(R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine[1]. Hydroxychloroquine is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro[2][3][4].
(-)-Corypalmine (Discretinine), an alkaloid that could be isolated from the stem of Guatteriopsis friesiana, possesses antimicrobial activity[1].
Glurate (4-Acetylbutyric acid; 5-Oxohexanoic acid) can be used to construct antiviral agents (acyclic nucleoside esters) (extracted from patent WO1997030052A1)[1].
Antifungal agent 30 (compound A18) is a potent antifungal agent. Antifungal agent 30 shows excellent antifungal activity against Candida albicans (CPCC400616) and Aspergillus fumigatus, with MIC of 0.03 and 0.5 μg/mL, respectively. Antifungal agent 30 also shows excellent antifungal activity against fluconazole-resistant strains. The potent antifungal activity of Antifungal agent 30 mainly causes by hydrogen and coordination bond interaction with the CYP51[1].
DENV-IN-7, a flavone analog, is a dengue virus (DENV) inhibitor with an EC50 value of 70 nM. DENV-IN-7 has low toxicity against normal cell and anti-dengue activity[1].
ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.
Pazufloxacin (T-3761) is a fluoroquinolone antibiotic.Target: AntibacterialPazufloxacin (T-3761), a new quinolone derivative, showed broad and potent antibacterial activity. T-3761 showed good efficacy in mice against systemic, pulmonary, and urinary tract infections with gram-positive and gram-negative bacteria, including quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa. The in vivo activity of T-3761 was comparable to or greater than those of ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin against most infection models in mice. The activities of T-3761 were lower than those of tosufloxacin against gram-positive bacterial systemic and pulmonary infections in mice but not against infections with methicillin-resistant Staphylococcus aureus [1]. T-3761 had a broad spectrum of activity and had potent activity against gram-positive and -negative bacteria. The MICs of T-3761 against 90% of the methicillin-susceptible Staphylococcus aureus, methicillin-susceptible and -resistant Staphylococcus epidermidis, and Clostridium spp. tested were 0.39 to 6.25 micrograms/ml. The MBCs of T-3761 were either equal to or twofold greater than the MICs. The 50% inhibitory concentrations of T-3761 for DNA gyrases isolated from E. coli and P. aeruginosa were 0.88 and 1.9 micrograms/ml, respectively [2].
Antitrypanosomal agent 9 (compound 1) is a potent antitrypanosomal agent. Antitrypanosomal agent 9 shows inhibitory activity against T. b. brucei, with an IC50 of 1.15 μM. Antitrypanosomal agent 9 can be used for human African trypanosomiasis (HAT) research[1].
Doripenem monohydrate is a new member of the carbapenem class of beta-lactam antibiotics with broad-spectrum coverage of Gram-positive, Gram-negative and anaerobic pathogens.Target: AntibacterialDoripenem is an ultra-broad-spectrum injectable antibiotic. It is a beta-lactam and belongs to the subgroup of carbapenems. It was launched by Shionogi Co. of Japan under the brand name Finibax in 2005 and is being marketed outside Japan by Johnson & Johnson. It is particularly active against Pseudomonas aeruginosa. It is recommended that those allergic to doripenem or to any type of beta-lactam antibiotics such as cephalosporin or other Carbapenems not receive doripenem.Doripenem appears as crystalline powder anywhere from a white to somewhat yellowish colour.Doripenem is moderately soluble in water, slightly soluble in methanol, and virtually insoluble in ethanol. Doripenem is also solution in N,N-dimethylformamide. Doripenem's chemical configuration has 6 asymmetrical carbon atoms (6 stereocentres) and is most commonly supplied as one pure isomer. In terms of doripenem for injection, the crystallized powered drug can form a monohydrate when mixed with water. However, Doripenem has not been proven to possess polymorphism.
HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.
Quellenin is an anti-saprolegnia compound. Quellenin can be isolated from deep-sea fungus Aspergillus sp. YK-76[1]
Pazufloxacin (T-3761) mesylate is a fluoroquinolone antibiotic.Target: AntibacterialPazufloxacin (T-3761), a new quinolone derivative, showed broad and potent antibacterial activity. T-3761 showed good efficacy in mice against systemic, pulmonary, and urinary tract infections with gram-positive and gram-negative bacteria, including quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa. The in vivo activity of T-3761 was comparable to or greater than those of ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin against most infection models in mice. The activities of T-3761 were lower than those of tosufloxacin against gram-positive bacterial systemic and pulmonary infections in mice but not against infections with methicillin-resistant Staphylococcus aureus [1]. T-3761 had a broad spectrum of activity and had potent activity against gram-positive and -negative bacteria. The MICs of T-3761 against 90% of the methicillin-susceptible Staphylococcus aureus, methicillin-susceptible and -resistant Staphylococcus epidermidis, and Clostridium spp. tested were 0.39 to 6.25 micrograms/ml. The MBCs of T-3761 were either equal to or twofold greater than the MICs. The 50% inhibitory concentrations of T-3761 for DNA gyrases isolated from E. coli and P. aeruginosa were 0.88 and 1.9 micrograms/ml, respectively [2].
Fellutanine A, a diketopiperazine alkaloid, is a fungal metabolite from cultures of Penicillium fellutanum[1].
(-)-Isocorypalmine, an alkaloid isolated from Corydalis chaerophylla, possesses antifungal activity[1].
Thiethylperazine dimaleate is a phenothiazine derivate, and an orally active dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a slective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
Antibacterial agent 129, an oxetanyl-quinoline derivative, has shown good antibacterial activity against P. mirabilis and B. subtilis with MICs of 31.25 μM and 31.5 μM and . Antibacterial agent 129 shows good antifungal activity against A. niger with a MIC of 31.25 μM. Antibacterial agent 129 shows excellent antimycobacterial activity with MIC 57.73 μM for M. tuberculosis H37Rv[1].
Ratjadone is a potent antifungal agent. Ratjadone has antifungal activity with MIC values in the range from 0.04 to 0.6 µg/mL for Mucor hiemalis, Phythophthora drechsleri, Ceratocystis ulmi, and Monilia brunnea[1].
(E)-Ethyl p-methoxycinnamate is a natural product found in Kaempferia galangal with anti-inflammatory, anti-neoplastic and anti-microbial effects. (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 in vitro with IC50s of 1.12 and 0.83 μM, respectively[1].
PD-1/PD-L1-IN 5 is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM[1].
ASN 07115873 is an anti-ZIKV compound (IC50: 189.2 pM), and can be used for antiviral research[1].
Sulfabrom (N 3517; Sulfabromomethazine) is a long-acting veterinary medicine that is used for the treatment of coccidiosis and various bacterial infections in the poultry, swine and cattle.
Antibiotic-202 is an antibiotic compound, for treating bacterial infections. Target: AntibacterialAntibiotic-202 is useful for the treatment or prevention of bacteria infections.
Antifungal agent 1 is a potent antifungal agent.
1,3,6-Trihydroxy-5-methoxyxanthone is a nature product that could be isolated form the root bark of Tovomita krukovii. 1,3,6-Trihydroxy-5-methoxyxanthone has anti-fungal effect[1][2].
Pyoluteorin is an antibiotic that inhibits Oomycete fungi, including the plant pathogen Pythium ultimum, and suppresses plant diseases caused by this fungus[1]. Pyoluteorin induces human triple-negative breast cancer MDA-MB-231 cells apoptosis in vitro. Pyoluteorin can be used for the research of human triple-negative breast cancer[2].
Sulfamoxole is a broad- spectrum chemotherapeutic antimicrobial agent. Sulfamoxole can be used for the study of pediatric infections[1].
EBOV/MARV-IN-2 (compound 13) is an Ebolavirus (EBOV, IC50=0.9 μM) and Marburg virus (MARV, IC50=2.7 μM) inhibitor[1].
Tobevibart is an IgG1-lambda, anti-HBV (hepatitis B virus) surface envelope protein humanized monoclonal antibody. Tobevibart shows antiviral activity[1].
JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC50: 5 nM). JAK2-IN-9 inhibits the phosphorylation of JAK2, STAT3, and STAT5. JAK2-IN-9 has metabolic stabilities. JAK2-IN-9 induces apoptosis. JAK2-IN-9 can be used for research of myeloproliferative neoplasms (MPNs)[1].
Methyl caffeate, an antimicrobial agent, shows moderate antimicrobial and prominent antimycobacterial activities. Methyl caffeate also exhibits α-glucosidase inhibition activity, oxidative stress inhibiting activity, anti-platelet activity, antiproliferative activity in cervix adenocarcinoma and anticancer activity in lung and leukmia cell lines[1].