Early preclinical development of Mycobacterium tuberculosis amino acid biosynthesis pathway inhibitor DRILS-1398 as a potential anti-TB drug

The search for new anti-tubercular agents is vital for the fight against Mycobacterium tuberculosis, particularly given the rise of drug-resistant strains. DRILS-1398, a pyrazolo[4,3-d]pyrimidine derivative, was discovered as a potent inhibitor of M.tb chorismate mutase (M.tb-CM) with an IC50 = 3.0...

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Published iniScience Vol. 28; no. 6; p. 112537
Main Authors Biswas, Deepesh, Edwin, Rebecca Kristina, Kumar, K. Shiva, Alam, Anwar, Kumar, Dhiraj, Chakraborty, Sandipan, Bulusu, Gopalakrishnan, Ahmad, Farhan Jalees, Shenoy, Gautham G., Singh, Lakshyaveer, Agarwal, Mansi, Siraj, Fouzia, Oruganti, Srinivas, Misra, Parimal, Ehtesham, Nasreen Zafar, Pal, Manojit, Hasnain, Seyed Ehtesham
Format Journal Article
LanguageEnglish
Published United States Elsevier Inc 20.06.2025
Elsevier
Subjects
Biological sciences
Medical Microbiology
Microbiology
Natural sciences
Pharmacology
Medical Microbiology
Biological sciences
Pharmacology
Microbiology
Natural sciences
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Abstract The search for new anti-tubercular agents is vital for the fight against Mycobacterium tuberculosis, particularly given the rise of drug-resistant strains. DRILS-1398, a pyrazolo[4,3-d]pyrimidine derivative, was discovered as a potent inhibitor of M.tb chorismate mutase (M.tb-CM) with an IC50 = 3.0 ± 0.2 μM (n = 3) and IC90 = 10 μM. The compound demonstrated efficacy against multi-drug resistant M.tb strains (MIC = 4 μg/mL, ∼10.0 μM) and effective inhibition of intracellular M.tb in THP-1 macrophages. With favorable pharmacokinetics, moderate stability in vitro, and a promising safety profile, DRILS-1398 showed no toxicity at doses up to 500 mg/kg b.w./day when dosed orally daily once for 7 consecutive days in mice. Both DRILS-1398 and its formulation DRILS-1398(F) were successful in clearing M.tb infection from the lungs and spleen in murine models. These findings suggest DRILS-1398 as a promising lead candidate for developing a first-in-class anti-tubercular drug. [Display omitted] •DRILS-1398 is a 1st in class inhibitor of M.tb amino acid biosynthetic pathway•DRILS-1398 is effective against intracellular MDR-M.tb•Formulated DRILS-1398 elicits superior pharmacokinetics properties and efficacy•DRILS-1398 is safe, non-toxic, and well-tolerated in animal models Biological sciences; Medical Microbiology; Microbiology; Natural sciences; Pharmacology
AbstractList The search for new anti-tubercular agents is vital for the fight against , particularly given the rise of drug-resistant strains. DRILS-1398, a pyrazolo[4,3- ]pyrimidine derivative, was discovered as a potent inhibitor of chorismate mutase ( -CM) with an IC = 3.0 ± 0.2 M ( = 3) and IC = 10 M. The compound demonstrated efficacy against multi-drug resistant strains (MIC = 4 μg/mL, ∼10.0 μM) and effective inhibition of intracellular in THP-1 macrophages. With favorable pharmacokinetics, moderate stability , and a promising safety profile, DRILS-1398 showed no toxicity at doses up to 500 mg/kg b.w./day when dosed orally daily once for 7 consecutive days in mice. Both DRILS-1398 and its formulation DRILS-1398(F) were successful in clearing infection from the lungs and spleen in murine models. These findings suggest DRILS-1398 as a promising lead candidate for developing a first-in-class anti-tubercular drug.
The search for new anti-tubercular agents is vital for the fight against Mycobacterium tuberculosis, particularly given the rise of drug-resistant strains. DRILS-1398, a pyrazolo[4,3-d]pyrimidine derivative, was discovered as a potent inhibitor of M.tb chorismate mutase (M.tb-CM) with an IC50 = 3.0 ± 0.2 μM (n = 3) and IC90 = 10 μM. The compound demonstrated efficacy against multi-drug resistant M.tb strains (MIC = 4 μg/mL, ∼10.0 μM) and effective inhibition of intracellular M.tb in THP-1 macrophages. With favorable pharmacokinetics, moderate stability in vitro, and a promising safety profile, DRILS-1398 showed no toxicity at doses up to 500 mg/kg b.w./day when dosed orally daily once for 7 consecutive days in mice. Both DRILS-1398 and its formulation DRILS-1398(F) were successful in clearing M.tb infection from the lungs and spleen in murine models. These findings suggest DRILS-1398 as a promising lead candidate for developing a first-in-class anti-tubercular drug.The search for new anti-tubercular agents is vital for the fight against Mycobacterium tuberculosis, particularly given the rise of drug-resistant strains. DRILS-1398, a pyrazolo[4,3-d]pyrimidine derivative, was discovered as a potent inhibitor of M.tb chorismate mutase (M.tb-CM) with an IC50 = 3.0 ± 0.2 μM (n = 3) and IC90 = 10 μM. The compound demonstrated efficacy against multi-drug resistant M.tb strains (MIC = 4 μg/mL, ∼10.0 μM) and effective inhibition of intracellular M.tb in THP-1 macrophages. With favorable pharmacokinetics, moderate stability in vitro, and a promising safety profile, DRILS-1398 showed no toxicity at doses up to 500 mg/kg b.w./day when dosed orally daily once for 7 consecutive days in mice. Both DRILS-1398 and its formulation DRILS-1398(F) were successful in clearing M.tb infection from the lungs and spleen in murine models. These findings suggest DRILS-1398 as a promising lead candidate for developing a first-in-class anti-tubercular drug.
The search for new anti-tubercular agents is vital for the fight against Mycobacterium tuberculosis, particularly given the rise of drug-resistant strains. DRILS-1398, a pyrazolo[4,3-d]pyrimidine derivative, was discovered as a potent inhibitor of M.tb chorismate mutase (M.tb-CM) with an IC50 = 3.0 ± 0.2 μM (n = 3) and IC90 = 10 μM. The compound demonstrated efficacy against multi-drug resistant M.tb strains (MIC = 4 μg/mL, ∼10.0 μM) and effective inhibition of intracellular M.tb in THP-1 macrophages. With favorable pharmacokinetics, moderate stability in vitro, and a promising safety profile, DRILS-1398 showed no toxicity at doses up to 500 mg/kg b.w./day when dosed orally daily once for 7 consecutive days in mice. Both DRILS-1398 and its formulation DRILS-1398(F) were successful in clearing M.tb infection from the lungs and spleen in murine models. These findings suggest DRILS-1398 as a promising lead candidate for developing a first-in-class anti-tubercular drug. [Display omitted] •DRILS-1398 is a 1st in class inhibitor of M.tb amino acid biosynthetic pathway•DRILS-1398 is effective against intracellular MDR-M.tb•Formulated DRILS-1398 elicits superior pharmacokinetics properties and efficacy•DRILS-1398 is safe, non-toxic, and well-tolerated in animal models Biological sciences; Medical Microbiology; Microbiology; Natural sciences; Pharmacology
The search for new anti-tubercular agents is vital for the fight against Mycobacterium tuberculosis, particularly given the rise of drug-resistant strains. DRILS-1398, a pyrazolo[4,3-d]pyrimidine derivative, was discovered as a potent inhibitor of M.tb chorismate mutase (M.tb-CM) with an IC50 = 3.0 ± 0.2 μM (n = 3) and IC90 = 10 μM. The compound demonstrated efficacy against multi-drug resistant M.tb strains (MIC = 4 μg/mL, ∼10.0 μM) and effective inhibition of intracellular M.tb in THP-1 macrophages. With favorable pharmacokinetics, moderate stability in vitro, and a promising safety profile, DRILS-1398 showed no toxicity at doses up to 500 mg/kg b.w./day when dosed orally daily once for 7 consecutive days in mice. Both DRILS-1398 and its formulation DRILS-1398(F) were successful in clearing M.tb infection from the lungs and spleen in murine models. These findings suggest DRILS-1398 as a promising lead candidate for developing a first-in-class anti-tubercular drug.
ArticleNumber 112537
Author Alam, Anwar
Bulusu, Gopalakrishnan
Siraj, Fouzia
Edwin, Rebecca Kristina
Agarwal, Mansi
Pal, Manojit
Ahmad, Farhan Jalees
Shenoy, Gautham G.
Kumar, Dhiraj
Singh, Lakshyaveer
Hasnain, Seyed Ehtesham
Biswas, Deepesh
Oruganti, Srinivas
Misra, Parimal
Kumar, K. Shiva
Ehtesham, Nasreen Zafar
Chakraborty, Sandipan
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Snippet The search for new anti-tubercular agents is vital for the fight against Mycobacterium tuberculosis, particularly given the rise of drug-resistant strains....
The search for new anti-tubercular agents is vital for the fight against , particularly given the rise of drug-resistant strains. DRILS-1398, a pyrazolo[4,3-...
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SubjectTerms Biological sciences
Medical Microbiology
Microbiology
Natural sciences
Pharmacology
Title Early preclinical development of Mycobacterium tuberculosis amino acid biosynthesis pathway inhibitor DRILS-1398 as a potential anti-TB drug
URI https://dx.doi.org/10.1016/j.isci.2025.112537
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