Synthesis and biological evaluation of BMS-986120 and its deuterated derivatives as PAR4 antagonists.


:BMS-986120 is a PAR4 antagonist that is being investigated as an antiplatelet agent in phase I clinical trial. An improved synthesis of BMS-986120 has been developed. Based on the novel synthetic approach to BMS-986120, a series of deuterated derivatives of BMS-986120 have been synthesized and biologically evaluated to search for more potent antiplatelet agents. The in vitro antiplatelet assay by turbidimetry demonstrated that PC-2 and PC-6 had IC50 values of 6.30 nM and 6.97 nM, respectively, versus BMS-986120 with an IC50 of 7.80 nM. The result of in vitro metabolic stability study showed that all of the deuterated compounds had similar half-life (T1/2) and intrinsic clearance (Clint) in comparison with BMS-986120. Further probing the metabolic profile of BMS-986120 is worth being conducted.


Bioorg Med Chem


Chen P,Ren S,Song H,Chen C,Chen F,Xu Q,Kong Y,Sun H




Has Abstract


2019-01-01 00:00:00














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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Godskesen M,Lundt I,Madsen R,Winchester B

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Rao CS,Chu JJ,Liu RS,Lai YK

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    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Hao M,Li Y,Liu L,Yuan X,Gao Y,Guan Z,Li W

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


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  • Synthesis, binding, nuclease resistance and cellular uptake properties of 2'-O-acetalester-modified oligonucleotides containing cationic groups.

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Biscans A,Rouanet S,Bertrand JR,Vasseur JJ,Dupouy C,Debart F

    更新日期:2015-09-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Nashaat S,Henen MA,El-Messery SM,Eisa H

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Opsenica D,Angelovski G,Pocsfalvi G,Juranić Z,Zizak Z,Kyle D,Milhous WK,Solaja BA

    更新日期:2003-07-03 00:00:00

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    pub_type: 杂志文章


    authors: Donkor IO,Xu J,Liu J,Cameron K

    更新日期:2020-05-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

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    authors: Sommer S,Weikart ND,Linne U,Mootz HD

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    pub_type: 杂志文章


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    更新日期:2010-11-15 00:00:00

  • Inhibition of monoamine oxidase B by selected benzimidazole and caffeine analogues.

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    pub_type: 杂志文章


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    更新日期:2007-06-01 00:00:00

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    pub_type: 杂志文章


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    更新日期:2004-05-15 00:00:00

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    pub_type: 杂志文章


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    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Nakano H,Inoue T,Kawasaki N,Miyataka H,Matsumoto H,Taguchi T,Inagaki N,Nagai H,Satoh T

    更新日期:2000-02-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Fujii H,Narita M,Mizoguchi H,Murachi M,Tanaka T,Kawai K,Tseng LF,Nagase H

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Kyei-Baffour K,Mohammad H,Seleem MN,Dai M

    更新日期:2019-05-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Chai H,Zhao Y,Zhao C,Gong P

    更新日期:2006-02-15 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ishida J,Yamamoto H,Kido Y,Kamijo K,Murano K,Miyake H,Ohkubo M,Kinoshita T,Warizaya M,Iwashita A,Mihara K,Matsuoka N,Hattori K

    更新日期:2006-03-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Crizanto de Lima E,Castelo-Branco FS,Maquiaveli CC,Farias AB,Rennó MN,Boechat N,Silva ER

    更新日期:2019-09-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: León LG,Donadel OJ,Tonn CE,Padrón JM

    更新日期:2009-09-01 00:00:00

  • Carbonic anhydrase activators: kinetic and X-ray crystallographic study for the interaction of D- and L-tryptophan with the mammalian isoforms I-XIV.

    abstract::An activation study of mammalian carbonic anhydrase (CA, EC isoforms I-XIV with D- and L-tryptophan has been performed both by means of kinetic and X-ray crystallographic techniques. These compounds show a time dependent activity against isozyme CA II, with activation constants of 1.13 microM for L-Trp and 0....

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Temperini C,Innocenti A,Scozzafava A,Supuran CT

    更新日期:2008-09-15 00:00:00

  • Glycoprotein-inspired materials promote the proteolytic release of cell surface L-selectin.

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Gordon EJ,Strong LE,Kiessling LL

    更新日期:1998-08-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Iyer MR,Rothman RB,Dersch CM,Jacobson AE,Rice KC

    更新日期:2013-06-01 00:00:00