Literature DB >> 11597491

Design, synthesis and pharmacological evaluation of 3-benzylazetidine-2-one-based human chymase inhibitors.

Y Aoyama1, M Uenaka, M Kii, M Tanaka, T Konoike, Y Hayasaki-Kajiwara, N Naya, M Nakajima.   

Abstract

3-Benzylazetidine-2-one derivatives were designed and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 3-benzylazetidine-2-ones led to compounds 23, which exhibited 3.1 nM inhibition of human chymase and enhancement of stability in human plasma (t(1/2) 6h).

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Year:  2001        PMID： 11597491     DOI： 10.1016/s0968-0896(01)00209-7

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  8 in total

Review 1.  Mast cell peptidases: chameleons of innate immunity and host defense.

Authors:  Neil N Trivedi; George H Caughey
Journal:  Am J Respir Cell Mol Biol       Date:  2009-11-20       Impact factor: 6.914

2.  Optimization of a β-Lactam Scaffold for Antibacterial Activity via the Inhibition of Bacterial Type I Signal Peptidase.

Authors:  Chien-Hung Yeh; Shawn I Walsh; Arryn Craney; M Greg Tabor; Ana-Florina Voica; Ramkrishna Adhikary; Sydney E Morris; Floyd E Romesberg
Journal:  ACS Med Chem Lett       Date:  2018-03-15       Impact factor: 4.345

3.  Ethyl 1'-[1-(4-methoxyphenyl)-3-phenoxy-4-phenylazetidin-1-yl]-1,3-dioxo-2',3',5',6',7',7a'-hexahydroindan-2-spiro-3'-1'H-pyrrolizine-2'-carboxylate.

Authors:  E Theboral Sugi Kamala; S Nirmala; L Sudha; N Arumugam; R Raghunathan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-08-30

4.  A combination of receptor-based pharmacophore modeling & QM techniques for identification of human chymase inhibitors.

Authors:  Mahreen Arooj; Sugunadevi Sakkiah; Songmi Kim; Venkatesh Arulalapperumal; Keun Woo Lee
Journal:  PLoS One       Date:  2013-04-26       Impact factor: 3.240

5.  2-[1-(4-Ethoxy-phen-yl)-2-oxo-4-styryl-azetidin-3-yl]isoindoline-1,3-dione.

Authors:  Mehmet Akkurt; Selvi Karaca; Ali Asghar Jarrahpour; Maaroof Zarei; Orhan Büyükgüngör
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-04-26

6.  3D QSAR pharmacophore modeling, in silico screening, and density functional theory (DFT) approaches for identification of human chymase inhibitors.

Authors:  Mahreen Arooj; Sundarapandian Thangapandian; Shalini John; Swan Hwang; Jong Keun Park; Keun Woo Lee
Journal:  Int J Mol Sci       Date:  2011-12-12       Impact factor: 5.923

7.  Crystal structure of a complex of human chymase with its benzimidazole derived inhibitor.

Authors:  Yoshiyuki Matsumoto; Shinji Kakuda; Masahiro Koizumi; Tsuyoshi Mizuno; Yumiko Muroga; Takashi Kawamura; Midori Takimoto-Kamimura
Journal:  J Synchrotron Radiat       Date:  2013-09-25       Impact factor: 2.616

8.  Synthesis and biological evaluation of new 2-azetidinones with sulfonamide structures.

Authors:  Oana Maria Dragostin; Florentina Lupascu; Cornelia Vasile; Mihai Mares; Valentin Nastasa; Ramona Florina Moraru; Dragos Pieptu; Lenuta Profire
Journal:  Molecules       Date:  2013-04-08       Impact factor: 4.411
  8 in total

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