Antibacterial agent 45, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Loganetin is a non-toxic natural product that may be applied in the antibacterial drug development for treating multidrug-resistant Gram negative infections.
Cefazedone (Refosporen) is a first-generation cephalosporin with activity against Gram-positive and Gram-negative bacteria, and it is effective in the treatment of infections caused by sensitive bacteria. Cefazedone is a time-dependent antibiotic, the time of concentration exceeds the minimum inhibitory concentration (MIC) is the key pharmacokinetic-pharmacodynamic (PK-PD) variable associated with the killing of pathogens[1].
PXYC1 is a ribosomal protein S1 (RpsA) antagonist with Kds of 0.81 and 0.31 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb)[1].
Ampicillin trihydrate (D-(-)-α-Aminobenzylpenicillin trihydrate) is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.
SSAA09E3 is a SARS-CoV entry inhibitor that inhibits SARS/HIV pseudotyped virus entry with an EC50 of 9.7 μM in 293T cells and inhibits SARS-CoV infection of Vero cells with an EC50 of 0.15 μM[1][2].
Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 mg/mL.
Trovafloxacin-d4 mesylate is the deuterium labeled Trovafloxacin mesylate. Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1[1][2][3].
Influenza A virus-IN-7 (compound 16r) is a potent and orally active influenza A virus inhibitor with an IC50 of 3.43 µM and CC50 of >100 µM. Influenza A virus-IN-7 shows anti-IAV activity with low cytotoxicity. Influenza A virus-IN-7 inhibits the transcription and replication of viral RNA[1].
Inz-5 is a fungal-selective mitochondrial cytochrome bc1 inhibitor. Inz-5 impairs fungal virulence and prevents the evolution of drug resistance[1].
Butylparaben sodium strongly influences the later stages of the spermatogenesis in the testis through the deterioration of hormonal control and/or RNA and protein synthesis[1].
Rhamnolipid RL2, is a rhamnolipid, shows antifungal activity[1][2].
JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a Ki of 0.33 nM for HIV-1 protease. JE-2147 has effective activities against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro[1][2].
HCV-IN-39 (Compound 18a) is a potent hepatitis C virus (HCV) nucleoside inhibitor with EC50 values of 0.644, 0.952 and 0.154 μM against GT1a, GT1b and GT1b CES1 replicons[1].
GSK3036656 (GSK070) is a potent, selective and orally active inhibitor of M. tuberculosis leucyl-tRNA synthetase, with an IC50 of 0.20 μM. GSK3036656 can be used for the research of tuberculosis[1].
Tuberculosis inhibitor 7 (compound 2d) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacterium tuberculosis (MIC90 of 0.63 μM) and Mycobacterium marinum (MIC90 of 0.63 μM)[1].
Kievitone, an isoflavanone, could be isolated from hypocotyls of Phaseolus vulgaris L. infected with Rhizoctonia solani Kühn. Kievitone has antifungal activity and antitumor activity[1][2].
Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs)[1][2].
Morin 3-O-β-D-glucopyranoside is a natural flavonoid with antifungal, anticancer and antioxidant activities. Morin 3-O-β-D-glucopyranoside inhibits reverse transcriptase, protein-tyrosine kinase and xanthine oxidase, and also shows anti-HIV, antiarteriosclerotic, and superoxide scavenging activities[1].
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines[1].
Arg-Trp is a dipeptide composed of arginine and tryptophan, and analogues of Arg-Trp-octyl ester show antibacterial activity[1].
LL-37 GKE is an active domain of LL-37. LL-37 GKE has antibacterial activity and has potential applications in antibiotics[1][2].
Antistaphylococcal agent 3 is an antistaphylococcal therapeutic agent.
TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8[1].
Salazopyridazine is an antibacterial agent. Salazopyridazine shows activities against ulcerative colitis. Salazopyridazine can be used for the research of rheumatic diseases[1][2].
Didanosine(Videx) is a reverse transcriptase inhibitor with an IC50 of 0.49 μM.Target: NRTIs; HIVDidanosine is a dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Didanosine demonstrated linear pharmacokinetic behavior over the dose ranges of 0.4 to 16.5 mg/kg intravenously and 0.8 to 10.2 mg/kg orally. Bioavailability of didanosine when administered as a solution with an antacid was approximately 43% for doses from 0.8 to 10.2 mg/kg in patients with AIDS and advanced AIDS-related complex. Bioavailability of didanosine from the citrate-phosphate-buffered solution, the formulation currently used in phase II and expanded access studies, was comparable to the formulation used in the phase I trials [1]. ddI might be responsible for fulminant hepatitis in all three AIDS patients. This toxic effect may be added to the list of potential adverse events occurring during ddI therapy [2].
Tafenoquine Succinate (WR 238605 Succinate) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent[1].
Antibacterial agent 47, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Mycobactin-IN-2 (compound 49) is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-2 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway[1].
Libivirumab (17.1.41) is a humanized anti-HBV monoclonal antibody. Libivirumab shows neutralization activity with IC50s of 35, 130 ng/mL for HBsAg, HBeAg, respectively[1].