Evidence map›Paper›PMID 29970308›Full record

ArticleBioorganic & medicinal chemistry letters2018

Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand.

Arun K Ghosh, Koena Ghosh, Margherita Brindisi, Emma K Lendy, Yu-Chen Yen, Nagaswamy Kumaragurubaran, Xiangping Huang, Jordan Tang, Andrew D Mesecar

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

2 citing papers in PubMed.

  1. Article
  2. A Review of the Medicinal Importance and Perspectives of the 2-isoxazoline Scaffold.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025
    Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors.

Arun K GhoshDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, United States; Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, United States. Electronic address: akghosh@purdue.edu.
Koena GhoshDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, United States.
Margherita BrindisiDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, United States.
Emma K LendyDepartment of Biochemistry, Purdue University, West Lafayette, IN 47907, United States.
Yu-Chen YenDepartment of Biological Sciences, Purdue University, West Lafayette, IN 47907, United States.
Nagaswamy KumaragurubaranDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, United States.
Xiangping HuangProtein Studies Program, Oklahoma Medical Research Foundation, United States.
Jordan TangProtein Studies Program, Oklahoma Medical Research Foundation, United States; Department of Biochemistry and Molecular Biology, University of Oklahoma Health Science Center, Oklahoma City, OK 73104, United States.
Andrew D MesecarDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, United States; Department of Biochemistry, Purdue University, West Lafayette, IN 47907, United States; Department of Biological Sciences, Purdue University, West Lafayette, IN 47907, United States.

Funding

Transgenic Mouse Core Facility Shared Resource (TMCF-SR)P30CA023168 · NCI · PURDUE UNIVERSITY WEST LAFAYETTE · PI John Tesmer · 1985 to 2026
$43.4M
SECRETASE INHIBITORS FOR TREATING ALZHEIMER'S DISEASER01AG018933 · NIA · OKLAHOMA MEDICAL RESEARCH FOUNDATION · PI TANG, JORDAN J · 2001 to 2011
$4.9M
DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORSR01GM053386 · NIGMS · UNIVERSITY OF ILLINOIS AT CHICAGO · PI GHOSH, ARUN K · 1995 to 2010
$3.7M
NCI NIH HHS P30 CA023168NIA NIH HHS R01 AG018933NIGMS NIH HHS R01 GM053386
6 · The paper itself

Abstract

We describe the design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors containing bicyclic isoxazoline carboxamides as the P3 ligand in combination with methyl cysteine, methylsulfonylalanine and Boc-amino alanine as P2 ligands. Inhibitor 3a displayed a BACE1 K

Indexed as

AlanineAmidesAmyloid Precursor Protein SecretasesAspartic Acid EndopeptidasesBridged Bicyclo CompoundsCarboxylic AcidsCatalytic DomainCrystallography, X-RayCysteineHumansIsoxazolesMolecular StructureProtease InhibitorsAlanineAmidesAmyloid Precursor Protein SecretasesAspartic Acid EndopeptidasesBACE1 protein, humanBridged Bicyclo CompoundsCarboxylic AcidsCysteineIsoxazolesmecysteineProtease InhibitorsAlzheimer’s diseaseBACE-1IsoxazolineMemapsin 2β-secretase

Identifiers

PMID29970308
PMCPMC6085084

What OpenQuestion holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.