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Fibrinolytic Enzymes for Thrombolytic Therapy
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Swaroop S. Kumar, Sabu Abdulhameed
Anticoagulants like coumarin derivatives were discovered in 1939 by the identification of dicumarol from spoiled sweet clover hay which is a vitamin K antagonist by Link and Campbell (Stahmann et al., 1941). Further studies on coumarin derivatives led to the discovery of warfarin which was initially used as rodenticide and later approved for clinical use as anticoagulant. It was the first oral thrombin inhibitor and found useful in preventing embolic strokes (Aguilar and Hart, 2005). Limitations of these vitamin K antagonists were bleeding complications, interaction with food, necrosis, and hair loss (Dantas et al., 2004; Ansell et al., 2008; Pirmohamed, 2006). Even though other coumarin derivatives such as phenprocoumon and acenocoumarol also were used as anticoagulants, warfarine is the most common vitamin K antagonist in practice and remains as affordable in cardiovascular disease management.
The Trouble with Pests
Published in Gary S. Moore, Kathleen A. Bell, Living with the Earth, 2018
Gary S. Moore, Kathleen A. Bell
Although rodent control has been discussed earlier in the chapter, a more detailed discussion of the rodenticide warfarin is offered here. Warfarin is among the most widely used rodenticides because it is effective in small quantities, reasonably non-toxic to humans, and does not promote bait shyness because it is a slow-acting poison. Warfarin is a coumadin compound and therefore a vitamin K antagonist that inhibits prothrombin synthesis. Repeated dosing over several days causes an overall reduction in the blood level prothrombin, which is necessary for coagulation. The consequence of such dosing is internal hemorrhaging, blood in the sputum and stools, and externally visible hematomas. The animals ultimately bleed to death. Some populations of rats have developed a resistance to warfarin. Consequently, more powerful versions known as superwarfarin, with a potency up to 200 times that of warfarin, have been developed that are more effective against these resistant strains.53–55 Such compounds include brodifacoum, difethialone, and flupropadine. As might be expected, these compounds have much higher toxicity to humans than warfarin (Figure 6.26).54 Other multiple dose poisons effective in controlling rats include fumarin, PMP, and diphacinone.
Synthesis and cytotoxic activity of some novel benzocoumarin derivatives under solvent free conditions
Published in Green Chemistry Letters and Reviews, 2019
Anhar Abdel-Aziem, Huda Refaat Mahmoud Rashdan, Entesar Mohamed Ahmed, Sara N. Shabaan
The organic solvents are volatile and harmful, causing risks to peoples who inhale them as well as the environment. Thus, development of less hazardous synthetic methods for organic reactions is one of our objectives in current research. The grinding method is one of green chemistry techniques as it is carried out in the absence of solvent (1–4). Moreover, the solvent-free reactions have numerous advantages: reduced pollution, low costs, high yields and purities of products (5, 6). Otherwise, many compounds which contain coumarin nucleus exhibit antimicrobial (7), analgesic (8), ulcerogenic (9), anticoagulant (10), antiviral (11) and anti-malarial (12), anti-inflammatory (13, 14) anti-leishmanial (15) as well as antioxidant (16, 17) activities. The anti-tumor activity of coumarins received a considerable interest owing to their cytotoxic activity against various types of cancer cells, including gastric cancer, liver cancer, colon cancer, breast cancer, prostate cancer, Periodontal Ligament, fibroblast, nasopharyngeal carcinoma, and normal fibroblast cell lines (18–22). In addition, coumarin derivatives can inhibit growth in human cancer cell lines (23) such as renal (ACHN), lung (A549, H727), leukemia (HL-60), breast (MCF7) and renal cell carcinoma (24). Coumarin and its derivatives are important components among the molecules in the drug industry. Warfarin, acenocoumarol and phenprocoumon are a derivatives of coumarin used as anticoagulant drugs. These are vitamin K antagonist which inhibits the coagulation via blocking of the coagulation factors [I, VII, IX and X] (25–27). Moreover, warfarin reduced metastases from intestinal cancer to a wide extent (28) and is also used beside the surgical treatment of cancer masses (29) (Figure 1).