To follow-up on our prior Part I review, this Part II review summarizes and provides updated literature on novel quinoline and quinazoline alkaloids isolated during the period of 2009-2016, together with the biological activity and the mechanisms of action of these classes of natural products. Over 200 molecules with a broad range of biological activities, including antitumor, antiparasitic and insecticidal, antibacterial and antifungal, cardioprotective, antiviral, anti-inflammatory, hepatoprotective, antioxidant, anti-asthma, antitussive, and other activities, are discussed. This survey should provide new clues or possibilities for the discovery of new and better drugs from the original naturally occurring quinoline and quinazoline alkaloids.
Inspired by quinine and its analogues,
we designed, synthesized,
and evaluated two series of quinoline small molecular compounds (a and 2a) and six series of quinoline derivatives
(3a–f) for their antifungal activities.
The results showed that compounds 3e and 3f series exhibited significant fungicidal activities. Significantly,
compounds 3f-4 (EC50 = 0.41 μg/mL) and 3f-28 (EC50 = 0.55 μg/mL) displayed the superior
in vitro fungicidal activity and the potent in vivo curative effect
against Sclerotinia sclerotiorum. Preliminary
mechanism studies showed that compounds 3f-4 and 3f-28 could cause changes in the cell membrane permeability,
accumulation of reactive oxygen species, loss of mitochondrial membrane
potential, and effective inhibition of germination and formation of S. sclerotiorum sclerotia. These results indicate
that compounds 3f-4 and 3f-28 are novel
potential fungicidal candidates against S. sclerotiorum derived from natural products.
Phytopathogenic fungi have become a serious threat to the quality of agricultural products, food security and human health globally, necessitating the need to discover new antifungal agents with de novo chemical scaffolds and high efficiency.
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