Anticandidal agent-1 (compound c2) is a potent and broad-spectrum anticandidal agent. Anticandidal agent-1 shows anticandidal activity against C. albicans and C. glabrata, with MIC50 values of 8.65 and 13.51 μg/mL, respectively. Anticandidal agent-1 inhibits biofilm by blocking hyphal elongation and filamentation[1].
Xenopsin precursor fragment is an antimicrobial peptide, and has antibacterial/antifungal (10-500 μg/mL) and anti-protozoal (MIC: 2-20 μg/mL) activity[1].
Tiprelestat is a potent human neutrophil elastase inhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease[1].
MA220607 is an antibacterial agent with low hemolytic toxicity and a dual-target mechanism of action (MOA). MA220607 promotes FtsZ protein polymerization, also increases the permeability of bacterial membranes and inhibits biofilm formation. The resistance rate of MA220607 is low, and the MICs against Gram-positive bacteria and Gram-negative bacteria are Table 0.062-2 μg/mL and 0.5-4 μg/mL, respectively)[1].
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca2+ influx through voltage-gated Ca2+ channels, leading to the reduction in [Ca2+]i in vascular smooth muscle cells and consequent peripheral vasodilation[1]. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM[2].
Avermectin B1a is an antiparasitic agent that paralyzes nematodes without causing hypercontraction or flaccid paralysis.
Antileishmanial agent-11 (compound 4d) is a potent anti-leishmanial agent. Antileishmanial agent-11 shows antiprotozoal activity against Leishmania brazilensis, Leishmania infantum, and T. cruzi, with IC50 values of 28.3, 24.8 and 13.0 μM, respectively[1].
Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CLpro inhibitor[1][2][3][4].
Hepatitis C Virus S5A/5B is a synthetic peptide substrate. Hepatitis C Virus S5A/5B mimics the NS5A/5B junction of the nonstructural protein (NS), served as the substrate for the study of HCV NS3 protease activity[1].
5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol[1].
Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration[1].
Fumonisin B2, a mycotoxin produced by Fusarium moniliforme in various grains, is a potent inhibitor of sphingosine N-acyltransferase (ceramide synthase) and disrupts de novo sphingolipid biosynthesis[1][2].
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research[1][2][3][4].
Anti-MRSA agent 2 (compound 14) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and relatively low cytotoxicity in normal cells. Anti-MRSA agent 2 has strong ability to destroy bacterial membrane and bind to genomic DNA[1].
Walrycin B is a novel antibacterial compound specifically targeting the essential WalR response regulator.IC50 value: 0.39 ug/ml (MIC for B. subtilis 168); 3.13 ug/ml (MIC for S. aureus N315) [1]Target: bacterial WalR response regulator; AntibacterialWalrycin B is known as an analog of toxoflavin (a phytotoxin from Burkholderia glumae), which has been shown to have a strong MIC for B. subtilis and S. aureus but whose mode of action is not clear. The compound could also interact with WalR to cause bactericidal effects. Walrycins are a new class of potent small molecule compounds that kill bacterial cells by targeting the RR WalR and inhibiting this essential signal transduction pathway. They not only have therapeutic potential but will also prove to be useful reagents for the further study of the WalK/WalR TCS. Walrycin B target WalR andlead to cell death in both B. subtilis and S. aureus.
Combi-1 is an antimicrobial peptide with broad-spectrum activity against different bacteria and yeast cells[1].
Solanesol is an aliphatic terpene alcohol mainly found in Solanaceous plants, with anti-inflammatory, neuroprotective, and antimicrobial activities[1].
Artelinic acid, a derivative of Artemisinin, is an antimalarial drug for the treatment of multidrug resistant strains of Plasmodium falciparum. Artelinic acid can be administered by various routes of administration, including intravenous, intramuscular and oral routes[1][2].
Pleurocidin is an antibacterial peptide derived from skin secretions of Winter Flounder[1].
Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.
Broxaldine is an antiprotozoal drug.
L 696229 is a specific inhibitor ofhuman immunodeficiency virus type 1 (HIV-1)reverse transcriptase (RT) activity that possesses antiviral activity[1].
FtsZ-IN-1 is a potent FtsZ inhibitor with quinolinium ring. FtsZ-IN-1 has stronger antibacterial activity against Gram-positive bacteria with MICs of 0.5-8 μg/mL. FtsZ-IN-1 significantly causes cell elongation of B. subtilis by enhancing FtsZ polymerization. FtsZ-IN-1 exhibits low hemolytic toxicity and low tendency to induce drug resistance. FtsZ-IN-1 has against drug-resistant bacteria activity[1].
Defensin HNP 4 (HNP 4) is a single 11 amino acid long fragment of HNP-41-11. Defensin HNP 4 has inhibitory effect against multidrug-resistant and non-resistant strains[1].
Pentamidine isethionate is an antimicrobial agent for prevention and treatment of Pneumocystis pneumonia (PCP) caused by Pneumocystis jirovecii.
Icariside D2, isolated from Annona glabra fruit, inhibits angiotensin-converting enzyme. Icariside D2 shows significant cytotoxic activity on the HL-60 cell line with the IC50 value of 9.0 ± 1.0 μM. Icariside D2 induces apoptosis [1][2].
Bibrocathol is antiseptic agent plays important role in acute eyelid diseases like blepharitis[1].