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Antitubercular agent-24 (Compound 1) is an anti-tubercular agent with an extracellular IC50 of 0.83 μM and an intracellular IC50 of 0.17 μM against M. tuberculosisH37Rv .
Antituberculosis agent-3 (Compound 2) is an antituberculosis agent. Antituberculosis agent-3 shows anti-mycobacterial activity, and can inhibit M. tuberculosisH37Rv strain growth (MIC=12.5 μg/mL) .
Antitubercular agent-31 (Compound 2) is an antitubercular agent with an MIC of 0.03 μM against M. tuberculosisH37Rv. Antitubercular agent-31 also inhibits DprE1 with an IC50 of 1.1 μM .
Antitubercular agent-13 (Compound 3d) is an antitubercular agent with MIC values of 0.007 µg/mL and 1.851 µg/mL against MTB H37Rv and MDR-MTB 16833, respectively. Antitubercular agent-13 shows metabolic instability .
Tuberculosis inhibitor 4 (compound 16), a mandelic acid-based spirothiazolidinone, has potent antimycobacterial activity against Mycobacterium tuberculosis strain H37Rv with the high inhibition value 98% at lower than 6.25 µg/mL concentration .
Antitubercular agent-25 (Compound 28) is an anti-tubercular agent with an extracellular IC50 of 0.42 μM and an intracellular IC50 of 0.20 μM against M. tuberculosisH37Rv. Antitubercular agent-25 exhibits good metabolic stability .
PknB-IN-1 (Compound 2) is a protein kinase B (PknB) inhibitor (IC50=14.4 μM). PknB-IN-1 shows anti-mycobacterial activity, can inhibit M. tuberculosisH37Rv strain growth (MIC=6.2 μg/mL) .
Antitubercular agent-39 (Compound P1) is a potent antitubercular agent. Antitubercular agent-39 is active against drug-resistant strains and drug-susceptible clinical isolates. Antitubercular agent-39 inhibits Mtb strain H37Rv with a MIC less than 1 μM .
HT1171 is a potent and selective inhibitor of mycobacterium tuberculosis proteasome. HT1171 shows strong anti-tuberculosis activity against Mycobacterium tuberculosisH37Rv with an MIC90 of 2 μg/mL and an MIC of 4 μg/mL. When HT1171 concentration is 100 μM, the inhibition rate of human normal hepatocytes L02 is 53.8%. HT1171 can be used in the research of antitubercular agent .
BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.
Telacebec (Q203) is a midazopyridine amide compound. Telacebec is active against Mycobacterium tuberculosisH37Rv with an MIC50 of 2.7 nM in culture broth medium.
Telacebec ditosylate is a midazopyridine amide compound. Telacebec ditosylate is active against Mycobacterium tuberculosisH37Rv with an MIC50 of 2.7 nM in culture broth medium.
MtTMPK-IN-1 (compound 3) is a potent Mycobacterium tuberculosis 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 .
NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosisH37Rv.
Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice .
Antituberculosis agent-8 (Compound 9i) is an antitubercular agent with an MIC of 3.53 μM (1.6 μg/mL) against M. tuberculosis H37Rv. Antituberculosis agent-8 also shows good antifungal activity against A. niger with an MIC of 62.50 μM .
Antitubercular agent-26 (Compound 32) is an orally active anti-tubercular agent with an extracellular IC50 of 0.50 μM and an intracellular IC50 of 0.51 μM against M. tuberculosisH37Rv. Antitubercular agent-26 shows good metabolic stability, low risk of cardiotoxicity and no genotoxicity .
DprE1-IN-5 (Compound 10) is a DprE1 inhibitor. DprE1-IN-5 has anti-TB activity against Mtb H37Rv strain (MIC: 4 μM). DprE1-IN-5 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-5 has high microsomal stability .
DprE1-IN-7 (Compound 64) is a DprE1 inhibitor. DprE1-IN-7 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-7 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-7 has high microsomal stability and medium clearance .
DprE1-IN-6 (Compound 56) is a DprE1 inhibitor. DprE1-IN-6 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-6 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-6 has high microsomal stability and medium clearance .
Polyketide synthase 13-IN-3 (compound 41) is a polyketide synthase 13 inhibitor，with a MIC of 0.0625-0.125 μg/mL against the M. tuberculosis strain H37Rv .
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL .
(Rac)-Sativan is an isoflavanoid with a broad spectrum of antimicrobial activity against bacteria and phytopathogenic fungi. (Rac)-Sativan exhibits antituberculosis activity against Mycobacterium tuberculosisH37Rv, with MIC values of 50 µg/mL .
Antituberculosis agent-7, an oxetanyl-quinoline derivative, has shown good antibacterial activity against P. mirabilis with a MIC of 31.25 μM. Antituberculosis agent-7 shows good antifungal activity against A. niger with a MIC of 62.5 μM. Antituberculosis agent-7 shows excellent antimycobacterial activity with MIC 3.41 μM for M. tuberculosisH37Rv .
MtTMPK-IN-2 (compound 15) is a potent Mycobacterium tuberculosis 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 Mycobacterium tuberculosis 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 .
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 Mycobacterium tuberculosis H37Rv strain (MIC=6.25 μg/mL) and significantly inhibits VEGFR-2 (IC50=15.27 nM) .
UH-NIP-16 exhibits antimicrobial activity against Mycobacterium tuberculosis, 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 .
Antitubercular agent-23 (Compound 3a) is a potent anticandidiasis and antitubercular agent with MIC values of 1.1 µg/ml and 1 µg/ml against Candida albicans MTCC 3017 and M. tuberculosis(H37Rv), respectively .
Antitubercular agent-22 (Compound 2) is a potent anticandidiasis and antitubercular agent with MIC values of 2.34 µg/ml and 2 µg/ml against Candida albicans MTCC 3017 and M. tuberculosis(H37Rv), respectively .
Mtb-IN-8 (compound 5jb) is an orally active inhibitor of Mycobacterium tuberculosis (Mtb) with MIC values of 0.03 μg/mL for H37Rv and 0.125-0.06 μg/mL for MDR-Mtb, respectively .
DprE1-IN-11 (compound 3) is an orally active DprE1 inhibitor with antituberculosis activity against MTB H37Rv and MDR-MTB strains (MIC <0.029-0.095 μM) .
Thiocarlide is a potent antibacterial agent. Thiocarlide inhibits Mycobacterium tuberculosisH37Rv, Mycobacterium bovisBCG, Mycobacterium avium, and Mycobacterium aurum A+ with MICs of 2.5, 0.5, 2.0 and 2.0 μg/mL, respectively .
Antibacterial agent 129, an oxetanyl-quinoline derivative, has shown good antibacterial activity against P. mirabilis and B. subtilis with MICs of 31.25 μM and 31.5 μM and . Antibacterial agent 129 shows good antifungal activity against A. niger with a MIC of 31.25 μM. Antibacterial agent 129 shows excellent antimycobacterial activity with MIC 57.73 μM for M. tuberculosisH37Rv .
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 Mycobacterium tuberculosisH37Rv .
MptpB-IN-2 (compound 20) is a selective mycobacterium tuberculosis 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 .
Benzothiohydrazide is an analogue of anti–tubercular agent Isoniazid. Benzothiohydrazide exhibits anti–tubercular activity, with MICs of 132 μM and 264 μM for M. tuberculosis wild type (H37Rv) and clinical mutant strains (IC1 and IC2) .
DprE1-IN-8 is a potent DprE1 inhibitor with an IC50 value of <0.75 μM. DprE1-IN-8 is against Mtb H37Rv with an IC50 of 6 nM and can be used for tuberculosis research .
Mtb-IN-7 (compoun R7) is a MAO-A/MAO-B inhibitor with the IC50 values over 40 μM. Mtb-IN-7 shows antimycobacterial activity against M. tuberculosis H37Rv with the MIC of 2.01 μM .
DprE1-IN-9 (compound B18) is an effective reversible DprE1 inhibitor and can bind to the receptor cavity of DprE1. DprE1-IN-9 shows strong antimycobacterial activity not only against non-pathogenic strain H37Ra (MIC=0.18 µg/mL) but also against pathogenic H37Rv and the clinical MDR and XDR isolates .
DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of tuberculosis.
BM635 mesylate is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 mesylate has a MIC50 of 0.6 μM against M. tuberculosisH37Rv. BM635 mesylate significantly improves the bioavailability compared to free-base BM635 .
The minimum inhibitory concentration (MIC) of a new 2- (quinoline-4-methoxy) acetamide antituberculotic agent against the reference strain of Mycobacterium tuberculosis H37Rv was as low as 0.3 μ M. It also inhibited the growth of Mycobacterium tuberculosis in the macrophage model of tuberculosis infection.
Anti-infective agent 8 (compound 9d) is an antibacterial agent with an MIC of 0.5 μg/mL against Staphylococcus aureus and Mycobacterium tuberculosis H37Rv. Anti-infective agent 8 has anti-biofilm activity and significantly reduces Staphylococcus aureus biofilm formation .
BM635 hydrochloride is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 hydrochloride has an MIC50 of 0.08 μM against M.tuberculosisH37Rv. BM635 hydrochloride doubles the in vivo exposure with respect to the free base BM635 .
MtInhA-IN-1 is a selective and orally active Mycobacterium tuberculosis 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 .
Antitubercular agent-18 (Compound 9a) is an antitubercular agent with MIC values of 2, 2, 2 and 128 µg/ml against M. tuberculosisH37Rv, Spec. 192, Spec 210 and Spec. 800, respectively. Antitubercular agent-18 shows highly selective antimycobacterial effects .
Antitubercular agent-17 (Compound 8a) is an antitubercular agent with MIC values of 2, 2, 2 and 128 µg/ml against M. tuberculosisH37Rv, Spec. 192, Spec 210 and Spec. 800, respectively. Antitubercular agent-17 shows highly selective antimycobacterial effects .
Antibacterial agent 216 (Compound 2a) is an antibacterial agent that exhibits significant bactericidal effects when combined with INH and RIF. Antibacterial agent 216 has demonstrated remarkable in vitro anti-tuberculosis activity against Mtb H37Rv and MDR clinical isolates and can be used for tuberculosis research .
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 .
BM212 is a potent Mycobacterial membrane protein Large 3 (MmpL3) inhibitor. BM212 has strong bactericidal activity against both M. tuberculosis and some nontuberculosis mycobacteria. BM212 exhibits antimycobacterial activity against M. tuberculosisH37Rv with an MIC of 5 µM .
Antimycobacterial agent-6 (compound 25) is a potent inhibitor of Mycobacterium tuberculosis (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 .
Mt KARI-IN-2 (compound 5b) is a potent Mycobacterium tuberculosis 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 Mycobacterium tuberculosis 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 Mycobacterium tuberculosis 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)
Antitubercular agent-21 (Compound 15) is an antitubercular agent with an MIC of o.4 µg/mL against M. tuberculosisH37Rv. Antitubercular agent-21 exhibits lower activity against other microorganism such as bacteria gram-positive, gram-negative or fungi. Antitubercular agent-21 shows low cytotoxicity .
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 .
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 Mycobacterium tuberculosis (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 Mycobacterium tuberculosisH37Rv strain (ATCC-27294) in vitro and depletes intracellular ATP levels at an IC50 value of 30μM .
Pks13-IN-1 (Compound 44) is an orally active inhibitor for Mycobacterium tuberculosisPolyketide synthase 13 (Pks13). Pks13-IN-1 inhibits M. tuberculosis strain H37Rv with a MIC of 0.07 μM. Pks13-IN-1 exhibits antibacterial efficacy in mouse model .
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 μg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization .
Mtb-IN-2 (compound 10c) is an antimicrobial agent against Mycobacterium tuberculosis (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.
(24S)-Cycloartane-3β,24,25-triol, a cycloartane, has antitubercular activity against Mycobacterium tuberculosisH37Rv (MIC: 32 μg/mL). (24S)-Cycloartane-3β,24,25-triol can be isolated from the flowers of Chrysanthemum morifolium .
MmpL3-IN-3 (Compound 12) is a MmpL3 inhibitor. MmpL3-IN-3 shows a MIC of 0.1 μM against H37Rv. MmpL3-IN-3 shows good stability in mouse liver microsomes. MmpL3-IN-3 can be used for anti-tubercular research .
2-Mercaptopyridine N-oxide sodium has bactericidal effect and is against a standard strain of Mycobacterium tuberculosis H37Rv (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 .
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 Mycobacterium tuberculosis H37Rv. 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 Mycobacterium tuberculosis H37Rv. Antitubercular agent-27 shows effective intracellular antimycobacterial activity and low cytotoxicity .
Antibacterial agent 118 (compound 20) is an antimycobacterial agent. Antibacterial agent 118 shows antibacterial activity against Mtb H37Ra, M. aurum, M. smegmatis, Mtb H37Rv and M. avium with MIC values of 40.7, 10.2, 163.0, 62.5 and 62.5 μM, respectively. Antibacterial agent 118 can be used for the research of tuberculosis .
PptT-IN-4 (Compound 3a) is a PptT inhibitor (IC50: 0.71 μM). PptT-IN-4 inhibits MtbH37Rv with a MIC value of 42 μM. PptT-IN-4 also inhibits hERG, hCav1.2, and hNav1.5 channels with IC50s of 11 μM, 8.1 μM, 6.9 μM respectively .
4-Allylcatechol (4-Allylpyrocatechol) is a xylan which has oral activity and can be 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 Mycobacterium tuberculosis H37Rv (MIC = 27.6 μg/mL) .
CYP121A1-IN-1 is a potent CYP121A1 inhibitor with favorable activity against Mycobacterium tuberculosis (H37Rv MIC90∼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 73 (compound 7a) is a potent antimicrobial agent. Antibacterial agent 73 exhibits very good antitubercular activity (MIC=0.65 µg/mL) against Mtb H37Rv. Antibacterial agent 73 shows good activity against fungal and bacterial. Antibacterial agent 73 also shows cytotoxicity in MCF-7 breast cancer cell lines, with IC50 of 8.20 μM .
Antitubercular agent-15 (Compound 5n) is an antitubercular agent with MIC90 values of 0.73, 7.69, 9.38, 18.80, 7.53 and 7.31 μg/mL against M. tuberculosisH37Rv, CF16, CF61, CF76, CF152 and CF161, respectively. Antitubercular agent-15 shows low cytotoxicity against macrophages and pulmonary fibroblasts .
Antitubercular agent-16 (Compound 5q) is an antitubercular agent with MIC90 values of 0.40, 20.11, 23.51, 19.62, 10.93 and 13.62 μg/mL against M. tuberculosisH37Rv, CF16, CF61, CF76, CF152 and CF161, respectively. Antitubercular agent-16 shows low cytotoxicity against macrophages and pulmonary fibroblasts .
WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for agent susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM.
Antituberculosis agent-2 (Compound 8d) is an antituberculosis agent against agent-sensitive and multidrug-resistant tuberculosis. Antituberculosis agent-2 shows anti-tuberculosis activity with MIC values of 0.454, 1.757 and 1.644 μg/mL against M. tuberculosisH37Rv, 13946 and 14862, respectively. Antituberculosis agent-2 displays favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability .
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 Mycobacterium tuberculosis H37Rv, and a selectivity index greater than 15 .
Antimycobacterial agent-4 is a 2-amino-4-(2-pyridyl) thiazole derivative, with antimycobacterial activity, antiplasmodial activity, and cytotoxicity on a mammalian cell line .
Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research .
Clofazimine (Standard) is the analytical standard of Clofazimine. This product is intended for research and analytical applications. Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research .
Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research .
Clofazimine (Standard) is the analytical standard of Clofazimine. This product is intended for research and analytical applications. Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research .
4-Allylcatechol (4-Allylpyrocatechol) is a xylan which has oral activity and can be 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 Mycobacterium tuberculosis H37Rv (MIC = 27.6 μg/mL) .
(Rac)-Sativan is an isoflavanoid with a broad spectrum of antimicrobial activity against bacteria and phytopathogenic fungi. (Rac)-Sativan exhibits antituberculosis activity against Mycobacterium tuberculosisH37Rv, with MIC values of 50 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 Mycobacterium tuberculosisH37Rv .
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 Mycobacterium tuberculosisH37Rv (MIC: 32 μg/mL). (24S)-Cycloartane-3β,24,25-triol can be isolated from the flowers of Chrysanthemum morifolium .
