Antidepressant-like Activity of 2-Pyrazoline Derivatives

Abstract

Antidepresan benzeri etkili 2-pirazolin türevleriAmaç: Yaygın, kronik ve tekrarlama riski olan psikiyatrik bir hastalık olarak depresyon, farklı sistemleri etkileyebilen semptomlar bütünüyle karakterize edilir. Patogenezinde rol oynayan çok farklı sistemlerin olması ve tedaviye verilen yanıtta görülen farklar, ilaç tedavisiyle tam bir iyileşme sağlanmasını engelleyerek yeni tedavi seçeneklerinin keşfedilmesi için yapılan çalışmaları hızlandırmaktadır. Daha önce birçok araştırmada pirazolin türevlerinin antidepresan ajan olarak tedavi potansiyeline sahip oldukları gösterilmiştir. Bu çalışmada ise bir seri yeni 2-pirazolin türevlerinin antidepresan benzeri etki profillerinin aydınlatılması amaçlanmıştır. Yöntem: Antidepresan benzeri aktivite Balb/C farelerde kuyruktan asma testi ve bu testte etkili olduğu tespit edilen maddeler için zorunlu yüzme testi kullanılarak değerlendirilmiştir. Her iki testte de antidepresan benzeri etkinin göstergesi, her bir hayvan için toplam hareketsiz kalma süresi olarak kabul edilmiştir. Bulgular: 3d ve 3e kodlu test bileşiklerinin antidepresan benzeri etkili olduğu belirlenmiş ve uygulanan her iki testte de referans ilaç imipramin grubunda gözlendiği gibi hareketsiz kalma sürelerinde kısalma gözlenmiştir. Ayrıca bileşikler farelerde lokomotor aktiviteyi etkilememiştir. Sonuç: Sonuçlarımız, 2-pirazolin türevi olan 3d ve 3e'nin depresyon tedavisinde yeni aday bileşiklerin tasarımı için potansiyel test maddeleri olduğunu göstermektedir. Anahtar sözcükler: Antidepresan benzeri aktivite, 2-pirazolin türevleri, zorunlu yüzme testi, kuyruktan asma testi ABS TRACT Antidepressant-like activity of 2-pyrazoline derivativesObjective: Depression is a common chronic recurrent psychiatric disorder, characterised by clusters of symptoms affecting many different systems. Due to complexity of the pathogenesis and differences in response to treatment, current therapies are incapable of providing an exact recovery, leading to attempts to investigate new treatment options. In many studies, it is shown that pyrazoline derivatives have the therapeutic potential as antidepressant agents. In this study, we aimed to investigate the antidepressant-like profile of a series of new 2-pyrazoline derivatives. Methods: Antidepressant-like activity was evaluated by using tail suspension test, which was followed by forced swim test for those compounds found effective in tail suspension test in Balb/c mice. The behavioural parameter observed in both tests was immobility period, which is an indicative of antidepressant-like effect. Results: Test compounds 3d and 3e were effective and a significant reduction in immobility time was observed when compared to results of imipramin, as the reference drug. Additionally, these two compounds did not alter the locomotor activity in mice. Conclusion:Our results indicate that two 2-pyrazoline derivatives, 3d and 3e, are potential compounds for use in designing of new candidates for the treatment of depression.

Microwave‐assisted Synthesis and Molecular Docking Study of Heteroaromatic Chalcone Derivatives as Potential Antibacterial Agents

“…It has a distinctive open chain flavonoid with two aromatic rings and three carbon atoms. Chalcone is a stable intermediate 2 for the synthesis of various heterocyclic compounds such as isoxazole, 3 pyrazoline, 4 epoxide, 5 thiazine, 6 indazole, 7 and pyrimidine 8 valuable in pharmaceutical industries 9 . A recent study disclosed a series of heterocyclic chalcones especially pyrazoline 10 derivatives with remarkable biological properties such as antioxidant, 11 antibacterial, 12 antidepressant, 13 anticancer, 14 antipyretic, 15 antimalarial, 16 antitubercular 17 as well as non‐biological applications in solar dyes, chemosensors, 18 photo‐conductors, 19 and optoelectronic devices 20 .…”

Pyrazoline as a medicinal scaffold

“…Pyrazole exhibits various biological activities and also has a potent medicinal scaffold 5 . Pyrazoline and its derivatives are having an antibacterial 6 , antimicrobial 7 , anti-inflammatory 8 , antioxidant 9 , antidiabetic 10 , anticancer 11 , antifungal 12 , antidepressant 13 , anticonvulsant 14 , analgesic 15 , and monoamine oxidases (MAOs) 16 .…”

“…K. Kaymakcıoğlu, S. Gumru, N. Beyhan, F. Aricioglu investigated a series of new 2-pyrazoline derivatives and activity was evaluated by using tail suspension test, Compounds 3d and 3e were effective and a significant reduction in immobility time was observed as compared to results of imipramine, as the reference standard drug. Compounds 3d and 3e remarked the potential for the treatment of depression33 .Anti-convulsant activityAhsan synthesized 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide and assayed the anticonvulsant activity and neuroprotection according to Antiepileptic Drug Development Programme protocol. Compound 4b showed neuroprotection activity with…”

Synthesis and Characterization of Some New Pyrazoline and Isoxazoline Derivatives as Antibacterial Agents

“…Pyrazolines can be effectively utilized as antibacterial, antifungal, antiviral, anticancer, anti-parasitic, antitubercular, antidepressant and insecticidal agents and considerable attention has been given to this class [9][10][11][12][13][14][15]. In addition, pyrazolines have played a crucial part in the development of theory in heterocyclic chemistry and also used extensively in organic synthesis [16][17].…”