- Design, synthesis and biological evaluation of novel inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
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This study is based on our attempts to further explore the structure-activity relationship (SAR) of VX-148 (3) in an attempt to identify inosine 5′-mono-phosphate dehydrogenase (IMPDH) inhibitors superior to mycophenolic acid. A five-point pharmacophore developed using structurally diverse, known IMPDH inhibitors guided further design of novel analogs of 3. Several conventional as well as novel medicinal chemistry strategies were tried. The combined structure- and ligand-based approaches culminated in a few analogs with either retained or slightly higher potency. The compounds which retained the potency were also checked for their ability to inhibit human peripheral blood mononuclear cells proliferation. This study illuminates the stringent structural requirements and strict SAR for IMPDH II inhibition.
- Dunkern, Torsten,Chavan, Sunil,Bankar, Digambar,Patil, Anuja,Kulkarni, Pritee,Kharkar, Prashant S.,Prabhu, Arati,Goebel, Heike,Rolser, Edith,Burckhard-Boer, Waltraud,Arumugam, Premkumar,Makhija, Mahindra T.
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p. 408 - 419
(2014/06/09)
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- One-pot green synthesis of azides from alcohols using bronsted acidic ionic liquid [HMIM][BF4] as solvent and catalyst
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Bronsted acidic ionic liquid, [HMIM][BF4], has been used as a non-volatile, eco-friendly solvent, and catalytic medium for the one-pot green synthesis of azides from corresponding alcohols. The [HMIM][BF 4] showed high reactivity than [BMIM][BF4] and [BMIM][PF6], affording azides in up to 97% yield, which could be easily separated from the reaction mixture. The ease of recyclability of [HMIM][BF4] makes the reaction economically and potentially viable for practical applications. Azides are versatile substrates in organic synthesis and serve as convenient intermediate in the synthesis of pharmaceutical heterocycles and natural products. By using dual functional [HMIM][BF 4] as solvent and catalyst, efficient synthesis of azides from their corresponding alcohols have been undertaken under eco-friendly conditions. This study may pave the way for practical application of [HMIM][BF4] in cholesterylamine synthesis.
- Garg, Bhaskar,Ling, Yong-Chien
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p. 737 - 742
(2014/07/22)
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- A mild and efficient method for preparation of azides from alcohols using acidic ionic liquid [H-NMP]HSO4
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We report here an efficient method for the synthesis and characterization of [H-NMP]HSO4 and its application as an efficient catalyst and solvent for preparation of azides from corresponding alcohols under mild conditions. This processor showed
- Hajipour, Abdol R.,Rajaei, Asiyeh,Ruoho, Arnold E.
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supporting information; experimental part
p. 708 - 711
(2011/03/17)
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- Methods for inhibiting mrp1
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The present invention relates to a compound of formula (I), which is useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.
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