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Journals / Turkish Journal of Pharmaceutical Sciences / 2007 / Cilt: 4 - Sayı: 2

Analjezik ve antienflamatuvar ajan olarak 2-(5,6-difenil-3(2H)-piridazinon-2-il)asetamit ve 3-(5,6-difenil-3(2H)-piridazinon -2-il)propanamit türevlerinin sentezleri

Synthesis of 2-(5,6-diphenyl-3(2h)-pyridazinone-2- yl) acetamide and 3-(5,6-diphenly-3(2H)-pyridazinone-2-yl)propanamide derivatives as analgesic and anti-inflammatory agents

Deniz S. DOĞRUER
SERDAR ÜNLÜ
Erden BANOĞLU
M. Fethi ŞAHİN
Esra KÜPELİ
Pages
57–70
DOI
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

Inhibitory activity of the active compounds on cyclooxygenase isoforms was also investigated by using in vitro human “whole blood assay” and found that these derivatives did not exert their analgesic and anti-inflammatory activities through COX inhibition and other mechanisms might be involved.

📌 3 Key Takeaways

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Objective & Hypothesis:In this study, new sixteen 2-[5,6-diphenyl-3(2H)-pyridazinone-2-yl] acetamide and 3-[5,6-diphenyl-3(2H)-pyridazinone-2-yl] propanamide derivatives were synthesized and their in vivo analgesic and anti-inflammatory activities were tested in mice.
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Key Findings & Data:The compound 8e which is a propanamide derivative exhibited higher analgesic and anti-inflammatory activities than other synthesized compounds and did not cause any gastric lesions and bleeding in stomachs of tested animals.
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Conclusion & Impact:Inhibitory activity of the active compounds on cyclooxygenase isoforms was also investigated by using in vitro human “whole blood assay” and found that these derivatives did not exert their analgesic and anti-inflammatory activities through COX inhibition and other mechanisms might be involved.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Siklooksijenaz inhibitörleri · Analjezikler · Kimya

Abstract

In this study, new sixteen 2-[5,6-diphenyl-3(2H)-pyridazinone-2-yl] acetamide and 3-[5,6-diphenyl-3(2H)-pyridazinone-2-yl] propanamide derivatives were synthesized and their in vivo analgesic and anti-inflammatory activities were tested in mice. Propanamide derivatives were found more potent than acetamide derivatives in terms of anti-inflammatory activity. The compound 8e which is a propanamide derivative exhibited higher analgesic and anti-inflammatory activities than other synthesized compounds and did not cause any gastric lesions and bleeding in stomachs of tested animals. Inhibitory activity of the active compounds on cyclooxygenase isoforms was also investigated by using in vitro human “whole blood assay” and found that these derivatives did not exert their analgesic and anti-inflammatory activities through COX inhibition and other mechanisms might be involved.

Özet

Bu çalışmada, onaltı yeni 2-[5,6-difenil-3(2H)-piridazinon-2-il] asetamit ve 3-[5,6-difenil-3(2H)-piridazinon-2-il] propanamit türevleri sentez edilmiş ve bunların analjezik ve antienflamatuvar etkileri fareler üzerinde test edilmiştir.Propanamit türevleri antienflamatuvar etki bakımından asetamit türevlerinden daha güçlü bulunmuştur. Propanamit türevi olan bileşik 8e sentezi yapılan diğer bileşikler ile karşılaştırıldığında daha yüksek analjezik ve antienflamatuvar etki göstermiş ve test edilen hayvanlarda gastrik lezyon veya kanamaya neden olmamıştır. Aktif bileşiklerin siklooksijenaz izoformlarıüzerine inhibitör etkileri “in vitro insan tam kan” yöntemiyle araştırılmış ve bu bileşiklerin analjezik ve antienflamatuvar etkilerini COX inhibibisyonu aracılığıyla göstermedikleri, başka mekanızmaların etkili olabileceği bildirilmiştir

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Cite This Article

DOĞRUER, D. S., ÜNLÜ, S., BANOĞLU, E., ŞAHİN, M. F., KÜPELİ, E. (2007). Analjezik ve antienflamatuvar ajan olarak 2-(5,6-difenil-3(2H)-piridazinon-2-il)asetamit ve 3-(5,6-difenil-3(2H)-piridazinon -2-il)propanamit türevlerinin sentezleri. Turkish Journal of Pharmaceutical Sciences, Cilt: 4 - Sayı: 2, 57–70. https://ajindex.com/articles/403895

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