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Literature DB >> 11425540

Total synthesis of human chymase inhibitor methyllinderone and structure--activity relationships of its derivatives.

Y Aoyama¹, T Konoike, A Kanda, N Naya, M Nakajima.

Abstract

Total synthesis of human chymase inhibitor methyllinderone has been achieved in only four steps with an overall yield of 21% from dimethyl squarate. We developed an efficient synthetic method for obtaining methyllinderone derivatives and found the active compound. In addition, we propose the inhibition mechanism of the active compound against human chymase using calculations.

Entities: Chemical Gene Species

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Year: 2001 PMID： 11425540 DOI： 10.1016/s0960-894x(01)00265-7

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

7 in total

1. Synthesis, antifungal activity, and structure-activity relationships of coruscanone A analogues.

Authors: K Suresh Babu; Xing-Cong Li; Melissa R Jacob; Qifeng Zhang; Shabana I Khan; Daneel Ferreira; Alice M Clark
Journal: J Med Chem Date: 2006-12-28 Impact factor: 7.446

2. Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.

Authors: Paul A Jackson; John C Widen; Daniel A Harki; Kay M Brummond
Journal: J Med Chem Date: 2016-12-20 Impact factor: 7.446

Review 3. Chymase inhibitors for the treatment of cardiac diseases: a patent review (2010-2018).

Authors: Sarfaraz Ahmad; Carlos M Ferrario
Journal: Expert Opin Ther Pat Date: 2018-10-10 Impact factor: 6.674

4. 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

Total synthesis of human chymase inhibitor methyllinderone and structure--activity relationships of its derivatives.

1. Synthesis, antifungal activity, and structure-activity relationships of coruscanone A analogues.

2. Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.

Review 3. Chymase inhibitors for the treatment of cardiac diseases: a patent review (2010-2018).

4. 3D QSAR pharmacophore modeling, in silico screening, and density functional theory (DFT) approaches for identification of human chymase inhibitors.

5. Searching for Chymase Inhibitors among Chamomile Compounds Using a Computational-Based Approach.

6. Concise Synthesis of Linderaspirone A and Bi-linderone.

7. Molecular modeling study for inhibition mechanism of human chymase and its application in inhibitor design.