Antitubercular agent-9 shows effective antitubercular activity with a MIC value of 1.03-2.32 μM.
Capreomycin is a peptide antibiotic, commonly grouped with the aminoglycosides, which is given in combination with other antibiotics for MDR-tuberculosis.IC50 value:Target: The drug should not be given with streptomycin or other drugs that may damage the auditory vestibular nerve. Patients on this drug will often require audiology tests. It is a cyclic peptide.Capreomycin is administered intramuscularly and shows bacteriostatic activity.
Antibacterial agent 41 (example 3) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Imazalil (Enilconazole) sulfate is a fungicide, widely used in agriculture, particularly in the growing of citrus fruits, also used in veterinary medicine as a topical antimycotic.
HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1[1].
Asimicin (Bullatacin) is antitumor acetogenin that can be isolated from the bark and seeds of the pawpaw tree, Asimina trilobal Dunal. Asimicin inhibits mitochondrial respiration through the inhibition of complex I. Asimicin shows toxicity to Aphis gossypii, mosquito larvae and mammalian[1][2][3][4].
Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2[1].
Protopine hydrochloride, an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine hydrochloride exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity[1][2].
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for therapeutic intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals[1].
Aeruginosin 98-B is a protease inhibitor. Aeruginosin 98-B inhibits trypsin, plasmin and thrombin with IC50 values of 0.6, 7.0 and 10.0 μg/mL, respectively[1].
1-Phenylsemicarbazide is an antifungal agent. 1-Phenylsemicarbazide has the potential for preventing mold growth on industrial products[1].
Camphor ((±)-Camphor) is a topical anti-infective and anti-pruritic and internally as a stimulant and carminative. However, Camphor is poisonous when ingested. Antiviral, antitussive, and anticancer activities[1]. Camphor is a TRPV3 agonist[2].
Gomisin M2 ((+)-Gomisin M2) is a lignan isolated from the fruits of Schisandra rubriflora with anti-HIV activity (EC50 of 2.4 μM). Gomisin M2 exhibits anti-cancer and anti-allergic activities and has the potential for Alzheimer’s disease research[1][2].
Thymol iodide is a compound of Iodide and Thymol. Thymol iodide acts as a substitute for iodoform[1]. Thymol iodide is an iodine derivative of Thymol (a phenol derived from thyme oil), which is mostly used as mild antiseptic and fungicide[2].
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity[1][2].
Tebuconazole is an agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively.
Polistes mastoparan is an antimicrobial peptide. Polistes mastoparan increases S. aureus cell K+ efflux and inhibits cell viability with EC50 of 5 μM[1].
Clindamycin is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla)[1].
SARS-CoV-2 Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent Mpro inhibitor (IC50=0.40 μM) with good anti-SARS-CoV-2 activity (EC50=1.1 μM). SARS-CoV-2 Mpro-IN-2 can be used in COVID-19 studies[1].
Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A[1][2].
Dehydrocavidine, a main active ingredient of Corydalis saxicola Bunting (Yanhuanglian), displays antinociceptive, hepatoprotective, and spasmolytic activities. Dehydrocavidine kills hepatitis viruses and promotes regeneration of hepatocytes[1].
FNC-TP is the intracellular active form of FNC. FNC is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV[1].
Antibacterial agent 143 (Compound 5a) is an antibacterial agent with MICs of 25, 25, 50 and 50 μg/mL against B. subtilis ATCC6633, . aureus ATCC6538, P. aeruginosa ATCC13525 and E. coli ATCC35218, respectively[1].
NIM811 (SDZ NIM811) is a potent mitochondrial permeability transition inhibitor. Sequence: Cyclo[{Aaa}-{Abu}-{Sar}-Ile-Val-Leu-Ala-{D-Ala}-Leu-Leu-Val].
Kakuol is a natural compound isolated from the rhizomes of Asarum sieboldii. Antifungal activity[1].
Chitinase-IN-1 is a insect chitinase and N- acetyl hexosaminidase inhibitor and pesticide; 50 uM/20 uM compound concentration's inhibitory percentage are 75%/67% for chitinase/N- acetyl-hexosaminidase respectively.
Nimorazole (K-1900) is a nitroimidazole anti-infective.
Pipecolic acid is a metabolite of lysine.
BRD-6929 (Cpd-60) is a brain-penetrant, selective inhibitor of HDAC1 and HDAC2 (IC50= 1 and 8 nM), extracted from patent US2018360927[1]. BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively[2]. BRD-6929 (TPB) potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1[3].
Murrayanol is a natural carbazole alkaloid with a variety of biological activities. Murrayanol shows anti-inflammatory, topoisomerase I and topoisomerase II (Topoisomerase) inhibition activities. Murrayanol also as a mosquitocidal and antimicrobial[1].