Evidence map›Paper›PMID 29995408›Full record

ArticleJournal of medicinal chemistry2018

Identification of the 4-Position of 3-Alkynyl and 3-Heteroaromatic Substituted Pyridine Methanamines as a Key Modification Site Eliciting Increased Potency and Enhanced Selectivity for Cytochrome P-450 2A6 Inhibition.

Travis T Denton, Pramod Srivastava, Zuping Xia, Gang Chen, Christy J W Watson, Alec Wynd, Philip Lazarus

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 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
1.1field-weighted citation impact, top 23% of its field
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, 15 citations in OpenAlex.

  1. Article
  2. The Novel CYP2A6 Inhibitor, DLCI-1, Decreases Nicotine Self-Administration in Mice.The Journal of pharmacology and experimental therapeutics · 2020
    Article
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

7 authors at 1 institution in 1 country.

Travis T DentonDepartment of Pharmaceutical Sciences , College of Pharmacy, Washington State University , Spokane , Washington 99202 , United States.ORCID 0000-0002-1222-2538
Pramod SrivastavaDepartment of Pharmaceutical Sciences , College of Pharmacy, Washington State University , Spokane , Washington 99202 , United States.
Zuping XiaDepartment of Pharmaceutical Sciences , College of Pharmacy, Washington State University , Spokane , Washington 99202 , United States.ORCID 0000-0002-2187-8889
Gang ChenDepartment of Pharmaceutical Sciences , College of Pharmacy, Washington State University , Spokane , Washington 99202 , United States.
Christy J W WatsonDepartment of Pharmaceutical Sciences , College of Pharmacy, Washington State University , Spokane , Washington 99202 , United States.
Alec WyndDepartment of Pharmaceutical Sciences , College of Pharmacy, Washington State University , Spokane , Washington 99202 , United States.
Philip LazarusDepartment of Pharmaceutical Sciences , College of Pharmacy, Washington State University , Spokane , Washington 99202 , United States.ORCID 0000-0002-8686-0874
Washington State University Spokane · US

Funding

The UGT2A and 3A metabolizing enzymes and tobacco-related cancer riskR01ES025460 · NIEHS · WASHINGTON STATE UNIVERSITY · PI LAZARUS, PHILIP · 2015 to 2019
$2.8M
NIEHS NIH HHS R01 ES025460
6 · The paper itself

Abstract

Cigarette smoking causes nearly one in every five deaths in the United States. The development of a specific inhibitor of cytochrome P450 2A6 (CYP2A6), the major nicotine-metabolizing enzyme in humans, which could be prescribed for the cessation of cigarette smoking, has been undertaken. To further refine the structure activity relationship of CYP2A6, previously synthesized 3-alkynyl and 3-heteroaromatic substituted pyridine methanamines were used as lead compounds. Isosteric pyridine replacement and appendage of all available positions around the pyridine ring with a methyl group was performed to identify a modification that would increase CYP2A6 inhibition potency, which led to 4g (IC

Indexed as

Cytochrome P-450 CYP2A6Enzyme InhibitorsHumansMethylaminesMicrosomes, LiverMolecular StructurePyridinesSmokingTobacco Use CessationCytochrome P-450 CYP2A6Enzyme InhibitorsMethylaminesPyridines

Identifiers

PMID29995408
PMCPMC6309628
OpenAlexW2842732852

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

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.