ChemInform Abstract: Synthesis, Characterization and anti‐HIV and Antitumor Activities of New Coumarin Derivatives.

Abstract

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Amination of Benzoxazoles by Visible-Light Photoredox Catalysis

“…17 Using commercially available 4-bromomethyl-7-methoxycoumarin, 1-Boc-piperazine, and benzoxazole, the desired product 6 was obtained with 42% total yield in two steps under mild conditions (Scheme 2).…”

1-(6-Fluoro-1,3-benzothiazol-2-yl)-3-phenyl-1H-pyrazole-4-carbaldehyde

“…For the biological activity of benzothiazole derivatives, see: Al-Soud et al (2006); Kini et al (2007); Munirajasekhar et al (2011); Gurupadayya et al (2008); Bowyer et al (2007); Mittal et al (2007); Rocío Pozas et al (2005); Rana et al (2008). For a related structure, see: Fun et al (2011).…”

“…The substituted benzothiazole derivatives have emerged as significant components in various diversified therapeutic applications. The literature review reveals that benzothiazoles and their derivatives show considerable activity including potent inhibition of human immunodeficiency virus type 1 (HIV-1) replication by HIV-1 protease inhibition (Al-Soud et al, 2006), antitumor (Kini et al, 2007), anthelmintic (Munirajasekhar et al, 2011) analgesic and antiinflammatory (Gurupadayya et al, 2008), antimalarial (Bowyer et al, 2007), antifungal (Mittal et al, 2007), anticandidous (Rocío Pozas et al, 2005) as well as various CNS activities (Rana et al, 2008). The structure of 2-[5-(4methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-6-methyl-1,3-benzothiazole has been reported by Fun et al (2011).…”

A two component protocol for synthesis of 3-(2-(substituted phenylamino)thiazol-4-yl)-2H-chromen-2-ones

“…A number of coumarin derivatives are used in the pharmaceutical industry as precursor molecules for the synthesis of many synthetic pharmaceutical compounds including anticoagulants and vitamin K antagonists, while others are used in the treatment of lymphedema. 1 Coumarin derivatives exhibit antibacterial, antifungal, 2,3 anticancer, 4 anti-HIV, 5,6 antitubercular, 7 antiacylcholineestrase, 8 antimutagenic, 9 anthelmintic, 10 anticoagulant, 11 anti-inflammatory, antihepatitis C, 12 and analgesic 13 properties.…”