# Developing triazolopyrimidines as novel anti-tubercular agents

> **NIH NIH R56** · SEATTLE CHILDREN'S HOSPITAL · 2022 · $492,250

## Abstract

Project Summary
Mycobacterium tuberculosis, the causative agent of tuberculosis, is a major health problem globally. The World
Health Organization reports that billions of people are latently infected with the organism, the number of new
cases continues to rise (>10 million in 2019) and >1 million died from tuberculosis in 2019. Current anti-tubercular
drugs are mainly effective against metabolically active and replicating bacteria. In addition to the need for new
antibiotics that are effective against both drug sensitive and drug resistant strains, there is an urgent need for
new therapeutics that can shorten therapy.
We have identified the triazolopyrimidines as anti-tubercular agents. The series has attractive biological
properties with potent anti-tubercular activity, activity against non-replicating (persistent/tolerant) bacteria, a
narrow spectrum of activity, and low cytotoxicity. Our preliminary data suggests that these molecules target a
key step in bacterial respiration. We have made analogs of the series which show potential for further
development.
Our long-term goal is to develop the triazolopyrimidines series as new anti-tubercular agents with excellent
physicochemical and biological properties. In this 3-year proposal we will complete sufficient exploration of the
series to generate proof of concept that the molecules work in an animal model of infection. We will also conduct
studies to identify the target and/or mode of action and to determine which other drugs (or drug candidates)
would be the best partners for a novel combination regimen.
The outcomes of this project would be (i) confirmation that the triazolopyrimidine series is a tractable series for
further development as a novel anti-tubercular drug; (ii) confirmation of the mode of action; and (iii) identification
of the best combination partners. Demonstration of in vivo activity and tractability of the series would lead to a
full drug discovery and development project in the future.

## Key facts

- **NIH application ID:** 10672660
- **Project number:** 1R56AI164599-01A1
- **Recipient organization:** SEATTLE CHILDREN'S HOSPITAL
- **Principal Investigator:** Tanya Parish
- **Activity code:** R56 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $492,250
- **Award type:** 1
- **Project period:** 2022-08-17 → 2024-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10672660

## Citation

> US National Institutes of Health, RePORTER application 10672660, Developing triazolopyrimidines as novel anti-tubercular agents (1R56AI164599-01A1). Retrieved via AI Analytics 2026-05-26 from https://api.ai-analytics.org/grant/nih/10672660. Licensed CC0.

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