Design, synthesis, and SAR study of novel 4,5-dihydropyrazole-Thiazole derivatives with anti-inflammatory activities for the treatment of sepsis

Design and Synthesis of Carbothioamide/Carboxamide-Based Pyrazoline Analogs as Potential Anticancer Agents: Apoptosis, Molecular Docking, ADME Assay, and DNA Binding Studies

“…Heterocyclic analogs such as 1 H -pyrazole-1-carbothioamide/carboxamide are often used to design and develop physiologically active novel medications. 12 − 16 The pyrazoline core showed the potential anticancer activity 17 − 21 , and 1 H -pyrazole-1-carbothioamide types also exhibited biological activities such as antibacterial, 22 antifungal, 23 antiviral, 24 antimalarial, 25 antioxidant, 26 anti-inflammatory, 27 , 28 , and analgesic effects. 29 − 31 Anticancer drugs have DNA as their primary intracellular target.…”

“…Natural compounds have fewer N–N bonds than living creatures because they are more difficult to form. Heterocyclic analogs such as 1 H -pyrazole-1-carbothioamide/carboxamide are often used to design and develop physiologically active novel medications. − The pyrazoline core showed the potential anticancer activity − , and 1 H -pyrazole-1-carbothioamide types also exhibited biological activities such as antibacterial, antifungal, antiviral, antimalarial, antioxidant, anti-inflammatory, , , and analgesic effects. − Anticancer drugs have DNA as their primary intracellular target. In the present era, researchers are learning about the interaction of medications with DNA, and they believe that this interaction is responsible for DNA damage produced by malignant tumor cells’ inability to proliferate quickly. , Medication and micro-molecules commonly employ noncovalent, intercalation, groove binding, and electrostatic binding to interact with DNA.…”

Alpha-Chymotrypsin Protects Against Acute Lung, Kidney, and Liver Injuries and Increases Survival in CLP-Induced Sepsis in Rats Through Inhibition of TLR4/NF-κB Pathway

“…56,57 Inhibition of cytokine synthesis was suggested as a strategy to increase survival during sepsis. 58,59 Following burn injury, signaling by IL-1β and IL-6 were proposed to play a critical role in the development of sepsis. 60 The study conducted by RaviKumar and colleagues 60 showed that a combination of chymotrypsin with trypsin (Chymoral Forte D. S. preparation) decreased the levels of serum IL-1β and IL-6.…”

Cu(OAc)2-catalyzed hydrazination of cyclopropanols and late-stage transformation to 4,5-dihydropyrazoles

“…8 In particular, 4,5-dihydropyrazoles have exhibited a wide range of pharmaceutical and agrochemical activities in recent reports; 9 for example, 4,5-dihydropyrazole derivatives 1 showed good inhibitory effect on the generation of NO and selective cytotoxic activity against tumor cell lines; 10 the 4,5-dihydropyrazolethiazole derivative 2 has anti-inflammatory bioactivity. 11 Cyclopropyl alcohols are highly reactive and can undergo various ring opening, expansion, and fragmentation reactions in the presence of metal catalysts because of their high ring strains. 12 In addition, cyclopropyl alcohols as synthetic intermediates have recently risen to prominence due to their facile preparation (from the Kulinkovich reaction or the Simmons-Smith reaction) and their unique reactivities as three-carbon synthons.…”

“…8 In particular, 4,5-dihydropyrazoles have exhibited a wide range of pharmaceutical and agrochemical activities in recent reports; 9 for example, 4,5-dihydropyrazole derivatives 1 showed good inhibitory effect on the generation of NO and selective cytotoxic activity against tumor cell lines; 10 the 4,5-dihydropyrazole-thiazole derivative 2 has anti-inflammatory bioactivity. 11…”