2-Hydroxyacetophenone is a principal root volatile of the Carissa edulis[1]. 2-Hydroxyacetophenone shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 1.8 mM[2].
Peptide T (TFA) is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
Rimantadine Hcl (Flumadine) is an anti-influenza virus drug.Target: Influenza VirusRimantadine are oral antiviral drugs useful in the prophylaxis and treatment of influenza A virus infections. rimantadine has prophylactic efficacy comparable to amantadine but lower potential for causing adverse effects [1]. double-blind study of children with influenza-like illness. 37 received rimantadine for five days. Of the total 37 children in the rimantadine group, 27% were found to have resistant isolated compared with 6% in the total group receiving acetaminophen (P < .04). Furthermore, the mean inhibitory concentration of rimantadine increased with time in the rimantadine group (r = .4, P = .002) [2].
Friulimicin A, a lipopeptide antibiotic, like Friulimicin B, is isolated from the actinomycete Actinoplanes friuliensis[1].
RO-9187 is a potent inhibitor of HCV virus replication with an IC50 of 171 nM.
Ascomycin(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. IC50 Value: 0.55 nM [1]Target: in vitro: When we used either CD4+CD8+ thymocytes or peripheral T cells activated by phorbol ester and ionomycin, the cell surface induction of CD5 was also partially blocked by CsA, FK-520 and rapamycin [2]. Ascomycinalso had a 3-fold lower immunosuppressive potency in a popliteal lymph node hyperplasia assay, resulting in an equivalent therapeutic index consistent with a common mechanistic dependence on calcineurin inhibition [3].in vivo: In 14-day studies, nephrotoxicity was not induced by continuous i.p. infusion of ascomycin at 10 mg/kg/day or daily oral administration (up to 50 mg/kg/day) in rats on a normal diet, nor by continuous i.v. infusion (up to 6 mg/kg/day) in rats on a low salt diet to enhance susceptibility [3].
Bromodiphenhydramine hydrochloride is a potent antihistamine with antimicrobial property. Bromodiphenhydramine hydrochloride inhibits a large number of Gram negative and Gram positive bacteria. Bromodiphenhydramine hydrochloride can be used for cutaneous allergies research[1][2][3].
Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Retusin (Quercetin-3,3',4',7-tetramethylether), a natural compound isolated from the leaves of Talinum triangulare, possesses antiviral and anti-inflammatory activities[1].
Patentiflorin A is a potent, broadspectrum HIV-1 inhibitor. Patentiflorin A also inhibits HIV drug-resistant strains[1].
PCL 016 is a topical antiviral agent, which inhibits adenovirus replication in rabbit.
Antibacterial agent 115 (Compound 10) is an orally active antibacterial and anti-inflammatory agent[1].
Demethoxypiplartine is an amide alkaloids which can be isolated from Piper flaviflorum and Piper sarmentosum. Demethoxypiplartine has antifungal activity against Cryptococcus neoformans with the IC50 of 18.1 μg/mL[1].
Stavudine sodium is a nucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.Target: HIV RT; NRTIsStavudine sodium is a dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV. Stavudine sodium is an analog of thymidine. It is phosphorylated by cellular kinases into active triphosphate. Stavudine sodium triphosphate inhibits the HIV reverse transcriptase by competing with natural substrate, thymidine triphosphate. It also causes termination of DNA synthesis by incorporating into it [1]. Mice were treated for 2 weeks with stavudine d4T (500 mg/kg/day), L-carnitine (200 mg/kg/day) or both drugs concomitantly. Body fatness was assessed by dual energy X-ray absorptiometry, and investigations were performed in plasma, liver, muscle and WAT. D4T reduced the gain of body adiposity, WAT leptin, whole body FAO and plasma ketone bodies, and increased liver triglycerides and plasma aminotransferases with mild ultrastructural abnormalities in hepatocytes [2].Clinical indications: HIV-1 infection FDA Approved Date: June 24, 1994 Toxicity: peripheral neuropathy; lipodystrophy
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[1].
Antileishmanial agent-8 (compound 18) has potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 5.64 μM. Antileishmanial agent-8 has relatively low cytotoxicity in L-6 cells (IC50=73.9 μM)[1].
PA3552-IN-1 (compound 15) is an antibiotic adjuvant that restores sensitivity of MDR P. aeruginosa DK2 strain to Polymyxin B. PA3552-IN-1 can reduce PA3552 expression[1].
β-Lactamase is the enzyme produced by bacteria. β-Lactamase mediates β-lactam resistance[1].
Ilimaquinone, a marine sponge metabolite, displays anticancer activity via GADD153-mediated pathway. Ilimaquinone can induce vesiculation of the Golgi apparatus[1]. Ilimaquinone exerts anti-HIV, anti-microbial, anti-inflammatory, and effects[2].
Calphostin C is a potent and specific inhibitor of protein kinase C. Calphostin C is an antitumor antibiotic. Calphostin C has 1000 times more inhibitory to protein kinase C with an IC50 of 0.05 μM than other protein kinases. Calphostin C induces apoptosis in some tumor cell lines. Calphostin C has potent cytotoxic activity and antitumor activity[1].
GRP-60367 is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains[1].
GNF-6702 (GNF6702) is a selective, non-competitive inhibitor of the kinetoplastid proteasome, inhibits the chymotrypsin-like activity of the T. cruzi proteasome with IC50 of 35 nM; displays no inhibitory effect on caspase-like and the trypsin-like activities (>10 uM); does not inhibit the mammalian proteasome or growth of mammalian cells, and is well-tolerated in mice; clears parasites in mouse models of kinetoplastid infections.
OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 potently inhibits the expression of HSV IEgenes[1].
LB80317 is an active metabolite of LB80380 and suppresses the DNA synthesis of HBV with an EC50 of 0.5 μM. LB80317 has antiviral effect and has the potential for chronic hepatitis B treatment[1][2].
Corydalmine (L-Corydalmine), an alkaloid isolated from roots of Corydalis Chaerophylla, inhibits spore germination of some plant pathogenic as well as saprophytic fungi[1]. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity[2]. Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway[3].
Limonene is a monoterpene in citrus peel oil. A popular disinfectant and food preservative. Antimicrobial activities[1]. Anti-proliferative activities[2]. Antioxidant and anti-inflammatory effect[3].
β-Lactamase-IN-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor. β-Lactamase-IN-8 can be used for researching antibacteria[1].
MMT5-14 is a remdesivir analogue with a higher antiviral activity in four variants of SARS-CoV-2 than Remdesivir (HY-104077). MMT5-14 inhibits SARS-CoV-2, α, β, γ and δ variants with EC50s of 0.4, 2.5, 15.9, 1.7 and 5.6 μM, respectively. MMT5-14 can be used for the research of COVID-19[1].
Foscarnet sodium (Trisodium phosphonoformate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet sodium is an antiherpesvirus agent used in cytomegalovirus retinitis[1][2][3].
Oxyphenbutazone is a phenylbutazone derivative, with anti-inflammatory effect. Oxyphenbutazone is a non-selective COX inhibitor. Oxyphenbutazone selectively kills non-replicating Mycobaterium tuberculosis[1][2].