' NIN KİMYASAL BİLEŞİMİ VE ANTİBAKTERİYEL AKTİVİTESİNİN İN VİTRO ANALİZİ

Eldrin ARGUELLES

POTANSİYEL FAAH İNHİBİTÖRÜ OLARAK BAZI ARİLHİDRAZON TÜREVİ BİLEŞİKLERİN TASARIMI VE SENTEZİ

Zehra Tuğçe GÜR MAZ, Sümeyye TURANLI, H. Burak CALISKAN

KULLANILMIŞ RUJ VE MASKARALARDA MİKROBİYOLOJİK KONTAMİNASYONUNUN ARAŞTIRILMASI

Kübra YAZICI, Müjde ERYILMAZ

PROPOLİS EKSTRAKTI BİTKİSEL YAĞLARIN OKSİDATİF STABİLİTESİNİ İYİLEŞTİRMEK İÇİN DOĞAL BİR ANTİOKSİDAN OLARAK ÖNERİLEBİLİR

Ümit ERDOĞAN

FARKLI KLİNİK ÖRNEKLERDEN İZOLE EDİLMİŞ KLEBSIELLA PNEUMONIAE İZOLATLARININ ANTİBİYOTİK DİRENÇ PROFİLİNİN İNCELENMESİ: COVID-19 PANDEMİSİ SÜRECİNDEKİ BİR YILLIK VERİLER

Derya DOĞANAY, Müzeyyen AYDIN, İbrahim Serkan AVŞAR