Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com Anti-infection Anti-infectives are drugs that can either kill an infectious agent or inhibit it from spreading. Anti-infectives include antibiotics and antibacterials, antifungals, antivirals and antiprotozoals. Antibiotics specifically treat infections caused by bacteria, most commonly used types of antibiotics are: Aminoglycosides, Penicillins, Fluoroquinolones, Cephalosporins, Macrolides, and Tetracyclines. New other approaches such as photodynamic therapy (PDT) and antibacterial peptides have been considered as alternatives to kill bacteria. The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Viral infections occur when viruses enter cells in the body and begin reproducing, often causing illness. Viruses are classified as DNA viruses or RNA viruses, RNA viruses include retroviruses, such as HIV, are prone to mutate. The currently available antiviral drugs target 4 main groups of viruses: herpes, hepatitis, HIV and influenza viruses. Drug resistance in the clinical utility of antiviral drugs has raised an urgent need for developing new antiviral drugs. Antiprotozoal drugs are medicines that treat infections caused by protozoa. Of which, malaria remains a major world health problem following the emergence and spread of Plasmodium falciparum that is resistant to the majority of antimalarial drugs. At present, antimalarial discovery approaches have been studied, such as the discovery of antimalarials from natural sources, chemical modifications of existing antimalarials, the development of hybrid compounds, testing of commercially available drugs that have been approved for human use for other diseases and molecular modelling using virtual screening technology and docking. References: [1] Scorzoni L, et al. Front Microbiol. 2017 Jan 23;8:36. [2] Dehghan Esmatabadi MJ, et al. Cell Mol Biol (Noisy-le-grand). 2017 Feb 28;63(2):40-48. [3] Raymund R, et al. Mayo Clin Proc. 2011 Oct; 86(10):1009-1026. www.MedChemExpress.com 1 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com Target List in Anti-infection • Arenavirus 3 • Bacterial 6 • CMV 62 • Enterovirus 65 • Filovirus 67 • Fungal 69 • HBV 82 • HCV 86 • HIV 96 • HSV 110 • Influenza Virus 113 • Parasite 118 • Reverse Transcriptase 135 • RSV 140 • SARS-CoV 143 www.MedChemExpress.com 3 Arenavirus An arenavirus is a virus which is a member of the family Arenaviridae. These viruses infect rodents and occasionally humans. Arenaviruses are a diverse family of small, enveloped, single-stranded RNA viruses which are generally propagated through asymptomatic, chronic infection of specific rodent hosts. Several arenaviruses are significant human pathogens, including five distinct hemorrhagic fever viruses designated category A by the CDC and NIAID, which is indicative of the level of highest threat to civilian populations. Several arenaviruses, including Lassa virus (LASV), are causative agents of hemorrhagic fever, for which effective therapeutic options are lacking. The convergence of sensitivity to diverse small-molecule inhibitors thus identifies a robust new target for arenavirus antiviral discovery within the viral entry phase. 4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Arenavirus Inhibitors & Modulators GP(33-41) LHF-535 Cat. No.: HY-P0323 Cat. No.: HY-112762 Bioactivity: GP(33-41), a 9-aa-long peptide, is the optimal sequence of the Bioactivity: LHF-535 is an antiviral agent extracted from patent GP1 epitope of lymphocytic choriomeningitis virus, and can WO2013123215A2, Compound 38, has EC 50s of <1 μM, <1 b upregulate H-2D molecules at the RMA-S (Db Kb) cell surface μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg [1] with SC 50 of 344 nM. virus, respectively . Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg ST-193 ST-193 hydrochloride Cat. No.: HY-101441 Cat. No.: HY-101441A Bioactivity: ST-193 is a potent broad-spectrum arenavirus inhibitor; Bioactivity: ST-193 hydrochloride is a potent broad-spectrum arenavirus inhibits Guanarito, Junin, Lassa and Machupo virus with IC50 inhibitor; inhibits Guanarito, Junin, Lassa and Machupo virus with IC values of 0.44, 0.62, 1.4 and 3.1 nM, respectively. values of 0.44, 0.62, 1.4 and 3.1 nM, respectively. 50 Purity: 99.78% Purity: 98.22% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg www.MedChemExpress.com 5 Bacterial Anything that destroys bacteria or suppresses their growth or their ability to reproduce. Heat, chemicals such as chlorine, and antibiotic drugs all have antibacterial properties. Many antibacterial products for cleaning and handwashing are sold today. Such products do not reduce the risk for symptoms of viral infectious diseases in otherwise healthy persons. This does not preclude the potential contribution of antibacterial products to reducing symptoms of bacterial diseases in the home. 6 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Bacterial Inhibitors & Modulators (+)-(3R,8S)-Falcarindiol (+)-Camphor ((3R,8S)-Falcarindiol; 3(R),8(S),9(Z)-Falcarindiol) Cat. No.: HY-N1976 (D-(+)-Camphor; (1R)-(+)-Camphor) Cat. No.: HY-B1173 Bioactivity: (+)-(3R,8S)-Falcarindiol is a polyacetylene found in carrots, Bioactivity: (+)-Camphor is an ingredient in cooking, and as an embalming has antimycobacterial activity, with an IC 50 of 6 μM and fluid for medicinal purposes, MIC of 24 μM against Mycobacterium tuberculosis H37Ra [1] [2]. Antineoplastic and anti-inflammatory activity [2]. Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 10mM x 1mL in DMSO, 1 g (+)-Viroallosecurinine (R)-Ofloxacin Cat. No.: HY-N5002 (Dextrofloxacin) Cat. No.: HY-B0330D Bioactivity: (+)-Viroallosecurinine, isolated from Securinega virosa as a Bioactivity: (R)-Ofloxacin (Dextrofloxacin) is an antibiotic useful for the cytotoxic alkaloid, exhibits a MIC of 0.48 μg/mL for Ps. treatment of a number of bacterial infections [1]. [1] [1] Aeruginosa and Staph. aureus . Antibacterial activity . Antibacterial activity [1]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 5 mg 2-(Methylamino)-1H-purin-6(7H)-one 4(3H)-Quinazolinone (N2-methylguanine) Cat. No.: HY-101412 Cat. No.: HY-W018800 Bioactivity: 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is a Bioactivity: 4(3H)-Quinazolinone is a building block in chemical synthesis. modified nucleoside. 2-(Methylamino)-1H-purin-6(7H)-one is an Biologically active nitrogen heterocyclic compounds. Possesses endogenous methylated nucleoside found in human fluids. a wide spectrum of biological properties like antibacterial, antifungal, anticonvulsant, anti-inflammatory, anti-HIV, anticancerous and analgesic activities [1] [2]. Purity: 98.0% Purity: 97.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 100 mg 4-(tert-Butyl)-benzhydroxamic Acid 4-Chlorosalicylic acid Cat. No.: HY-114818 Cat. No.: HY-W016867 Bioactivity: 4-(tert-Butyl)-benzhydroxamic Acid is a PqsR antagonist with Bioactivity: 4-Chlorosalicylic acid is a pharmaceutical intermediate. Inhibits monophenolase and diphenolase activity with IC s IC50s of 12.5 μM and 23.6 μM for E. coli and P. aeruginosa, 50 respectively. 4-(tert-Butyl)-benzhydroxamic Acid reduces the of 1.89 mM and 1.10 mM. Potent antimicrobial activity. Against production of the virulence factor pyocyanin in P. aeruginosa<… E. coli with the MIC of 250 μg/mL and with the MBC of 500 μg/… Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 100 mg 4-Hydroxybenzoic acid 5-hydroxypyrazine-2-carboxylic acid Cat. No.: HY-Y0264 Cat. No.: HY-76210 Bioactivity: 4-Hydroxybenzoic acid, a phenolic derivative of benzoic acid, Bioactivity: 5-hydroxypyrazine-2-carboxylic acid , a metabolite of could inhibit most gram-positive and some gram-negative anti-tuberculosis drug pyrazinamide (PZA). bacteria, with an IC50 of 160 μg/mL. Purity: 98.0% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g 1 g www.MedChemExpress.com 7 6-Amino-5-azacytidine 7-Aminocephalosporanic acid Cat. No.: HY-111643 (7-ACA) Cat. No.: HY-B1434 Bioactivity: 6-Amino-5-azacytidine inhibits the growth of bacteria E. coli Bioactivity: 7-Aminocephalosporanic acid is the core chemical structure for [1]. the synthesis of cephalosporin antibiotics, is a potent β-lactamase inhibitor. Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 100 mg 10 mg A7132 AAI101 Cat. No.: HY-U00225 Cat. No.: HY-103095 Bioactivity: A7132 is an antibacterial agent. A7132 possess broad and Bioactivity: AAI101 is an extended-spectrum β-lactamase inhibitor, against potent antibacterial activity. many resistant Gram-negative pathogens. Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Acetohydroxamic acid Acetylazide (AHA) Cat. No.: HY-B1235 (Acetylkelfizina; Acetylsulfamethoxypyrazine; FI6073) Cat. No.: HY-101575 Bioactivity: Acetohydroxamic acid is a potent and irreversible inhibitor of Bioactivity: Acetylazide is a synthetic broad-spectrum bacteriostatic bacterial and plant urease and also used as adjunctive therapy antibiotic.