- Pyrimethamine(RP4753) is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR).
- Sitafloxacin is a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections. Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci.
- Seyedeh Bita Mousavinafchi, .et al. , Food Sci Nutr, 2022, Nov 21;11(2):1142-1153 PMID: 36789060
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CCR5 antagonist
Vicriviroc Malate is a second generation orally active CCR5 antagonist, which is also a potent inhibitor of HIV-1 entry into target cells, with a mean IC50 =0.46 nM and IC50 =1~10 nM to HIV isolates (n=52).- Tomohiro Nabekura, .et al. , Antimicrob Agents Chemother, 2015, Dec; 59(12): 7666-7670 PMID: 26416870
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CCR2 antagonist
MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2 on human monocytes and low nM in the chemotaxis assay. It has good PK profiles in preclinical species and demonstrated efficacy in animal models.- Murakami K, .et al. , Vet Immunol Immunopathol, 2016, Dec;182:52-58 PMID: 27863550
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CCR2 Antagonist
INCB8761(PF-4136309) is a potent, selective, and orally bioavailable CCR2 antagonist. -
NS3 protease inhibitor
Asunaprevir is an inhibitor of the viral enzyme serine protease NS3.- Mahim Khan, .et al. , BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
- Kato N, .et al. , Arch Virol, 2019, Dec 12 PMID: 31832864
- Fay EJ, .et al. , J Virol, 2018, Fay EJ PMID: 30282710
- Bennie Lemmens, .et al. , Mol Cell, 2018, Jul 5; 71(1): 117-128.e3 PMID: 30008317
- Ueda Y, .et al. , Virus Res, 2017, May 2;235:37-48 PMID: 28322919
- Furihata T, .et al. , Int J Antimicrob Agents, 2015, Oct;46(4):381-8 PMID: 26163159
- Tomomi Furihata, .et al. , Antimicrob Agents Chemother, 2014, 58(8): 4555-4564 PMID: 24867984
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β-lactamase inhibitor
Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor.- Lara Muñoz-Muñoz, .et al. , Antibiotics (Basel), 2023, Feb; 12(2): 335 PMID: 36830246
- Moonsuk Bae, .et al. , Antibiotics (Basel), 2021, Dec 5;10(12):1492 PMID: 34943704
- Taeeun Kim, .et al. , Antibiotics (Basel), 2020, Dec 15;9(12):912 PMID: 33334045
- Annelien Everaert, .et al. , Antimicrob Resist Infect Control, 2016, 5: 44 PMID: 27895902
- Avermectin B1a is an antiparasitic agent that paralyzes nematodes without causing hypercontraction or flaccid paralysis.
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Polymerase inhibitor
Balapiravir (R1626, RG1626) is the prodrug of a nucleoside analogue inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase (R1479, RG1479). -
NNRT inhibitor
Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV. - Faropenem daloxate is the first oral penem in a new class of beta-lactam antibiotics.
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HCV Nucleoside Inhibitor
PSI-6130(R 1656) is a Hepatitis C Virus Nucleoside Inhibitor.- Amitava Adhikary, .et al. , J Am Chem Soc., 2014, 136(44): 15646-15653 PMID: 25296262
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NNRT inhibitor
Rilpivirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs, such as efavirenz. -
NS5B polymerase inhibitor
Tegobuvir (GS-9190 is a non-nucleoside NS5B polymerase inhibitor. -
CCR4 antagonist
GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96??0.11. -
NNRT inhibitor
MK-1439 is a non-nucleoside reverse transcriptase inhibitor -
HIV protease inhibitor
Fosamprenavir is a prodrug of amprenavir, an inhibitor of human immunodeficiency virus (HIV) protease. -
CCR 2 antagonist
Teijin compound 1 is a specific CCR 2 antagonist with IC50s of 24 and 180 nM in chemotaxis and binding assay, respectively. -
IMPDH inhibitor
AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).
- Kevin Chiem, .et al. , Microbiol Spectr, 2023, Aug 17;11(4):e0474522 PMID: PMC10434227
- Desarey Morales Vasquez, .et al. , Viruses, 2020, Sep; 12(9): 1041 PMID: 32961956
- Park JG, .et al. , J Virol, 2020, Mar 17;94(7) PMID: 31941776
- Dunham EC, .et al. , Antiviral Res, 2018, Sep;157:140-150 PMID: 30031760
- Quinupristin is a semi-synthetic analogue of virginiamycin B (ostreogyrcin B, pristinamycin IA, Streptogramin B) formed by a Mannich condensation and elimination to generate an exocyclic methylene alpha to the ketone of the 4-piperidinone.
- Prodigiosin (Prodigiosine) is a secondary metabolite of Symbiotic bacteria, with anti-fungal and anti-cancer activity.
- Erythromycin Cyclocarbonate, derivative of Erythromycin, inhibits protein synthesis of bacteria by binding to the 50S ribosome.
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NF-κB inhibitor
SC75741 is a potent NF-kB inhibitor with EC50 of 200 nM.- Yunshang Yang, .et al. , Biomed Pharmacother, 2023, Feb;158:114113 PMID: 36516692
- Yajun Li, .et al. , Cell Prolif, 2022, Oct;55(10) PMID: 35708050
- Crystal A Mendoza, .et al. , Antiviral Res, 2021, Jan;185:104993 PMID: 33296695
- Amadacycline is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.
- Amadacycline methanesulfonate is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.
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HIV-1 attachment inhibitor
BMS-663068 is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.- Min Li, .et al. , Nat Commun, 2020, 11: 4051 PMID: 32792548
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HIV-1 attachment inhibitor
BMS-663068 tris is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection. -
CCR5 antagonist
Vicriviroc maleate is a CCR5 antagonist with IC50 of 0.91 nM in clinical development for the treatment of HIV-1. -
HCV Polymerase Inhibitor
VCH-759 is a non-nucleoside inhibitor of HCV RNA-dependent polymerase with sub-micromolar IC50 values versus genotype 1a/1b replicons.- Hassan GS, .et al. , Eur J Med Chem, 2019, Oct 1;184:111747 PMID: 31604164
- Oritavancin is a novel semisynthetic glycopeptide antibiotics. On August 6, 2014, the FDA approved oritavancin for treatment of skin infections. Oritavancin possesses potent and rapid bactericidal activity in vitro against a broad spectrum of both resistant and susceptible Gram-positive bacteria, including Staphylococcus aureus, MRSA, enterococci, and streptococci.
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Calcineurin/PP2B inhibitor
Ascomycin is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. It has been researched for the treatment of autoimmune diseases and skin diseases, and to prevent rejection after an organ transplant.