Category: indole-building-block. In 2019.0 MOL DIVERS published article about CINNAMIC ACID; INFLUENZA; REPLICATION; CHALCONES; DISCOVERY; DOCKING in [Malbari, Khushboo D.; Chintakrindi, Anand S.; Ganji, Lata R.; Kanyalkar, Meena A.] Prin KM Kundnani Coll Pharm, Dept Pharmaceut Chem, Plot 23,Jote Joy Bldg,Rambhau Salgaonkar Marg, Mumbai 400005, Maharashtra, India; [Gohil, Devanshi J.; Kothari, Sweta T.] Haffkine Inst Training Res & Testing, Mumbai 400012, Maharashtra, India; [Joshi, Mamata, V] Tata Inst Fundamental Res, Natl Facil High Field NMR, Homi Bhabha Rd, Mumbai 400005, Maharashtra, India in 2019.0, Cited 35.0. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4.
The rate of mutability of pathogenic H1N1 influenza virus is a threat. The emergence of drug resistance to the current competitive inhibitors of neuraminidase, such as oseltamivir and zanamivir, attributes to a need for an alternative approach. The design and synthesis of new analogues with alternate approach are particularly important to identify the potential neuraminidase inhibitors which may not only have better anti-influenza activity but also can withstand challenge of resistance. Five series of scaffolds, namely aurones (1a-1e), pyrimidine analogues (2a-2b), cinnamic acid analogues (3a-3k), chalcones (4a-4h) and cinnamic acid linkages (5a-5c), were designed based on virtual screening against pandemic H1N1 virus. Molecular modelling studies revealed that the designed analogues occupied 430-loop cavity of neuraminidase. Docking of sialic acid in the active site preoccupied with the docked analogues, i.e. in 430-loop cavity, resulted in displacement of sialic acid from its native pose in the catalytic cavity. The favourable analogues were synthesized and evaluated for the cytotoxicity and cytopathic effect inhibition by pandemic H1N1 virus. All the designed analogues resulting in displacement of sialic acid suggested alternate binding mechanism. Overall results indicated that aurones can be measured best among all as potential neuraminidase inhibitor against pandemic H1N1 virus. [GRAPHICS] .
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles