- Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.
- Thanh Quang Nguyen, .et al. , Microbiol Spectr, 2023, Jun 15;11(3):e0063123 PMID: 37158736
- Zewen Wen, .et al. , J Antibiot (Tokyo), 2022, Sep;75(9):498-508 PMID: 35896611
- Xiaoming Liu, .et al. , J Antibiot (Tokyo), 2022, Aug;75(8):463-471 PMID: 35760902
- Sato T, .et al. , Microb Drug Resist, 2018, Jul/Aug;24(6):860-867 PMID: 29232167
- Dinah B. Aziz, .et al. , Front Microbiol, 2018, May 11 PMID: 29867841
- Toyotaka Sato, .et al. , Antimicrob Agents Chemother, 2017, Feb; 61(2): e01654-16 PMID: 27855067
- Bacitracin is a mixture of related cyclic polypeptides produced by organisms of the licheniformis group of Bacillus subtilis var Tracy, which disrupts both gram positive and gram negative bacteria by interfering with cell wall and peptidoglycan synthesis.
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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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HCV Protease inhibitor
VX-222 is a small molecule non-nucleoside inhibitor of HCV NS5B polymerase that is being investigated for the treatment of hepatitis C virus infection.- Wataru Ito, .et al. , Antivir Chem Chemother, 2015, Dec; 24(5-6): 148-154 PMID: 27503576
- Hui Shen, .et al. , PLoS One., 2013, 8(12): e82299 PMID: 24358168
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nucleoside analogue reverse transcriptase inhibitor
Zalcitabine is a potent nucleoside analogue reverse transcriptase inhibitor used in the treatment of HIV infection. -
Hsp90 inhibitor
Geldanamycin binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity.- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
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HIV integrase inhibitor
S/GSK1349572 is a potent next generation HIV integrase inhibitor and demonstrates a superior resistance profile substantiated with 60 integrase mutant molecular clones.- Lea El Khoury, .et al. , PeerJ Preprints, 2019, 7:e27833v1
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HCCR2 antagonist
INCB 3284 dimesylate is a potent, selective hCCR2 antagonist that exhibits potenct antagonism against monocyte chemoattractant molecule binding to hCCR2 and chemotaxis activity. -
Transcriptase inhibitor
Abacavir sulfate is a nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS. -
Neuraminidase Inhibitor
Peramivir is a neuraminidase inhibitor, acting as a transition-state analogue inhibitor of influenza neuraminidase and thereby preventing new viruses from emerging from infected cells.- Daisuke Kato, .et al. , PLoS One, 2018, 13(7): e0200761 PMID: 30001430
- Yuuki Kurebayashi, .et al. , PLoS One, 2016, 11(5): e0156400 PMID: 27232333
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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. -
protein synthesis inhibitor
Retapamulin is an antibacterial agent, specifically a protein synthesis inhibitor- Merianne Mohamad, .et al. , Nucleic Acids Res, 2022, Feb 28;50(4):2128-2142 PMID: 35137182
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HIV Entry Inhibitor
BMS-806, also known as BMS-378806 , is a type of medicine called an entry inhibitor. Entry inhibitors work by blocking HIV from entering human cells. BMS-378806 (BMS-806) is a small molecule that blocks the binding of host-cell CD4 with viral gp120 protein and therefore inhibits the first steps of HIV-1 infection. -
Reverse transcriptase inhibitor
Entecavir hydrate is a nucleoside analog (more specifically, a guanosine analogue) that inhibits reverse transcription, DNA replication and transcription in the viral replication process. Entecavir is an oral antiviral drug used in the treatment of hepatitis B infection.- Masaaki Toyama, .et al. , Antimicrob Agents Chemother, 2022, Jun 21;66(6) PMID: 35604213
- Toyama M, .et al. , Virus Res, 2019, Oct 2;271:197677 PMID: 31376401
- Kazumoto Murata, .et al. , Gut, 2018, Feb; 67(2): 362-371 PMID: 27789659
- Jianfei L, .et al. , Biochem Pharmacol, 2017, Dec 15;146:224-232 PMID: 29038020
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HCV replication Inhibitor
Anguizole is a small molecule inhibits HCV replication and alters NS4B's subcellular distribution.- Choi M, .et al. , Virus Genes., 2013, Dec;47(3):395-407 PMID: 23868571
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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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HCV Protease Inhibitor
Boceprevir is a protease inhibitor used as a treatment for hepatitis C genotype 1.- Ueda Y, .et al. , Virus Res, 2017, May 2;235:37-48 PMID: 28322919
- Shirasaki T, .et al. , Hepatology., 2014, 60(5):1519-30 PMID: 24962339
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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). -
NS5A inhibitor
BMS-790052 is an NS5A inhibitor under investigation for the treatment of hepatitis C virus (HCV) infection.- Shirasaki T, .et al. , Hepatology., 2014, 60(5):1519-30 PMID: 24962339
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HCV NS3 protease Inhibitor
Ciluprevir is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease.- Mahim Khan, .et al. , BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
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HIV Protease Inhibitor
Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. Saquinavir inhibits both HIV-1 and HIV-2 proteases.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- PA-824 is an experimental anti-tuberculosis drug.
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Thanh Quang Nguyen, .et al. , Antimicrob Agents Chemother, 2022, Dec 20;66(12):e0044822 PMID: 36321819
- Wang X, .et al. , Cell Chem Biol, 2019, Nov 7. pii: S2451-9456(19)30355-1 PMID: 31711854
- Alexandre López-Gavín, .et al. , Int J Antimicrob Agents., 2015, Nov;46(5):582-5 PMID: 26421981
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NNRT inhibitor
Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV. -
HSV DNA replication inhibitor
Fiacitabine is a selective inhibitior of DNA replication of herpes simplex virus(HSV) with IC50 values of 2.5 nM and 12.6 nM for HSV1 and HSV2, respectively. - Faropenem daloxate is the first oral penem in a new class of beta-lactam antibiotics.
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HIV-1 integrase inhibitor
HIV-1 integrase inhibitor is uesful for anti-HIV. -
HIV-1 integrase inhibitor
HIV-1 integrase inhibitor 2, in the treatment of human immunodeficiency virus (HIV) infection. -
HIV-1 protease inhibitor
Nelfinavir is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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NS3 protease inhibitor
Narlaprevir is a potent, selective, orally bioavailable NS3 protease inhibitor(Ki=6 nM; EC90=40 nM) -
influenza virus neuraminidase inhibitor
Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses. -
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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HCV Nucleotide Inhibitor
PSI-7977 is a phosphoramidate prodrug of PSI-7851, a nucleoside analog that, when phosphorylated, inhibits the RNA-dependent RNA polymerase of hepatitis C virus (EC50 = 92 nM).- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
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influenza virus neuraminidase (NA) inhibitor
Peramivir trihydrate (RWJ-270201 trihydrate;BCX-1812 trihydrate) is a highly potent, selective and orally active influenza virus neuraminidase (NA) inhibitor, with IC50 values ranging from 0.9 to 4.3 nM for nine NA subtypes. -
HCV NS5B polymerase inhibitor
Mericitabine (RG 7128; R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication. -
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.