Ultrasound Promoted Synthesis and Anticoagulant Activity of 2-Amino- 4H-chromen-4-ylphosphonates

Abstract

The findings from this study highlight that ultrasonication of the one pot three component reaction of salicylaldehyde derivatives, malononitrile and dialkyl phosphite with piperazine as a catalyst for the synthesis of 2-amino-4H-chromen-4-ylphosphonates is the best method. In vitro coagulant assay in terms of prothrombin time (PT) revealed that 4j, 4h and 4g possess promising anticoagulant properties. Other compounds (4a-l) were also found to have significant anticoagulant effect when compared with the heparin as positive control. Thus, these compounds qualify for further clinical studies to be used as the blood anticoagulants.

Facile one‐pot three‐component route to an assembly of 2‐amino‐4H‐chromenes and spirochromenes promoted via ceria nanoparticles in a benign manner

“…4H-chromenes, both natural and synthetic category, exhibit a broad therapeutic potential in the treatment of diverse diseases [13][14][15][16] and distributed throughout the nature with a wide range of remarkable biological properties. [17][18][19][20] Compounds with spirocyclic unit are existent in a wide number of natural products and drug targets. [21][22][23][24] Especially, pyran-annulated spirooxindoles have drawn keen attention for a broad spectrum of bioactivities such as antimicrobial, antioxidant, anti-HIV, anticancer, anticoagulant, antianaphylactic, and photochromic properties.…”

NEt3-Promoted Construction of Functionalized 4H-Chromenes via [4+2] Cycloaddition Reaction of ortho-Quinone Methides with β-Ketothioamides

“…[4] Miroestrol was considered to be a rejuvenating drug. [5] Some are endowed with a broad spectrum of biological properties such as anticancer, [6] antimicrobial, [7] antimalarial, [8] anticoagu-lant, [9] antifungal, [10] and antioxidant activities. [11] Although various approaches for the preparation of 4H-chromenes have been established, [12] efficient and practical synthetic methods to access 4H-chromenes are still extremely desirable.…”

Recent progress on coumarinscaffold‐basedanti‐microbial agents (PartIII)

“…Coumarins present a variety of bioactivities, including anticoagulant drugs, [ 46–49 ] and vitamin K antagonists. [ 50–55 ] The most incredible ones are warfarin, acenocoumarol, and phenprocoumon, currently in use in several countries.…”