Penicillin G benzathine (Benzathine benzylpenicillin) is an antibiotic against many bacterial infections[1].
C-215 is a novel inhibitor of mycobacterial membrane protein large 3 (MmpL3) with MIC90 of 16 uM against M. tuberculosis.
Cartap hydrochloride, an organonitrogen insecticide, can cause a marked irreversible Ca2+-dependent contracture in both isolated mouse and rabbit phrenic nerve-diaphragms. Cartap hydrochloride significantly increases the level of endogenous reactive oxygen species (ROS) in C2C12 cells[1].
Mpro/PLpro-IN-1 (Compound 29) is a potent inhibitor of Mpro/PLpro. Mpro/PLpro-IN-1 is a dual acting SARS-CoV-2 proteases inhibitor featuring micromolar inhibitory potency versus Mpro (IC50 = 1.72 μM) and submicromolar potency versus PLpro (IC50 = 0.67 μM)[1].
MDL 101146 is an orally active neutrophil elastase inhibitor. MDL 101146 inhibits neutrophil elastase for human with a Ki value of 25 nM. MDL 101146 can be used for the research of arthritis[1][2].
Antibacterial agent 123 (compound 111) is a potent membrane-disrupting agent to combat antibiotic-resistant Gram-positive bacteria[1].
CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy[1].
Isobellidifolin, a xanthone, is a free radical scavenger and antioxidant compound. Isobellidifolin has potent antifungal effect[1].
Pentamidine(MP-601205) is an antimicrobial agent.Target: AntiparasiticPentamidine has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin [1]. Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4-2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs [2].
Biapenem is a parenteral carbapenem antibacterial agent with a broad spectrum.Target: AntibacterialBiapenem is a carbapenem antibiotic of in vitro antibacterial activity encompassing many Gramnegative and Gram-positive aerobic and anaerobic bacteria, including species producing β-lactamases. Biapenem is more stable than imipenem, mero-penem and panipenem to hydrolysis by human renal dihydropeptidase-I (DHP-I), and therefore does not require the coadministration of a DHP-I inhibitor. In randomised, nonblind or double-blind clinical trials, biapenem showed good clinical and bacteriological efficacy (similar to that of imipenem/ cilastatin) in the treatment of adult patients with intra-abdominal infections, lower respiratory infections or complicated urinary tract infections.
2,3-Butanediol-d8 is the deuterium labeled 2,3-Butanediol[1]. 2,3-Butanediol is a butanediol derived from the bioconversion of natural resources[2].
4',7-Dimethoxyisoflavone is isolated from the leaves of Albizzia lebbeck, which shows antifungal activity.
Pritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate hydrate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2[1].
Valacyclovir hydrochloride hydrate is a potent antiviral agent. Valacyclovir hydrochloride hydrate can be used in the management of herpes simplex, herpes zoster and herpes B. Valacyclovir hydrochloride hydrate can be formulate ocular inserts for the treatment of ocular herpes. Valacyclovir hydrochloride hydrate is a prodrug and can be rapidly converted into acyclovir in vivo[1][2].
Antileishmanial agent-7 (compound 23) is a potent antileishmanial agent. Antileishmanial agent-7 shows antileishmanial activity against Leishmania donovani and L-6, with IC50 values of 6.89 and 259 μM, respectively[1].
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease[2].
Falcipain-2/3-IN-2 (Compound 12) is a dual falcipain-2 and falcipain-3 inhibitor[1].
HEX3 is a fragment of the adenoviral hexon. Hexon is the major capsid protein of adenovirion and is comprised of three identical polypeptide chains.
Quinidine hydrochloride monohydrate is a clinical anti-arrythmic drug which is also a potent blocker of K+ channel with an IC50 of 19.9 μM.
Descarbamoyl cefuroxime is a degradation product of Cefuroxime. Descarbamoyl cefuroxime is also an intermediate for the synthesis of Cephalosporin antibiotics[1][2].
Difloxacin hydrochloride is a broad-spectrum antibacterial drug. Difloxacin hydrochloride inhibits bacterial DNA gyrase and exhibits a concentration-dependant bactericidal effect by interference with the activity of DNA gyrase and topoisomerase IV[1].
Succinylsulfathiazole is a sulfonamide, it is an ultra long acting drug.
TSPP tetrasodium is a photosensitizer that has shown impressive effects in in vivo regression of cancer and microorganism infections (Ex: 413 nm, Em: 640 nm)[1][2].
(+)-SJ733 is a clinical candidate for malaria which can also inhibit Na+-ATPase PfATP4.
Kojibiose, an orally active prebiotic disaccharide, can specifically inhibit the activity of α-glucosidase I. kojibiose is a proliferation factor for Bifidobacterium, lactic acid bacteria, and eubacteria. kojibiose is a low-calorie sweetener capable of increasing the absorption of iron. Kojibiose exhibits antitoxic activity. Kojibiose reduces hepatic expression of inflammatory markers in vivo[1][2].
Delavirdine mesylate is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor (NNRTI) of HIV-1.
Moniliformin sodium salt is a potent, water-soluble mycotoxin isolate from Fusarium moniliforme.
SARS-CoV-2 Mpro-IN-9 (compound c7) is a nonpeptidic, noncovalent SARS-CoV-2 Mpro inhibitor (IC50=0.085 μM), with improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. SARS-CoV-2 Mpro-IN-9 inhibits viral replication (EC50=1.10 μM) in SARS-CoV-2-infected Vero E6 cells, while exhibits low cytotoxic effects (CC50>50 μM)[1].
Sodium Houttuyfonate is a natural compound extracted from Houttuynia cordata, with anti-inflammatory and anti-fibrotic effects. Sodium Houttuyfonate ameliorates LPS induced mastitis by inhibiting the NF κB pathway[1][2].
Azulene (Cyclopentacycloheptene) is as an isomer of naphthalene with high anti-HIV activity. Azulene, isolated from the distillation of chamomile oil, is a scaffold in medicinal chemistry[1][2][3].