Antimycobacterial agent-4 (4-nitro-N-[4-(2-pyridyl)thiazol-2-yl]benzamide) has antibacterial activity against Mycobacterium tuberculosis.

Antimycobacterial agent-3 is an antimycobacterial agent with low cytotoxicity. antimycobacterial agent-3 is effective against sensitive MTB strain H37Rv and resistant clinical isolates (MIC < 0.029-0.110 μ M).

Antimycobacterial agent-1 (compound 33) demonstrates potent antimycobacterial activity against Mycobacterium tuberculosis H37Ra, with a minimal inhibitory concentration (MIC) value of 1 μg/ml. Notably, antimycobacterial agent-1 exhibits low cytotoxicity in normal cells, as evidenced by an IC50 value of 143.2 μg/ml in Vero cells [1].

Antimycobacterial agent-6 (compound 25) effectively inhibits Mycobacterium tuberculosis, including wild-type and fluoroquinolone-resistant strains, by targeting the Mtb DprE1-C387S mutant. It displays minimal inhibitory concentrations (MIC90) of 0.9 μM for H37Rv and MoxR strains, and 0.5 μM for the DprE1-P116S strain [1].

Antimycobacterial agent-2 is an effective anti-mycobacterial agent with a MIC99 of 0.8 μM against Mycobacterium tuberculosis (M.tb) H37Rv. Antimycobacterial agent-2 is cytotoxic, acting on CHO cells (IC50: 48.1 μM).

Linaroside exhibited 30% inhibition for antimycobacterial activity against Mycobacterium tuberculosis, strain H(37)Rv at 6.25 microg mL(-1) concentration.

Azadiradione (AZD) (AZD) from the methanolic extract of seeds of Azadirachta indica

Tuberculosis Inhibitor 10 moderately inhibits the enzyme MSMEG_6649 and potentiates the antimycobacterial activity of PAS [1].

Calpinactam is a fungal metabolite originally isolated from M. alpina that has antimycobacterial activity. It is active against M. smegmatis (MIC = 0.78 μg/ml) but not a panel of 13 other bacteria and fungi. Calpinactam increases survival in a silkworm model of M. smegmatis infection (ED50 = 5 μg/larva).

25-Desacetyl rifampicin is a major active metabolite of the rifamycin antibiotic rifampicin .125-Desacetyl rifampicin is active againstM. smegmatis(MIC99= 2.66 μM). 1.Kigondu, E.M., Njoroge, M., Singh, K., et al.Synthesis and synergistic antimycobacterial screening of chlorpromazine and its metabolitesMed. Chem. Commun.5502-506(2014)

BM212 is an antimycobacterial compound.It inhibits the growth of laboratory and clinical isolate M. tuberculosis strains.

Amycolatopsin A is a macrolide polyketide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 0.4 and 4.4 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin A is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 0.08 and 1.2 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

5,6-Desmethylenedioxy-5-methoxyaglalactone is cytotoxic to small cell lung cancer (NCI-H187) cell line. It has antimycobacterial activity against Mycobacterium tuberculosis H(37)Ra.

2-Desoxy-4-epi-pulchellin has potent in vitro cytotoxicities against the K562, MCF-7, Hela, DU145, U937, H1975, SGC-7901, A549, MOLT-4, and HL60 cell lines with IC50 values ranging from 0.10 to 46.7uM, while it shows significant antiviral (H1N1 and H3N2) activities, it also displays significant antimycobacterial activity (IC50=7.6 uM).

Cabraleahydroxylactone displays antimycobacterial activity against Mycobacterium tuberculosis, it is weakly cytotoxic to a breast cancer (BC) cell line.It shows antiviral activity against herpes simplex virus type-1 with an IC50 value of 3.20 ug/mL, in comparison with the standard acyclovir (IC50=1.90ug/mL).

Compound 14, also known as Tuberculosis Inhibitor 11, enhances the antimycobacterial efficacy of antitubercular agent [1].

Lariatin A is an antimycobacterial lasso peptide originally isolated from R. jostii. It is active against M. tuberculosis and M. smegmatis in vitro (MICs = 0.39 and 0.1 μg/ml, respectively). Lariatin A increases survival in a silkworm model of M. smegmatis infection (ED50 = 0.5 μg/g).

AB131, an inhibitor of MSMEG 6649 and Rv2172c (KD values of 0.16 and 0.02 μM, respectively), enhances the antimycobacterial efficacy of the antitubercular agent [1].

Amycolatopsin B is a bacterial metabolite originally isolated fromAmycolatopsisthat has anticancer activity.1It is cytotoxic to NCI H460 lung and SW620 colon cancer cells (IC50s = 0.28 and 0.14 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

Thiocarlide (isoxyl) is a thiourea derivative that was used in the 1960s to successfully treat tuberculosis (TB). It has considerable antimycobacterial activity in vitro and is effective against multi-drug resistant strains of Mycobacterium tuberculosis in the range of 1-10 µg/ml. [1] [2] At concentrations of 10 µM, isoxyl inhibits the synthesis of M. bovis during six hours of exposure which is similar to isoniazid (INH) and ethionamide (ETH), two other predominant anti-tuberculosis drugs. Unlike INH and ETH, isoxyl also partially inhibits the synthesis of fatty acids. Isoxyl shows no acute toxicity against primary macrophage cell cultures as demonstrated by diminution of redox activity.[2]

Goniotriol shows antimycobacterial activity against Mycobacterium tuberculosis (MIC =100 microg/mL). It exhibits antiplasmodial activity against Plasmodium falciparum (IC50=2.6 microg/mL). Goniotriol shows cytotoxicity against cancer cells, KB, BC1, NCI-H

Dapsone (Sulphadione) has activity against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae.

I2906 showed antimycobacterial and cytotoxic activity against mycobacterium tuberculosis.

Methyl caffeate (Methyl caffeate acid) acid

PptT-IN-4 (Compound 3a) is a PptT inhibitor exhibiting an IC50 of 0.71 μM. It also demonstrates antimycobacterial activity against Mtb H37Rv, with a MIC of 42 μM, and inhibits hERG, hCav1.2, and hNav1.5 channels with IC50 values of 11 μM, 8.1 μM, and 6.9 μM, respectively [1].

Griselimycin is a natural antimycobacterial product that is currently being pursued as a therapy for tuberculosis.

Ethambutol-d8 is a deuterated compound of Ethambutol. Ethambutol has a CAS number of 74-55-5. Ethambutol is a bacteriostatic antimycobacterial agent obstructed the formation of cell wall by inhibiting arabinosyl transferases.

Antituberculosis agent-7, an oxetanyl-quinoline derivative, exhibits potent antibacterial activity against P. mirabilis, with a minimum inhibitory concentration (MIC) of 31.25 μM, and antifungal efficacy against A. niger, with a MIC of 62.5 μM. Furthermore, it demonstrates remarkable antimycobacterial activity, achieving a MIC of 3.41 μM against M. tuberculosis H37Rv [1].

Ganorbiformin B, a lanostane triterpenoid, belongs to the same structural class as ganoderic acids, sharing the lanostane skeleton. It is the C-3 epimer of ganoderic acid T, known for its potent antimycobacterial activity against Mycobacterium tuberculosis H37Ra [1].

Tuberculosis inhibitor 5 (Compound 11i) is a potent anti-tuberculosis agent with no apparent cytotoxicity. tuberculosis inhibitor 5 is an antimycobacterial biphenyl analogue.

Tuberculosis inhibitor 4 (compound 16) is a spirothiazolidinone based on mandelic acid that exhibits potent antimycobacterial action. The inhibitor inhibited 98% of Mycobacterium tuberculosis strain H37Rv at concentrations below 6 μg mL.

BRD-8000.3 is a narrow-spectrum, bactericidal antimycobacterial agent known for its specific inhibition of EfpA. It exhibits potent activity against wild-type strains and proves to be a valuable tool in tuberculosis research[1].

Tetrahdroxysqualene shows antimycobacterial activity with an MIC of 10.0 microg/mL, while showing only modest cytotoxicity.

Rifabutin (LM-427) inhibits bacterial DNA-dependent RNA polymerase, thereby suppressing the initiation of RNA formation and leading to inhibition of RNA synthesis and transcription. Rifabutin is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties.

Evocarpine shows antimycobacterial, and vasorelaxant effects, it can inhibit Ca2+ influx through voltage-dependent calcium channels.

DprE1-IN-9 (compound B18) is an efficient reversible inhibitor of DprE1, interacting with the enzyme's receptor cavity. It exhibits potent antimycobacterial properties, demonstrating activity against both non-pathogenic H37Ra (MIC=0.18 µg/mL) and pathogenic strains, including H37Rv, as well as clinical MDR and XDR isolates [1].

Antituberculosis agent-6 is a potent antimycobacterial and antifungal compound with significant activity against M. tuberculosis (MIC of 3.49 μM) and A. niger (MIC of 62.50 μM), respectively. It also demonstrates high gastrointestinal (GI) absorption.

Anti-infective agent 1 (compound 3a) serves as a potent, selective antiprotozoal and antimycobacterial compound. It showcases antiparasitic efficacy against P. falciparum and T. brucei rhodesiense, demonstrating IC50 values of 10.95 and 0.06 μM, respectively. Moreover, it displays antimycobacterial properties against Mycobacterium smegmatis, exhibiting a minimum inhibitory concentration (MIC) of 8 μg/mL [1].

ISOBERGAPTEN is a plant growth regulating substance, it is the principal constituents responsible for the antimycobacterial activity of the roots of Heracleum maximum; it may form an important class of natural defensive agents against fungi.

CBR-6672, a type II NADH dehydrogenase inhibitor, demonstrates potent antimycobacterial activity against mycobacterium tuberculosis (Mtb) with a minimum inhibitory concentration (MIC) of 0.14 μM [1].

Kahalalide A has antimycobacterial activity isolated from the mollusk Elysia rufescens.

Antitubercular agent-28 (compound 2) has antimycobacterial activity for resistant isolates of Mycobacterium tuberculosis H37Rv. Antitubercular agent-28 is a potent antitubercular agent with an MIC value of 4.5 μM, an IC 50 value of 1.5 μM, and an IC 90 value of 2.5 μM. Antitubercular agent-28 shows effective intracellular antimycobacterial activity with low cytotoxicity [1].

Antibacterial agent 118 (also known as compound 20) is a potent antimycobacterial compound with activity against various mycobacterial strains, including Mtb H37Ra, M. aurum, M. smegmatis, Mtb H37Rv, and M. avium. The minimum inhibitory concentration (MIC) values for Antibacterial agent 118 against these strains are 40.7 μM, 10.2 μM, 163.0 μM, 62.5 μM, and 62.5 μM, respectively. This compound holds potential for tuberculosis research [1].

DprE1-IN-7 (Compound 64) is a DprE1 inhibitor with potent anti-tuberculosis (TB) activity, demonstrating a minimum inhibitory concentration (MIC) of 1 μM against the Mtb H37Rv strain. It exhibits antimycobacterial effects on drug-resistant strains. Additionally, DprE1-IN-7 shows high microsomal stability and exhibits medium clearance [1].

IpOHA is a potent inhibitor of plant KARI and functions as an antimycobacterial agent, demonstrating a K_i value of 97.7 nM against Mycobacterium tuberculosis (Mt) [1].

Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial agent that can be used in the research of tuberculosis(TB). Anti-inflammatory agent 11 inhibits the growth of Mtb H37Rv and M299 with MIC 50 of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 is also an anti-inflammatory agent that inhibits NO through the suppressing expression of iNOS and also inhibited the production of TNF-α and IL-1β [1].

Anti-infective agent 2 (compound 3k) is an antiprotozoal and antimycobacterial agent. Anti-infective agent 2 exhibits antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC 50 values of 0.07 and 2.20 μM, respectively. Anti-infective agent 2 exhibits antimycobacterial activity against Mycobacterium smegmatis with a MIC of 32 μg/mL [1].

Antitubercular agent-27 (compound 1) exhibits potent antitubercular properties, demonstrated by an IC50 of 3.2 μM, an MIC of 7.8 μM, and an IC90 of 7.0 μM. It effectively targets resistant Mycobacterium tuberculosis H37Rv isolates, displaying significant intracellular antimycobacterial activity with low cytotoxicity [1].

Antitubercular agent-18 (Compound 9a) is an antitubercular agent that exhibits highly selective antimycobacterial effects, with minimum inhibitory concentration (MIC) values of 2 μg/ml against M. tuberculosis H37Rv, Spec. 192, and Spec. 210, and 128 μg/ml against Spec. 800, demonstrating its efficacy in inhibiting the growth of these mycobacterial strains [1].

Cabraleadiol displays antimycobacterial activity against Mycobacterium tuberculosis, it also is weakly cytotoxic to a breast cancer (BC) cell line. Cabraleadiol inhibits photosystem II (PS II) and induces the appearance of small G band which is related wi