N‑Alkyl and N‑Aryl Aminopyrazole Spirocarbamates: A Two-Pronged Lead Optimization Strategy to Identify Orally Bioavailable Plasma Kallikrein Inhibitors.
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| Title: | N‑Alkyl and N‑Aryl Aminopyrazole Spirocarbamates: A Two-Pronged Lead Optimization Strategy to Identify Orally Bioavailable Plasma Kallikrein Inhibitors. |
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| Authors: | Merchant RR; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States., Chernyak N; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States., Lopez JA; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States., Sharp PP; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States., Mandal M; Department of Discovery Chemistry, Merck & Co., Inc., Rahway, New Jersey 07065, United States., He J; Department of Discovery Chemistry, Merck & Co., Inc., Rahway, New Jersey 07065, United States., Hruza A; Department of Discovery Chemistry, Merck & Co., Inc., Rahway, New Jersey 07065, United States., Rearden P; Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., South San Francisco, California 94080, United States., Tatosian DA; Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., Rahway, New Jersey 07065, United States., Esmay J; Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., South San Francisco, California 94080, United States., Yang S; Computational and Structural Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States., Cheng AC; Computational and Structural Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States., Ellsworth K; Quantitative Biosciences, Merck & Co., Inc., Rahway, New Jersey 07065, United States., Ogawa A; Quantitative Biosciences, Merck & Co., Inc., South San Francisco, California 94080, United States., Piou T; Department of Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States., Fier P; Department of Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States., Hicks J; Department of Discovery Chemistry, Merck & Co., Inc., Rahway, New Jersey 07065, United States., Sinz C; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States., Ogawa AK; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States. |
| Source: | ACS medicinal chemistry letters [ACS Med Chem Lett] 2026 Feb 24; Vol. 17 (3), pp. 744-749. Date of Electronic Publication: 2026 Feb 24 (Print Publication: 2026). |
| Publication Type: | Journal Article |
| Journal Info: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 101521073 Publication Model: eCollection Cited Medium: Print ISSN: 1948-5875 (Print) Linking ISSN: 19485875 NLM ISO Abbreviation: ACS Med Chem Lett Subsets: PubMed not MEDLINE |
| Database: | MEDLINE Ultimate |
| FullText | Text: Availability: 0 |
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| Header | DbId: mdl DbLabel: MEDLINE Ultimate An: 41847638 AccessLevel: 2 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: N‑Alkyl and N‑Aryl Aminopyrazole Spirocarbamates: A Two-Pronged Lead Optimization Strategy to Identify Orally Bioavailable Plasma Kallikrein Inhibitors. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AU" term="%22Merchant+RR%22">Merchant RR</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Chernyak+N%22">Chernyak N</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Lopez+JA%22">Lopez JA</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Sharp+PP%22">Sharp PP</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Mandal+M%22">Mandal M</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., Rahway, New Jersey 07065, United States.<br /><searchLink fieldCode="AU" term="%22He+J%22">He J</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., Rahway, New Jersey 07065, United States.<br /><searchLink fieldCode="AU" term="%22Hruza+A%22">Hruza A</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., Rahway, New Jersey 07065, United States.<br /><searchLink fieldCode="AU" term="%22Rearden+P%22">Rearden P</searchLink>; Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Tatosian+DA%22">Tatosian DA</searchLink>; Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., Rahway, New Jersey 07065, United States.<br /><searchLink fieldCode="AU" term="%22Esmay+J%22">Esmay J</searchLink>; Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Yang+S%22">Yang S</searchLink>; Computational and Structural Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Cheng+AC%22">Cheng AC</searchLink>; Computational and Structural Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Ellsworth+K%22">Ellsworth K</searchLink>; Quantitative Biosciences, Merck & Co., Inc., Rahway, New Jersey 07065, United States.<br /><searchLink fieldCode="AU" term="%22Ogawa+A%22">Ogawa A</searchLink>; Quantitative Biosciences, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Piou+T%22">Piou T</searchLink>; Department of Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States.<br /><searchLink fieldCode="AU" term="%22Fier+P%22">Fier P</searchLink>; Department of Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States.<br /><searchLink fieldCode="AU" term="%22Hicks+J%22">Hicks J</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., Rahway, New Jersey 07065, United States.<br /><searchLink fieldCode="AU" term="%22Sinz+C%22">Sinz C</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States.<br /><searchLink fieldCode="AU" term="%22Ogawa+AK%22">Ogawa AK</searchLink>; Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States. – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%22101521073%22">ACS medicinal chemistry letters</searchLink> [ACS Med Chem Lett] 2026 Feb 24; Vol. 17 (3), pp. 744-749. <i>Date of Electronic Publication: </i>2026 Feb 24 (<i>Print Publication: </i>2026). – Name: TypePub Label: Publication Type Group: TypPub Data: Journal Article – Name: TitleSource Label: Journal Info Group: Src Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22American+Chemical+Society%22">American Chemical Society </searchLink><i>Country of Publication: </i>United States <i>NLM ID: </i>101521073 <i>Publication Model: </i>eCollection <i>Cited Medium: </i>Print <i>ISSN: </i>1948-5875 (Print) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%2219485875%22">19485875 </searchLink><i>NLM ISO Abbreviation: </i>ACS Med Chem Lett <i>Subsets: </i>PubMed not MEDLINE |
| PLink | https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=mdl&AN=41847638 |
| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1021/acsmedchemlett.6c00066 Languages: – Code: eng Text: English PhysicalDescription: Pagination: StartPage: 744 Titles: – TitleFull: N‑Alkyl and N‑Aryl Aminopyrazole Spirocarbamates: A Two-Pronged Lead Optimization Strategy to Identify Orally Bioavailable Plasma Kallikrein Inhibitors. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Merchant RR – PersonEntity: Name: NameFull: Chernyak N – PersonEntity: Name: NameFull: Lopez JA – PersonEntity: Name: NameFull: Sharp PP – PersonEntity: Name: NameFull: Mandal M – PersonEntity: Name: NameFull: He J – PersonEntity: Name: NameFull: Hruza A – PersonEntity: Name: NameFull: Rearden P – PersonEntity: Name: NameFull: Tatosian DA – PersonEntity: Name: NameFull: Esmay J – PersonEntity: Name: NameFull: Yang S – PersonEntity: Name: NameFull: Cheng AC – PersonEntity: Name: NameFull: Ellsworth K – PersonEntity: Name: NameFull: Ogawa A – PersonEntity: Name: NameFull: Piou T – PersonEntity: Name: NameFull: Fier P – PersonEntity: Name: NameFull: Hicks J – PersonEntity: Name: NameFull: Sinz C – PersonEntity: Name: NameFull: Ogawa AK IsPartOfRelationships: – BibEntity: Dates: – D: 24 M: 02 Text: 2026 Feb 24 Type: published Y: 2026 Identifiers: – Type: issn-print Value: 1948-5875 Numbering: – Type: volume Value: 17 – Type: issue Value: 3 Titles: – TitleFull: ACS medicinal chemistry letters Type: main |
| ResultId | 1 |
