m. tuberculosis

Pyrazinamide (Pyrazinecarboxamide), an antimycobacterial, is utilized therapeutically as an antitubercular agent, which is a synthetic pyrazinoic acid amide derivative.

GSK572A is a novel and potent potent inhibitor of EchA6, which can be used to treat tuberculosis.

GSK2556286 (GSK286) is an orally active inhibitor of Mycobacterium tuberculosis (M. tuberculosis), effective against multidrug-resistant (MDR), extensively drug-resistant (XDR), and drug-sensitive (DS) strains. It inhibits the growth of human macrophages with an IC50 value of 0.07 μM.

Sodium 4-aminosalicylate dihydrate (4-Amino-salicylic acid sodium salt) is the sodium salt form of aminosalicylic acid, an analog of para-aminobenzoic acid (PABA) with antitubercular activity. Sodium 4-aminosalicylate dihydrate exerts its bacteriostatic activity against Mycobacterium tuberculosis by competing with PABA for enzymes involved in folate synthesis, thereby suppressing growth and reproduction of M. tuberculosis, eventually leading to cell death.

Lansoprazole sulfide (AG-177) is an active metabolite of Lansoprazole with similar activity.Lansoprazole is a proton pump inhibitor and antitubercular agent with an IC50= 0.59 µM against Mycobacterium tuberculosis.

sCNH240 (2-Fluoro-N-[3-(3-thienyl)-5-isoxazolyl]benzenesulfonamide) is a potential and selective Rv1625c Cya activator with good cell permeability and oral activity, IC90=1.24 μM in cholesterol-supplemented 7H12 medium against Mycobacterium tuberculosis (Mtb) H37Rv strain, and inhibition of CYP2C19, CYP2C9 and hERG channels.

C-215 is a novel inhibitor of mycobacterial membrane protein large 3 (MmpL3).

BM635 is an MmpL3 inhibitor with outstanding anti-mycobacterial activity (MIC50: 0.12 μM against M. tuberculosis H37Rv).

BM635 hydrochloride is an MmpL3 inhibitor with outstanding anti-mycobacterial activity (MIC50: 0.12 μM against M. tuberculosis H37Rv).

BM635 mesylate is an MmpL3 inhibitor with outstanding anti-mycobacterial activity (MIC50: 0.12 μM against M. tuberculosis H37Rv).

CRS400393 is an effective anti-mycobacterial drug , with MIC of 0.03, 2, and ≤ 0.12 µg mL against M. abs., M. avium, M. intracellulare, and M. tuberculosis, respectively.

Norverapamil hydrochloride (D591 hydrochloride) ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

WAY-299801 is an antibacterial compound that demonstrates significant antimycobacterial activity against various Mycobacterium strains and clinically isolated M. tuberculosis in vitro.

Pks13-IN-1 (Compound 44) is an orally active inhibitor of Mycobacterium tuberculosis polyketide synthase 13 (Pks13). It inhibits the M. tuberculosis H37Rv strain with a minimum inhibitory concentration (MIC) of 0.07 μM. In mouse models, Pks13-IN-1 demonstrates antibacterial activity.

SMARt751 targets the transcriptional regulator VirS, inhibiting its ability to bind DNA, which in turn enhances the expression of the mymA operon and activates Ethionamide. This activation increases the antimicrobial efficacy of Ethionamide against Mycobacterium tuberculosis, and overcomes its resistance. Furthermore, SMARt751 augments Ethionamide's antibacterial activity in mouse models and reduces its effective dose. Additionally, SMARt751 can permeate the blood-brain barrier.

Mitonafide (NSC-300288) suppresses the activity of M. tuberculosis NAD+ dependent DNA ligase A. Mitonafide is a DNA intercalating agent.

DprE1-IN-377790 is a novel DprE1 inhibitor, killing M. tuberculosis.

Q-203 Ditosylate, also known as Q-203, is a mycobacterium tuberculosis protein potentially for the treatment of tuberculosis. The optimized IPA compound Q203 inhibited the growth of MDR and XDR M. tuberculosis clinical isolates in culture broth medium in

A039 is a highly active bactericidal agent against M. tuberculosis.

Beauvericin A is a cyclodepsipeptide and derivative of beauvericin originally isolated fromB. bassianathat has diverse biological activities.1,2,3It is active againstM. tuberculosis(MIC = 25 μg/ml) andP. falciparum(IC50= 12 μg/ml).2Beauvericin A is toxic to brine shrimp (LD100= 32 μg/ml).3 1.Gupta, S., Montillor, C., and Hwang, Y.-S.Isolation of Novel Beauvericin Analogues from the Fungus Beauveria bassianaJ. Nat. Prod.58(5)733-738(1995) 2.Nilanonta, C., Isaka, M., Kittakoop, P., et al.Antimycobacterial and antiplasmodial cyclodepsipeptides from the insect pathogenic fungus Paecilomyces tenuipes BCC 1614Planta Med.66(8)756-758(2000) 3.Shi, S., Li, Y., Ming, Y., et al.Biological activity and chemical composition of the endophytic fungus Fusarium sp. TP-G1 obtained from the root of Dendrobium officinale Kimura et MigoRec. Nat. Prod.12(6)549-556(2018)

Dimethyldioctadecylammonium (DDA) is a cationic amphipathic lipid. DDA liposomes containing an Ag85B-ESAT-6 antigen induce antigen deposition at an intramuscular or subcutaneous injection site in mice, increasing immune cell exposure to the antigen. In a guinea pig model of M. tuberculosis infection, spleen bacterial load is reduced and lung and spleen lesion numbers are decreased when the mycobacterial lipid antigens Ac2SGL and PIM2 are administered in liposomes comprised of DDA and a synthetic analog of the mycobacterial cord factor trehalose 6,6-dibehenate (TDB). DDA has also been used in the study of lipid bilayer dynamics.

Nornidulin is a depsidone originally isolated from [A. nidulans] with antibacterial activity against [M. tuberculosis] and [M. ranoe], and antifungal activity against [T. tonsurans] and [M. audouini]. It inhibits the growth of methicillin-resistant [S. aureus] (MRSA; MIC = 2 μg ml) and has larvicidal activity toward Artemia (LC50 = 1.7 μg ml). Nornidulin exhibits cytotoxic activity in MOLT-3 cells (IC50 = 35.7 μM) but not in HuCCA-1, HepG2, or A549 cells (IC50s = >116.4 μM).

3-hydroxy Myristic acid methyl ester is a hydroxylated fatty acid methyl ester that has been found in E. camaldulensis and E. torelliana extracts. [1] It is active against M. tuberculosis (MIC = 49.5 μg ml) and is non-cytotoxic to Vero cells (IC50 = >100 μM). 3-hydroxy Myristic acid methyl ester is also a volatile compound that contributes to the aroma of red wild strawberries (F. pentaphylla) but is not present in cultivated strawberries (Fragaria x ananassa).[2] Reference:[1]. Lawal, T.O., Adeniyi, B.A., Adegoke, A.O., et al. In vitro susceptibility of Mycobacterium tuberculosis to extracts of Eucalyptus camaldulensis and Eucalyptus torelliana and isolated compounds. Pharm. Biol. 50(1), 92-98 (2012).[2]. Duan, W., Sun, P., Chen, L., et al. Comparative analysis of fruit volatiles and related gene expression between the wild strawberry Fragaria pentaphylla and cultivated Fragaria × ananassa. Eur. Food Res. Technol. 244(1), 57-72 (2018).

Chevalone C is a meroterpenoid fungal metabolite originally isolated from E. chevalieri. It is active against M. tuberculosis H37Ra (MIC = 6.3 μg/ml) and is cytotoxic to BC1 human breast cancer cells (IC50 = 8.7 μg/ml). Chevalone C inhibits the growth of multidrug-resistant isolates of E. coli, S. aureus, and E. faecium in a disc diffusion assay when used at a concentration of 15 μg/disc. It also induces cell death in HCT116 colorectal carcinoma cells.