Luliconazole(NND 502) is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.IC50 Value: Target: AntifungalLuliconazole is an antifungal that belongs to the azole class. Although the exact mechanism of action against dermatophytes is unknown, luliconazole appears to inhibit ergosterol synthesis by inhibiting the enzyme lanosterol demethylase. Inhibition of this enzyme’s activity by azoles results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and a corresponding accumulation of lanosterol. In a fertility study in rats, subcutaneous doses of 1, 5 and 25 mg/kg/day luliconazole were administered prior to and during mating and through early pregnancy. Treatment related effects on reproductive function were noted in females (decreased live embryos and decreased corpus luteum) at 5 and 25 mg/kg/day and males (decreased sperm counts) at 25 mg/kg/day. No treatment related effects on fertility or reproductive function were noted at 1 mg/kg/day (0.1X MRHD based on BSA comparisons).
Isobavachromene is an antibacterial agent[1].
Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV with an IC50 of 12 nM.
Lipoxamycin hemisulfate is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM[1][2].
Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM[1][2].
Fexinidazole is a 5-nitroimidazole drug currently in clinical development for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species of the protozoan parasite Trypanosoma brucei. Target: Antiparasiticin vivo: Fexinidazole shows dose-related efficacy in the T. b. rhodesiense (STIB900) acute mouse model at intraperitoneal (i.p.) doses of 20 to 50 mg/kg/day and oral (per os [p.o.]) doses of 25 to 100 mg/kg/day given on four consecutive days, with 100 mg/kg/day p.o. being 100% curative. Fexinidazole is shown to be effective in the GVR35 mouse model, which mimics the advanced and fatal stage of the disease, when parasites have disseminated into the brain. [1]
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabI inhibitor. Meleagrin is a lead c-Met inhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies[1][2][3].
Toltrazuril is an antiprotozoal agent that acts upon Coccidia parasites.Target: AntiparasiticToltrazuril is an antiprotozoal agent that acts upon Coccidia parasites. Toltrazuril induces changes in the fine structure of coccidian development stages that are mainly due to a swelling of the endoplasmatic reticulum and of the Golgi apparatus and to abnormalities in the peri-nuclear space, disturbance in nuclear division. Treated with toltrazuril showed a considerably lower mean opg to that of group C (5.78 opg versus 144.62 opg) (p < 0.05) and a FOCR of 97.7 %. The higher efficacy (99.23 %) was observed at 15 days post treatment; however, the average efficacy of the drug remained extremely high (> 90 %) for all the study.
BMS-986224 is a potent, selective and orally bioavailable APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr1) apelin-13. BMS-986224 has the potential for the research of heart failure[1].
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer[1].
Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis[1][2][3][4][5].
Doxorubicin is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of topoisomerase-II-mediated DNA repair.
Pomotrelvir (PBI-0451) is a selective, orally active SARS-CoV-2 3CL protease inhibitor. Pomotrelvir has antiviral activity and can be used in the research of novel coronavirus (COVID-19)[1].
Horminone is an abietan diterpene quinone that can be isolated from Labiatae family. Horminone increases of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) serum levels in vivo. Horminone inhibits the growth of Trypanosoma cruzi and shows antibacterial activity[1].
G43 is a potent, selective glucosyltransferase inhibitor, with the Kd of 3.7μM and 46.9 nM for GtfB and GtfC, respectively. G43 has antibacterial to S. mutans in vitro and in vivo, and can be used for dental caries study[1][2].
Ridinilazole is a novel antibacterial with MICs range of 0.06-0.25 µg/mL (MIC90=8 µg/mL) against C. difficile.
Corydalmine hydrochloride inhibits spore germination of some plant pathogenic as well as saprophytic fungi[1]. Corydalmine hydrochloride acts as an oral analgesic agent, exhibiting potent analgesic activity[2]. Corydalmine hydrochloride alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway[3].
Cilgavimab (AZD-1061; COV2-2130) is a humanized SARS-CoV-2-neutralizing monoclonal antibody, can compose monoclonal-antibody combination AZD7442 with Tixagevimab (HY-P99556). Cilgavimab shows protective action on mouse models of SARS-CoV-2 infection[1].
Cyclic HPMPC is a potent antiviral agent. Cyclic HPMPC can increase arterial oxygen saturation levels in lethal vaccinia virus (IHD strain)-infected mice. Cyclic HPMPC improves the outcome of congenital guinea pig cytomegalovirus (GPCMV) infection and decreases viral replication in guinea pig model[1][2].
BRITE-338733 is a RecA ATPase inhibitor, with an IC50 of 4.7 µM[1].
A potent and selective HDAC3 inhibitor with IC50 of 0.26 uM, with no activity against HDAC1/4/6/8; induces dose-dependent selective increase of NF-κB acetylation in human colon cancer HCT116 cells, induces growth inhibition of cancer cells, and activates HIV gene expression in latent HIV-infected cells; shows promising activity for anticancer and antiviral benefits.
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[1].
Dimetridazole is a nitroimidazole class drug that combats protozoan infections.Target: AntiparasiticDimetridazole (DMZ) is a 5-nitroimidazole drug traditionally used for the prevention and treatment of histomoniasis in turkeys, trichomoniasis in pigeons, genital trichomoniasis in cattle and the prevention and treatment of haemorrhagic enteritis in pigs.
LolCDE-IN-1 is an inhibitor of the Lol proteins (LolCDE) complex, with antibacterial activity[1].
Malachite Green Carbinol base (MGOH, MGCB) is a derivative of Malachite green (MG) with not fluorescence. Malachite green carbinol base (MGOH, MGCB), as a pH regulation reagent，MGCB molecule could release OH- under UV light irradiation and generate a progressive shift in pH values. MGCB solution turns from colorless to deep green rapidly when exposed to a high-pressure UV lamp (500 W, 50 W/cm)[1][2].
Garvicin KS, GakC is a peptide at sizes of 32 amino acids to form bacteriocin garvicin KS (GarKS), with other 2 peptides, GakA, and GakB. Garvicin KS, GakC inhibits fibroblast viability and proliferation. Garvicin KS peptides inhibit MSSA with MIC values in the order GakB >GakC >GakA[1].
Isoeugenol is an essential oil constituent of nutmeg, clove, and cinnamon. Isoeugenol inhibits growth of Escherichia coli and Listeria innocua with MICs of 0.6 mg/mL and 1 mg/mL, respectively[1].
Ganciclovir (BW 759) sodium, a nucleoside analogue and an orally active antiviral agent, shows activity against CMV. Ganciclovir sodium also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir sodium inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir sodium has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1)[1][2][3].
Kadsulignan N, a natural product has anti-HIV activity (EC50: 43.56 μM). Kadsulignan N is also a COX-2 ligand (Ki: 72.24 nM)[1][2].