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Tuberculosis inhibitor 4 (compound 16), a mandelic acid-based spirothiazolidinone, has potent antimycobacterial activity against Mycobacteriumtuberculosis strain H37Rv with the high inhibition value 98% at lower than 6.25 µg/mL concentration .
UH-NIP-16 exhibits antimicrobial activity against Mycobacteriumtuberculosis, with MIC50 of 1.86 and 3.05 μM, for pathogenic mycobacterial strains H37Rv and CDC1551. UH-NIP-16 synergizes with Streptomycin (HY-B1906), Isoniazid (HY-B0329), Ethambutol (HY-B0535) and Bedaquiline (HY-14881), potentiates their anti-tuberculosis activities .
VEGFR-2/InhA-IN-1 is a pyrazole-based dual inhibitor of InhA-VEGFR with anti-tuberculosis and anti-angiogenic activities. VEGFR-2/InhA-IN-1 has good antibacterial activity against MycobacteriumtuberculosisH37Rv strain (MIC=6.25 μg/mL) and significantly inhibits VEGFR-2 (IC50=15.27 nM) .
MptpB-IN-2 (compound 20) is a selective mycobacteriumtuberculosis protein tyrosine phosphatase B (MptpB) inhibitor with IC50s of 0.64 μM, 4.06 μM and 4.14 μM for MptpB, MptpA and PTP1B, respectively. MptpB-IN-2 shows weak antituberculosis activity with a MIC of 64.9 μM for Mtb H37Rv .
BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosisH37Rv and Mycobacterium smegmatis, respectively.
Telacebec (Q203) is a midazopyridine amide compound. Telacebec is active against MycobacteriumtuberculosisH37Rv with an MIC50 of 2.7 nM in culture broth medium.
Telacebec ditosylate is a midazopyridine amide compound. Telacebec ditosylate is active against MycobacteriumtuberculosisH37Rv with an MIC50 of 2.7 nM in culture broth medium.
DL-Syringaresinol ((±)-Syringaresinol), a lignin, inhibits UVA-induced upregulation of MMP-1 by suppressing MAPK/AP-1 signaling in human HaCaT keratinocytes and dermal fibroblasts (HDFs). DL-Syringaresinol has antiphotoaging properties against UVA-induced skin aging. DL-Syringaresinol exhibits weak antimycobacterial activity against MycobacteriumtuberculosisH37Rv .
Thiocarlide is a potent antibacterial agent. Thiocarlide inhibits MycobacteriumtuberculosisH37Rv, Mycobacterium bovisBCG, Mycobacterium avium, and Mycobacterium aurum A+ with MICs of 2.5, 0.5, 2.0 and 2.0 μg/mL, respectively .
NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent MycobacteriumtuberculosisH37Rv.
The minimum inhibitory concentration (MIC) of a new 2- (quinoline-4-methoxy) acetamide antituberculotic agent against the reference strain of MycobacteriumtuberculosisH37Rv was as low as 0.3 μ M. It also inhibited the growth of Mycobacteriumtuberculosis in the macrophage model of tuberculosis infection.
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of MycobacteriumtuberculosisH37Rv with a MIC value of 0.1 μg/mL .
Mtb-IN-8 (compound 5jb) is an orally active inhibitor of Mycobacteriumtuberculosis (Mtb) with MIC values of 0.03 μg/mL for H37Rv and 0.125-0.06 μg/mL for MDR-Mtb, respectively .
MtInhA-IN-1 is a selective and orally active Mycobacteriumtuberculosis NADH-dependent enoyl-acyl carrier protein reductase (MtInhA) inhibitor with an IC50 of 0.23 μM. MtInhA-IN-1 potently against M. tuberculosisH37Rv strain with a MIC value of 0.4 μM .
Anti-infective agent 8 (compound 9d) is an antibacterial agent with an MIC of 0.5 μg/mL against Staphylococcus aureus and MycobacteriumtuberculosisH37Rv. Anti-infective agent 8 has anti-biofilm activity and significantly reduces Staphylococcus aureus biofilm formation .
MtTMPK-IN-1 (compound 3) is a potent Mycobacteriumtuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 2.5 μM. MtTMPK-IN-1 has moderate to weak activity against MtbH37Rv and low cytotoxicity in human fibroblast cells MRC-5. MtTMPK-IN-1 can be used for researching tuberculosis .
Amycolatopsin A is a 20-membered macrolide, that can be isolated from a strain of the rare actinomycete Amycolatopsis sp. MST‐108494. Amycolatopsin A shows antimycobacterial activity against Mycobacterium bovis (BCG) and M. tuberculosis (H37Rv) with IC50 values of 0.4 µM and 4.4 µM, respectively .
2-Mercaptopyridine N-oxide sodium has bactericidal effect and is against a standard strain of MycobacteriumtuberculosisH37Rv (ATCC 27294) with MIC90 of 7.20 μM. 2-Mercaptopyridine N-oxide sodium and its complex with iron, gallium, and bismuth have good anti-M. tuberculosis activity. 2-Mercaptopyridine N-oxide sodium has potential for the treatment of tuberculosis .
Mtb-IN-2 (compound 10c) is an antimicrobial agent against Mycobacteriumtuberculosis (Mtb), without cytotoxicity. Mtb-IN-2 significantly decreases colony-forming units (CFU) in spleen of murine tuberculosis models, and distinguishes both drug-sensitive and drug-resistant Mtb H37Rv strains. Mtb-IN-2 affects methionine metabolism but not folate pathway directly.
Mt KARI-IN-2 (compound 5b) is a potent Mycobacteriumtuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 2.02 μM. Mt KARI-IN-2 has inhibitory activity against MtbH37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 86 μg/mL) .
Mt KARI-IN-4 (compound 5c) is a potent Mycobacteriumtuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 5.48 μM. Mt KARI-IN-4 has inhibitory activity against MtbH37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 72 μg/mL) .
Mt KARI-IN-5 (compound 6c) is a potent Mycobacteriumtuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 4.72 μM. Mt KARI-IN-5 has inhibitory activity against MtbH37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC50 > 64 μg/mL)
Antimycobacterial agent-2 (compound 58) is a potent antimycobacterial agent. Antimycobacterial agent-2 shows anti-mycobacterial activities with an MIC99 of 0.8 µM for Mycobacteriumtuberculosis (M.tb) H37Rv. Antimycobacterial agent-2 shows cytotoxic activities with an IC50 of48.1 µM for CHO cells .
ATP synthase inhibitor 3 (compound PT6) is an orally active inhibitor of mycobacterial F-ATP synthase (IC50=0.788 μM). ATP synthase inhibitor 3 inhibits the growth of MycobacteriumtuberculosisH37Rv strain (ATCC-27294) in vitro and depletes intracellular ATP levels at an IC50 value of 30μM .
4-Allylcatechol (4-Allylpyrocatechol) is a xylan isolated from the root of Piper taiwanense. 4-Allylcatechol has a strong inhibitory activity against collagen-induced platelet aggregation (IC50=5.3 μM). In addition, 4-Allylcatechol has anti-tuberculosis activity against MycobacteriumtuberculosisH37Rv (MIC=27.6 μg/mL) .
(24S)-Cycloartane-3β,24,25-triol, a cycloartane, has antitubercular activity against MycobacteriumtuberculosisH37Rv (MIC: 32 μg/mL). (24S)-Cycloartane-3β,24,25-triol can be isolated from the flowers of Chrysanthemum morifolium .
Antimycobacterial agent-6 (compound 25) is a potent inhibitor of Mycobacteriumtuberculosis (Mtb)，targeting to both wild-type and fluoroquinolone-resistant Mtb strains. Antimycobacterial agent-6 inhibits Mtb DprE1-C387S mutant with MIC90s of 0.9 μM (H37Rv)，0.9 μM (MoxR)，0.5 μM (DprE1-P116S)，respectively .
MtTMPK-IN-2 (compound 15) is a potent Mycobacteriumtuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 1.1 μM. MtTMPK-IN-2 has inhibitory activity against MtbH37Rv (MIC = 12.5 μM). MtTMPK-IN-2 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 6.1 μM). MtTMPK-IN-2 can be used for researching tuberculosis .
MtTMPK-IN-3 (compound 25) is a potent Mycobacteriumtuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 0.12 μM. MtTMPK-IN-3 has inhibitory activity against MtbH37Rv (MIC = 12.5 μM). MtTMPK-IN-3 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 12.5 μM). MtTMPK-IN-3 can be used for researching tuberculosis .
Antitubercular agent-28 (compound 2) is a potent antitubercular agent with an IC50 value of 1.5 µM, an MIC value of 4.5 µM, an IC90 value of 2.5 µM. Antitubercular agent-28 shows antimycobacterial activity for resistant isolates of MycobacteriumtuberculosisH37Rv. Antitubercular agent-28 shows effective intracellular antimycobacterial activity and low cytotoxicity .
Antitubercular agent-27 (compound 1) is a potent antitubercular agent with an IC50 value of 3.2 µM, an MIC value of 7.8 µM, an IC90 value of 7.0 µM. Antitubercular agent-27 shows antimycobacterial activity for resistant isolates of MycobacteriumtuberculosisH37Rv. Antitubercular agent-27 shows effective intracellular antimycobacterial activity and low cytotoxicity .
CYP121A1-IN-1 is a potent CYP121A1 inhibitor with favorable activity against Mycobacteriumtuberculosis (H37RvMIC90∼6.25 μM, ∼2.2 μg/mL). CYP121A1-IN-1 can markedly reduce the production of mycocyclosin via inhibiting the CYP121A1 mediated turnover of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin .
Antibacterial agent 228 (Compound 8) inhibits the mycobacterial ribosome (IC50 for Mycobacterium smegmatis is 2.31 μM) and exhibits antibacterial activity against M. tuberculosisH37Rv (MIC=2 and 0.25 μg/mL for wildtype and Δ1258c mutant), M. abscessus ATCC 19977 (MIC=8 and 8 μg/mL for wildtype and Δ2780c mutant) and M. smegmatis (MIC=8 μg/mL) .
I-A09 and its derivatives, specifically 1,2,3-triazole-adamantylacetamide hybrids (5a–u), exhibit significant antitubercular activity. These hybrids were synthesized using copper-catalyzed click chemistry, combining bioactive fragments from antitubercular I-A09 and substituted adamantyl urea. The compound N-(1-adamantyl)-2-azido acetamide was reacted with various alkyl/aryl acetylenes to produce new analogues. Among them, N-(1-adamantan-1-yl)-2-(4-(phenanthren-2-yl)-1H-1,2,3-triazol-1-yl)acetamide (5t) showed the most promise with a minimum inhibitory concentration (MIC) of 3.12 μg/mL against MycobacteriumtuberculosisH37Rv, and a selectivity index greater than 15 .
Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 11 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 11 can be used for tuberculosis (TB) research .
Anti-inflammatory agent 15 (compound 29) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 15 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 2.3 and 7.8 μM, respectively. Anti-inflammatory agent 15 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 15 can be used for tuberculosis (TB) research .
4-Allylcatechol (4-Allylpyrocatechol) is a xylan isolated from the root of Piper taiwanense. 4-Allylcatechol has a strong inhibitory activity against collagen-induced platelet aggregation (IC50=5.3 μM). In addition, 4-Allylcatechol has anti-tuberculosis activity against MycobacteriumtuberculosisH37Rv (MIC=27.6 μg/mL) .
DL-Syringaresinol ((±)-Syringaresinol), a lignin, inhibits UVA-induced upregulation of MMP-1 by suppressing MAPK/AP-1 signaling in human HaCaT keratinocytes and dermal fibroblasts (HDFs). DL-Syringaresinol has antiphotoaging properties against UVA-induced skin aging. DL-Syringaresinol exhibits weak antimycobacterial activity against MycobacteriumtuberculosisH37Rv .
Amycolatopsin A is a 20-membered macrolide, that can be isolated from a strain of the rare actinomycete Amycolatopsis sp. MST‐108494. Amycolatopsin A shows antimycobacterial activity against Mycobacterium bovis (BCG) and M. tuberculosis (H37Rv) with IC50 values of 0.4 µM and 4.4 µM, respectively .
(24S)-Cycloartane-3β,24,25-triol, a cycloartane, has antitubercular activity against MycobacteriumtuberculosisH37Rv (MIC: 32 μg/mL). (24S)-Cycloartane-3β,24,25-triol can be isolated from the flowers of Chrysanthemum morifolium .
