- Hybrids of Small-Molecule CD4 Mimics with Polyethylene Glycol Units as HIV Entry Inhibitors
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CD4 mimics are small molecules that inhibit the interaction of gp120 with CD4. We have developed several CD4 mimics. Herein, hybrid molecules consisting of CD4 mimics with a long alkyl chain or a PEG unit attached through a self-cleavable linker were synthesized. In anti-HIV activity, modification with a PEG unit appeared to be more suitable than modification with a long alkyl chain. Thus, hybrid molecules of CD4 mimics, with PEG units attached through an uncleavable linker, were developed and showed high anti-HIV activity and low cytotoxicity. In investigation of pharmacokinetics in a rhesus macaque, a hybrid compound had a more effective PK profile than that of the parent compound, and intramuscular injection was a more useful administration route to maintain the high blood concentration of the CD4 mimic than intravenous injection. The presented hybrid molecules of CD4 mimics with a PEG unit would be practically useful when combined with a neutralizing antibody.
- Kobayakawa, Takuya,Tsuji, Kohei,Konno, Kiju,Himeno, Ai,Masuda, Ami,Yang, Tingting,Takahashi, Kohei,Ishida, Yusuke,Ohashi, Nami,Kuwata, Takeo,Matsumoto, Kaho,Yoshimura, Kazuhisa,Sakawaki, Hiromi,Miura, Tomoyuki,Harada, Shigeyoshi,Matsushita, Shuzo,Tamamura, Hirokazu
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supporting information
p. 1481 - 1496
(2021/02/27)
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- OIL THICKENING AGENT
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PROBLEM TO BE SOLVED: To provide oil thickening agents which dissolve in oils readily and form a transparent oil gel. SOLUTION: The present invention provides an oil thickening agent which is a compound having an unsymmetrical diamide structure represented by formula (I) or (II). The invention also provides cosmetics, skin external preparations, and emulsion compositions containing the thickener. [R1 is a saturated or unsaturated straight chain alkyl group, alkenyl group, or alkynyl group of C9 to 30; A is an alkylene group of C1 to 10, an aralkylene group or arylene group having 8 to 10 carbon atoms; and R2 is a saturated/unsaturated branched alkyl group having 7 to 30 carbon atoms.] SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0029
(2019/03/26)
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