Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors.

A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives were synthesized via converting the readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and then reacting with different substituted amines. The molecular structures of two representative compounds, that is, 3 and 5l were confirmed by single crystal X-ray diffraction study. All the compounds synthesized were evaluated for their cyclooxygenase (COX) inhibiting properties in vitro. The compound 5i showed balanced selectivity towards COX-2 over COX-1 inhibition and good docking scores when docked into the COX-2 protein.

PIN it on auxin: the role of PIN1 and PAT in tomato development.

The growth and development of plants is regulated by several external and internal factors including auxin. Its distribution regulates several developmental processes in plants. Auxin molecules function as mobile signals and are involved in the spatial and temporal coordination of plant morphogenesis and in plant responses to their environment. The intercellular transport of auxin is facilitated by transport proteins and the disruption of polar auxin flow results in various developmental abnormalities. In this review, we discuss the developmental and physiological significance of over-accumulation of PIN1 auxin transport facilitator protein in tomato as seen in the enhanced polar auxin transport pct1-2 mutant.