Evidence map›Paper›PMID 41531426›Full record

ArticleOrganic & biomolecular chemistry2026

Regioselective multicomponent synthesis of α-boryl ureas: discovery of a potent main protease inhibitor.

Yusif I Gyasi, Satyanarayana Nyalata, Sophea Pa, Disni Gunasekera, Veerabhadra R Vulupala, Nagarjun R Mallampudi, Gopal R Ramidi, Shiqing Xu

Abstract read
In one paragraph

Article in Organic & biomolecular chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing 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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

8 authors.

Yusif I GyasiDepartment of Chemistry, Texas A&M University, College Station, Texas 77843, USA. shiqing.xu@tamu.edu.
Satyanarayana NyalataDepartment of Chemistry, Texas A&M University, College Station, Texas 77843, USA. shiqing.xu@tamu.edu.
Sophea PaDepartment of Chemistry, Texas A&M University, College Station, Texas 77843, USA. shiqing.xu@tamu.edu.
Disni GunasekeraDepartment of Chemistry, Texas A&M University, College Station, Texas 77843, USA. shiqing.xu@tamu.edu.
Veerabhadra R VulupalaDepartment of Chemistry, Texas A&M University, College Station, Texas 77843, USA. shiqing.xu@tamu.edu.
Nagarjun R MallampudiDepartment of Chemistry, Texas A&M University, College Station, Texas 77843, USA. shiqing.xu@tamu.edu.ORCID 0000-0003-3420-2826
Gopal R RamidiDepartment of Chemistry, Texas A&M University, College Station, Texas 77843, USA. shiqing.xu@tamu.edu.
Shiqing XuDepartment of Chemistry, Texas A&M University, College Station, Texas 77843, USA. shiqing.xu@tamu.edu.ORCID 0000-0001-6260-9290

Funding

The Development of Reversible Covalent PROTAC Technology as a New Anti-COVID-19 StrategyR21AI164088 · NIAID · TEXAS A&M UNIVERSITY · PI XU, SHIQING · 2021 to 2022
$406k
Development of PROTACs Targeting Papain-like Protease as Broad-Spectrum Anti-Coronavirus TherapeuticsR21AI166521 · NIAID · TEXAS A&M UNIVERSITY · PI XU, SHIQING · 2022 to 2023
$405k
NIAID NIH HHS R21 AI164088NIAID NIH HHS R21 AI166521
6 · The paper itself

Abstract

The development of efficient synthetic methods for α-boryl ureas is of significant interest due to their potential as drug-like scaffolds in medicinal chemistry. Herein, we present a multicomponent strategy that transforms α-haloboronates, trimethylsilyl isocyanate, sodium iodide, and amines into diverse drug-like scaffold α-boryl ureas under mild conditions. This protocol features broad substrate scope and great functional-group tolerance, and enables the regioselective synthesis of previously inaccessible α-boryl ureas, including late-stage functionalization of drug molecules. Mechanistic studies suggest that a regioselective 1,2-boronate migration pathway may underlie the different regioselectivities observed with primary and secondary amines. To highlight the potential of this methodology in drug discovery, an α-boryl urea analog of nirmatrelvir was synthesized, exhibiting remarkable inhibitory activity (IC

Indexed as

Protease InhibitorsSARS-CoV-2UreaDrug DiscoveryHumansMolecular StructureStereoisomerismProtease InhibitorsUrea

Identifiers

PMID41531426
PMCPMC12800895

What OpenQuestion holds

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Registered trials

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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.