mic-2

PF-04753299 is a potent and selective inhibitor of UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC), demonstrating bactericidal effects against gonococcal isolates and exhibiting inhibitory activity against E. coli, P. aeruginosa, and K. pneumoniae, with minimum inhibitory concentration (MIC) 90 values of 2 μg ml, 4 μg ml, and 16 μg ml, respectively. This compound is utilized in researching gram-negative bacterial infections [1].

IMPDH2-IN-2 is a potent inhibitor of inosine 5'-monophosphate dehydrogenase (IMPDH) (Ki,app: 14 μM) and a potential anti-tuberculosis agent, exhibiting moderate antibacterial effects with MIC values of 6.3 and 11 μM in minimal GAST Fe and rich 7H9 ADC Tween media, respectively.

4-Chlorosalicylic acid (4-Chloro-2-hydroxybenzoic acid, 4-chloro salicylic acid) is antimicrobial compositions comprising a metal salt and a benzoic acid analog.

2,6-Dichlorodiphenylamine, an analogue of Diclofenac Sodium, exhibits anti-Candida albicans activity. Diclofenac Sodium, a potent and nonselective COX inhibitor, has IC50 values of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells. [1]. Makoto Urai, et al. Potent Drugs That Attenuate anti-Candida albicans Activity of Fluconazole and Their Possible Mechanisms of Action. J Infect Chemother. 2014 Oct;20(10):612-5.

Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic derived from tetracycline that binds to the 30S ribosomal subunit, disrupting the binding of aminoacyl-tRNA to the mRNA-ribosome complex.

1. Octyl Gallate is an antioxidant approved by the US Food and Drug Administration (FDA) as a food additive. 2. Octyl Gallate has antimetastatic activity. 3. Octyl Gallate shows antimicrobial activity against H. pylori, with a minimum inhibitory concentration (MIC) value of 125 ug mL. 4. Combination therapy with octyl gallate and ferulic acid improves cognition and neurodegeneration in a transgenic mouse model of Alzheimer's disease.5. Octyl Gallate is a potential anticancer agent, it exhibited decreased MCF-7 & MDA-MB-231 survival and induced apoptosis, with IC50 value of 40 uM. 6. Octyl gallate (Octyl 3,4,5-trihydroxybenzoate) has antiviral activity, it shows an inhibitory effect on the growth of herpes simplex virus type 1 (HSV-1) in HEp-2 or Vero cells. 7. Octyl gallate shows antifungal activity against Saccharomyces cerevisiae ATCC7754 and Zygosaccharomyces bailii ATCC 60483.

2,4′-Dichloroacetanilide (2-chloro-N-(4-chlorophenyl)acetamide) has antifungal activity and inhibits T. asteroides with a minimum inhibitory concentration (MIC) of 6.25 μg mL.

DL-Menthol ((±)-Menthol) is a racemic mixture of the monoterpene alcohols (–)-menthol and (+)-menthod, which have been found in Cannabis. (–)-Menthol is more common than (+)-menthol in nature and exhibits analgesic, antibacterial, and anticancer properties, as well as inhibits cholinesterase.2 (+)-Menthol inhibits the growth of F. verticillioides (MIC: 1.5 mM) but, unlike (–)-menthol, does not exhibit analgesic, antibacterial, anticancer, or cholinesterase inhibitory activities.

BPH-1358 (NSC-50460) (NSC-50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor. With IC50s of 1.8 μM and 110 nM, respectively. And it is active against S. aureus in vitro (MIC ~250 ng mL)[1][2].

ALPHA-PINENE ((-)-Alpha-Pinene) is a bicyclic monoterpene found in pine trees and other plants, including Cannabis with diverse biological activities [1]. It reduces the growth of a panel of seven Gram-positive bacteria, seven Gram-negative bacteria, and eight yeast strains with MIC values of 0.75-1.29, 1.05-1.59, and 0.7-1.17%, respectively [2]. It has insecticidal activity against C. molestus larvae with LC50 values ranging from 47 to 49 mg L.3 ALPHA-PINENE (100 μg ml) induces apoptosis, increases anion superoxide production and DNA fragmentation, and activates caspase-3 in B16 F10 melanoma cells [4]. In a B16 F10 mouse xenograft model, ALPHA-PINENE(100 ml of a 10 mg ml solution) reduces the number of metastatic lung nodules by approximately 7-fold. ALPHA-PINENE(8.6 mg L, aerosol) also increases the time spent in the open arms of the elevated plus maze by approximately 2-fold in mice, indicating anxiolytic-like activity [5].

7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) exhibits anti-inflammatory, antibacterial, and antifungal activities, along with moderate antitrypanosomal activity, having an MIC value of 19.0 µg mL.

Bellidifolin (Bellidifoline) has anti-oxidation, hepatoprotective, anti-inflammatory and antitumor actions, it may contribute to the protective effects associated with nerve injury initiated by hypoxia by mechanisms related to inhibition of cell apoptosis independent of the ERK pathway. Bellidifolin shows interesting inhibitory activity of monoamine oxidases (MAO) A, it could be useful for treating type-2 diabetes, likely via the improvement of insulin resistance (IR). Bellidifolin also shows an antifungal effect (MIC values of 50 microg mL).

Chlorhexidine-d8 is intended for use as an internal standard for the quantification of chlorhexidine by GC- or LC-MS. Chlorhexidine is a bis(biguanide) antimicrobial disinfectant and antiseptic agent. It inhibits growth of clinical methicillin-resistant S. aureus (MRSA) isolates (MIC90 = 4 μg/ml). It is also active against canine isolates of MRSA, methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. pseudintermedius (MRSP), and methicillin-susceptible S. pseudintermedius (MSSP; MIC90s = 4, 2, 2, and 1 mg/L, respectively). Chlorhexidine inhibits growth of E. faecium strains (MICs = 1.2-19.6 μg/ml) and C. albicans (MIC = 5.15 μg/ml). It generates cations that bind to and destabilize the bacterial cell wall to induce death.6 Chlorhexidine also completely inhibits matrix metalloproteinase-2 (MMP-2) and MMP-9 when used at concentrations of 0.0001 and 0.002%, respectively, in a gelatin degradation assay. Formulations containing chlorhexidine have been used in antisept......

1-Heptadecanoyl-rac-glycerol is a monoacylglycerol that contains heptadecanoic acid at the sn-1 position. It is active against the bacteria E. aerogens, E. cloacae, P. mirabilis, and S. faecalis (MIC = 78 μg/ml for all).1 1-Heptadecanoyl-rac-glycerol has been found in T. africana, I. sonorae, and wheat bran.1,2,3 |1. Kuete, V., Metuno, R., Ngameni, B., et al. Antimicrobial activity of the methanolic extracts and compounds from Treculia africana and Treculia acuminata (Moraceae). S. Afr. J. Bot. 74(1), 111-115 (2008).|2. Fernández-Galicia, E., Calada, F., Roman-Romos, R., et al. Monoglycerides and fatty acids from Ibervillea sonorae root: Isolation and hypoglycemic activity. Planta Med. 73(3), 236-240 (2007).|3. Prinsen, P., Gutiérrez, A., Faulds, C.B., et al. Comprehensive study of valuable lipophilic phytochemicals in wheat bran. J. Agric. Food Chem. 62(7), 1664-1673 (2014).

Tigecycline tetramesylate (GAR-936 tetramesylate), a broad-spectrum glycylcycline antibiotic, exhibits a mean inhibitory concentration (MIC) for E. coli (MG1655 strain) of approximately 125 ng/mL [1]. For Acinetobacter baumannii (A. baumannii), the MIC 50 and MIC 90 values stand at 1 and 2 mg/L, respectively [2].

Antibacterial agent 32 exhibits potent antimicrobial activity against E. coli strains NCTC 13351, M 50, and 7 MP, with minimum inhibitory concentration (MIC) values of 1 mcg/mL, 2 mcg/mL, and 8 mcg/mL, respectively (WO2013030733A1, example 43).

Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg ml, respectively.References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984). Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg ml, respectively. References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984).

3-O-(E)-p-coumaroyl tormentic acid may be promising lead compound for developing an effective drug for treatment of leukemia, it induces apoptotic cell death in human leukemia (HL60) via mainly mitochondrial pathway by, at least in part, Topo I inhibition. 3-O-trans-p-coumaroyltormentic acid shows cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro, the IC50 values of 13.72, 14.29,14.61, 14.04 uM, respectively. 3beta-O-cis-p-Coumaroyltormentic acid, and 3beta-O-trans-p-coumaroyltormentic acid are weakly selective for vancomycin-resistant Enterococcus (VRE) compared with eukaryotic cells, with an MIC of 59.4microg/mL and a 50% inhibitory concentration (IC50) of 72.0microg/mL for monkey kidney epithelial (MA104) cells. A mixture of 3-O-cis-p-coumaroyltormentic acid and 3-O-trans-p-coumaroyltormentic acid shows an inhibitory effect comparable to (-)-epigallocatechin gallate (EGCG) of green tea on the activation of Epstein-Barr virus early antigen (EBV-EA) induced by 12-O-tetradeca--noylphorbol-13-acetate (TPA).

Anti-MRSA agent 2 (compound 14) is a potent inhibitor of methicillin-resistant Staphylococcus aureus (MRSA) (MIC: 0.098 μg ml), exhibiting relatively low toxicity to normal cells. It strongly disrupts bacterial membranes and effectively binds to bacterial genomic DNA.

VEGFR-2 DHFR-IN-1 (compound 8b) is a chemical inhibitor of VEGFR-2 and DHFR, with IC50 values of 0.384 μM and 7.881 μM, respectively. It possesses effective antibacterial activity against pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg mL. Additionally, it exhibits potent cytotoxicity against cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, making it a valuable tool for cancer research [1].

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg/ml) and Kurono (MIC: 0.0005 μg/ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg/ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg/ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg/ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg/kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1/2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg/kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg/kg to 2.5 mg/kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg/kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.

Tuberculosis inhibitor 8 (compound 3b), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against both Mycobacterium tuberculosis and Mycobacterium marinum with an MIC 90 of 0.69 μM [1].

ABT-719 is a 2-pyridinone antimicrobial agent that is more effective against Enterococcus faecalis strains than ciprofloxacin and vancomycin, which showed resistance to ciprofloxacin and vancomycin covering a range of MIC.

Benastatin B is a polyketide synthase-derived benastatin that has been found in Streptomyces and has diverse biological activities. It inhibits glutathione S-transferase (GST; Ki = 3.7 µM for the rat liver enzyme).2 Benastatin B also inhibits the transglycosylase activity of A. baumannii, C. difficile, E. coli, and S. aureus recombinant penicillin-binding proteins (PBPs; IC50s = 16, 53.3, 30.7, and 31.6 µM, respectively).3 It is active against several bacteria, including methicillin-resistant S. aureus (MRSA; MIC = 3.12 µg/ml).

Ranitidine bismuth citrate, an orally administered Histamine H2-receptor antagonist, demonstrates a potent inhibitory concentration (IC 50) of 3.3 μM and exhibits high selectivity towards SARS-CoV-2-infected cells. It is widely utilized as an anti-Helicobacter pylori agent, exhibiting a minimum inhibitory concentration (MIC 90) value of 16 ng/L.

LolCDE-IN-2 is a potent inhibitor of the Lol protein (LolCDE) and demonstrates antibacterial activity against E. coli MG1655, with a minimum inhibitory concentration (MIC) of 2 μg ml [1].

LpxA-IN-1, a novel UDP-N-acetylglucosamine acyltransferase (LpxA) inhibitor exhibiting potent activity (IC 50 2 nM), effectively targets Pseudomonas aeruginosa with a minimum inhibitory concentration (MIC) of 8 μg/mL.

1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, a diacylglycerol acyltransferase inhibitor and angiotensin II receptor blocker, exhibits IC50 values of 20.1 μM and 34.1 μM, respectively, and demonstrates significant anti-Helicobacter pylori activity with a minimum inhibitory concentration (MIC) of 10 μg mL [1] [2] [3].

Murepavadin (POL7080) (TFA), a 14-amino-acid cyclic peptide, serves as a highly potent, specific antibiotic with remarkable antimicrobial activity against P. aeruginosa, demonstrated by MIC 50 and MIC 90 values of 0.12 mg/L. It uniquely targets the lipopolysaccharide transport protein D, showing potential for research on bacterial resistance [1] [2].

UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) with efficacy against HER2+ breast cancer xenografts, including cell lines resistant to anti-HER2 drugs [1]. Additionally, it functions as an inhibitor of the Filamentous temperature-sensitive protein Z (FtsZ), selectively inhibiting the growth of the Gram-positive bacterium B. subtilis with minimum inhibitory concentration (MIC) values of 100 μM, while showing no activity against the Gram-negative bacterium E. coli [2].

Nocardamine is a ferrioxamine siderophore that has been found inStreptomycesand has diverse biological activities.1,2,3,4It chelates iron in a chrome azurol S assay (IC50= 9.9 μM).1Nocardamine inhibitsM. smegmatisandM. bovisbiofilm formation (MIC = 10 μM for both), an effect that can be reversed by iron.2It is cytotoxic to T47D, SK-MEL-5, SK-MEL-28, and RPMI-7951 cancer cells (IC50s = 6, 18, 12, and 14 μM, respectively).3Nocardamine also induces morphological changes in BM-N4 insect cells.4 1.Lopez, J.A.V., Nogawa, T., Futamura, Y., et al.Nocardamin glucuronide, a new member of the ferrioxamine siderophores isolated from the ascamycin-producing strain Streptomyces sp. 80H647J. Antibiot. (Tokyo)72(12)991-995(2019) 2.Ishida, S., Arai, M., Niikawa, H., et al.Inhibitory effect of cyclic trihydroxamate siderophore, desferrioxamine E, on the biofilm formation of Mycobacterium speciesBiol. Pharm. Bull.34(6)917-920(2011) 3.Kalinovskaya, N.I., Romaneko, L.A., Irisawa, T., et al.Marine isolate Citricoccus sp. KMM 3890 as a source of a cyclic siderophore nocardamine with antitumor activityMicrobiol. Res.166(8)654-661(2011) 4.Matsubara, K., Sakuda, S., Tanaka, M., et al.Morphological changes in insect BM-N4 cells induced by nocardamineBiosci. Biotechnol. Biochem.62(10)2049-2051(1998)

Carbazomycin A is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities.1,2It is active againstS. aureus,T. asteroides, andT. mentagrophytes(MIC = 12.5 μg/ml for all), as well as the plant pathogenic fungusP. oryzae(MIC = 25 μg/ml). Carbazomycin A is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 26.2, 30.1, 18.4, and 32.6 μg/ml, respectively).2 1.Sakano, K.-I., Ishimaru, K., and Nakamura, S.New antibiotics, carbazomycins A and B. I. Fermentation, extraction, purification and physico-chemical and biological propertiesJ Antibiot. (Tokyo)33(7)683-689(1980) 2.Intaraudom, C., Rachtawee, P., Suvannakad, R., et al.Antimalarial and antituberculosis substances from Streptomyces sp. BCC26924Tetrahedron67(39)7593-7597(2011)

3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003). 3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4 References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003).

3-O-Methylellagic acid, a natural product isolated from Myrciaria cauliflora, exhibits anti-inflammatory and antibacterial activities. This compound not only inhibits glucose transport but also demonstrates a minimum inhibitory concentration (MIC) of 32 μg/mL against Staphylococcus aureus ATCC 25923 [1] [2] [3].

Sordarin is an inhibitor of fungal protein synthesis originally isolated from S. araneosa.[1] It binds to elongation factor 2 (EF-2) in the presence of ribosomes and inhibits the uncoupled GTPase activity of equimolar mixtures of EF-2 and ribosomes from C. albicans (IC50 = 0.1 μM). Sordarin inhibits protein synthesis in cell-free lysates of C. albicans, C. glabrata, and C. neoformans (IC50s = 0.01, 0.2, and 0.06 μg/ml, respectively) but not in rabbit reticulocytes (IC50 = >100 μg/ml).[1] [2] It inhibits the growth of C. albicans (MIC = 8 μg/ml) but not C. glabrata or C. neoformans (MICs = >125 μg/ml).

Piliformic acid is a fungal metabolite found in [N. pseudotrichia] with diverse biological activities. It is cytotoxic to BC-1 human breast cancer cells (IC50 = 5 μg ml) and active against [L. braziliensis] amastigotes (IC50 = 78.5 μM). It also shows activity against the plant pathogenic fungi [C. gloeosporioides] (MIC = 292 μM).

Globosuxanthone A, a dihydroxanthenone with anticancer activity, exhibits significant antifungal activity against Fusarium graminearum, Fusarium solani, and Botrytis cinerea, with MIC values of 4, 8, and 16 μg mL, respectively [1] [2].

Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg/ml) and induces efflux of potassium ions from B. subtilis without affecting Na+/K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg/ml. It inhibits the growth of B. halodurans (MIC = 10 ng/ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromycin (3.4 nM) reverses bleomycin-induced cell cycle arrest at the G2 phase in Jurkat cells. It inhibits replication of the HIV-1 strains LAV-1 and RF and the HIV-2 strain LAV-2 in MT-4 cells (IC50s = 0.008, 0.11, and 0.007 μM, respectively). It also inhibits replication of a clinical isolate of HIV-1, strain KK-1, in MT-4 cells and peripheral blood mononuclear cells (PBMCs; IC50s = 0.14 and <0.1 μM, respectively).

Emeguisin A is a depsidone fungal metabolite originally isolated fromE. unguis.1It is active against the bacteriaS. aureusand methicillin-resistantS. aureus(MRSA; MIC = 0.5 μg/ml for both), the fungusC. neoformans(MIC = 0.5 μg/ml), and the protozoanP. falciparum(IC50= 2.2 μM).2 1.Kawahara, N., Nozawa, K., Nakajima, S., et al.Isolation and structures of novel fungal depsidones, emeguisins A, B, and C, from Emericella unguisJ. Chem. Soc., Perkin Trans. 12611-2614(1988) 2.Klaiklay, S., Rukachaisirikul, V., Aungphao, W., et al.Depsidone and phthalide derivatives from the soil-derived fungus Aspergillus unguis PSU-RSPG199Tetrahedron Lett.57(39)4348-4351(2016)

Tigecycline mesylate is a first-in-class, broad-spectrum antibiotic. It also has activity against antibiotic-resistant organisms.

Antitubercular agent-22 (Compound 2) is an effective antimicrobial agent against Candida albicans MTCC 3017 (MIC: 2.34 μg ml) and M. tuberculosis (H37Rv) (MIC: 2 μg ml).

Sporogen-AO 1 is a fungal metabolite originally isolated fromA. oryzaethat has diverse biological activities.1,2,3,4,5It inhibits HIV-1 Tat transactivation in a cell-based assay with an IC50value of 15.8 μM.4Sporogen-AO 1 is cytotoxic to HeLa, KB, and NCI H187 cancer cells (IC50s = 8.3, 9, and 5.1 μM, respectively).2,5It is active againstC. albicans(MIC = 4 mM).3 1.Tanaka, S., Wada, K., Marumo, S., et al.Structure of sporogen-ao 1, a sporogenic substance of Aspergillus oryzaeTetrahedron Lett.25(51)5907-5910(1984) 2.Motohashi, K., Hashimoto, J., Inaba, S., et al.New sesquiterpenes, JBIR-27 and -28, isolated from a tunicate-derived fungus, Penicillium sp. SS080624SCf1J. Antibiot. (Tokyo)62(5)247-250(2009) 3.Yurchenko, A., Smetanina, O.F., Kalinovsky, A., et al.Biologically active metabolites of the facultative marine fungus Penicillium citrinumChem. Nat. Compd.48(6)996-998(2013) 4.Jayasuriya, H., Zink, D.L., Polishook, J.D., et al.Identification of diverse microbial metabolites as potent inhibitors of HIV-1 Tat transactivationChem. Biodivers.2(1)112-122(2005) 5.Tansakul, C., Rukachaisirikul, V., Chalothorn, T., et al.Synthesis and cytotoxicity against KB and NCI-H187 cell lines of sporogen AO-1 analoguesPhytochem. Lett.22128-132(2017)

Lytixar is a Synthetic Antimicrobial Peptide, it shows activity against Daptomycin-Nonsusceptible, Methicillin-Resistant, Vancomycin-Intermediate, Vancomycin-Resistant, and Linezolid-Nonsusceptible Staphylococcus aureus. LTX-109 demonstrated a MIC range o

Lynronne-2, an antimicrobial peptide, exhibits activity against Gram-positive bacteria, including methicillin-resistant MRSA strains (MIC: 32-256 μg/mL), and demonstrates effectiveness in combating P. aeruginosa infections [1].

FtsZ-IN-2 is an inhibitor of the bacterial cytokinin FtsZ and has an inhibitory effect on GTPase activity. ftsZ-IN-2 exhibited anti-staphylococcal effects with MIC values of 2 μg/ml for both MSSA and MRSA.

Antitubercular agent-28 (compound 2) exhibits antimycobacterial activity against resistant isolates of Mycobacterium tuberculosis H37Rv with an MIC of 4.5 μM, an IC50 of 1.5 μM, and an IC90 of 2.5 μM. It demonstrates effective intracellular antimycobacterial activity with low cytotoxicity [1].

Methylchloroisothiazolinone/methylisothiazolinone mixture (MCIT/MIT) is a mixture of isothiazolinone-derived biocides.1,2It is effective against Gram-positive and Gram-negative bacteria with MIC values of 0.0002, 0.0002, 0.00005, and 0.00005% (w/w) forS. aureus,P. aeruginosa,A. niger, andC. albicans, respectively.2MCIT/MIT can elicit contact sensitization.3Formulations containing MCIT/MIT have been used for controlling microbial growth in industrial and household products. 1.Frenzel, E., Schmidt, S., Niederweis, M., et al.Importance of porins for biocide efficacy against Mycobacterium smegmatisApplied and Environmental Microbiology77(9)3068-3073(2011) 2.Lundov, M.D., Johansen, J.D., Zachariae, C., et al.Low-level efficacy of cosmetic preservativesInt. J. Cosmet. Sci.33(2)190-196(2011) 3.Scherrer, M.A.R., and Rocha, V.B.Increasing trend of sensitization to methylchloroisothiazolinone/methylisothiazolinone (MCI/MI)An. Bras. Dermatol.89(3)527-528(2014)

MsbA-IN-5 (compound 40) is a potent and highly selective MsbA inhibitor with an IC50 of 2 nM, suitable for use in Gram-negative studies.