Microbiologia/Virologia

<p>Cephalosporin C exhibits relatively weak resistance to Gram-positive and Gram-negative bacteria. It is stable against penicillinase, but can be decomposed by cephalosporinase. When hydrolyzed to remove its side chain, it yields 7-amino-cefenoic acid (7-ACA), which is an essential raw material for the production of semisynthetic cephalosporins.</p>

Colistin adjuvant-2 is a compound that acts as a potentiation agent for colistin, effectively enhancing its activity against Gram-negative bacteria [1].

Faldaprevir sodium: HCV treatment, inhibits NS3/NS4A protease, P-glycoprotein, CYP3A4, UGT1A1.

3'-NH-Tr-2',3'-DMF-ddA-5'-CE-Phosphoramidite serves as a precursor of adenosine nucleotide monomers used in the solid-phase synthesis of oligonucleotides, particularly for modifying oligonucleotides such as terminally modified DNA strands. It features Trityl (Tr), Cyanoethyl (CE), and Dimethylformamidine (DMF) protective groups, classifying it as a ddNTP adenosine nucleoside suitable for applications like oligonucleotide solid-phase synthesis, probe design, and chain termination sequencing.

Antifungalagent 127 (Compound 6c) is an antifungal agent with potent inhibitory activity against Botrytis cinerea and Rhizoctonia solani.

AB25583 is a small molecule inhibitor of Polθ helicase (Polθ-hel) with an IC50 of 6 nM. It selectively kills cells deficient in BRCA1/2 and synergizes with Olaparib in cancer cells harboring pathogenic BRCA1/2 mutations. AB25583 can be utilized in tumor research.

KL-50, a selective toxin, effectively targets tumors deficient in the DNA repair protein O6-methylguanine-DNA-methyltransferase (MGMT), which corrects O6-alkylguanine lesions. This compound induces both DNA damage response pathways and cell cycle arrest in MGMT-deficient cells, regardless of mismatch repair (MMR) status. KL-50 shows promise in the study of brain tumors lacking MGMT.

<p>MBX-1162, a bis-indole compound, has demonstrated unique substrate specificity related to MepA and MepR in studies investigating its resistance mechanisms in Staphylococcus aureus. It has not shown cross-resistance with related compounds.</p>

Laninamivir trifluoroacetate, a long-acting antiviral, treats and prevents Influenza A and B via nasal spray.

<p>And1 degrader 1 (Compound A15) is a degrader of acidic nucleoplasmic DNA-binding protein 1 (And1) that notably induces degradation of And1 in NSCLC cells. When combined with Olaparib (1 μM), And1 degrader 1 at a concentration of 5 μM effectively inhibits proliferation in A549 and H460 cells. This compound is applicable in cancer research studies.</p>

K13787 is an acetohydroxy acid synthase (AHAS) inhibitor with antibacterial properties. It exhibits antimicrobial activity against various non-tuberculous mycobacteria (NTM) as well as clarithromycin (CLR) resistant strains.

XR8-89, a potent PLpro inhibitor (IC50=0.1μM), blocks SARS-CoV-2 replication; useful for research.

BMS-818251 is a potent small-molecule inhibitor that targets HIV-1 entry, with an EC50 value of 0.019 nM. It exhibits over 10 times greater efficacy on the cross-subtype panels of the 208-HIV-1 strain compared to BMS-626529. BMS-818251 enhances potency through interactions with gp120 residues in the conserved β20-β21 hairpin.

<p>Lamivudine, a drug for HIV-1 and HBV, inhibits reverse transcriptase and resembles zalcitabine.</p>

UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 values of 15 nM and 19 nM, respectively. It is effective in inhibiting invasion and migration of TNBC cells in vitro. Additionally, UNC0638 hydrate acts as an inhibitor of EHMT1/2 and induces the expression of fetal hemoglobin (HbF) in cultures of human erythroid progenitor cells. Furthermore, it exhibits antiviral activity against FMDV (foot-and-mouth disease virus) and VSV (vesicular stomatitis virus), demonstrating remarkable potency and selectivity across various epigenetic and non-epigenetic targets.

NNRT-IN-5 (compound 10d) is an orally available non-nucleoside reverse transcriptase (Reverse Transcriptase) inhibitor.

Apalcillin (PC-904) combined with Ro 48-1220 (a penicillin sulfone β-lactamase inhibitor) exhibits broad-spectrum activity against Gram-negative aerobic and anaerobic bacteria, excluding Klebsiella acid-producing strains. This combination shows strong efficacy against β-lactamase-producing Moraxella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae with an effective MIC of 11 μg/mL. Additionally, it inhibits Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter at low MICs (0.25 to 4 μg/mL). However, it has limited efficacy against oxacillin-resistant staphylococci and some Gram-positive bacteria. Apalcillin/Ro 48-1220's effectiveness against certain extended-spectrum β-lactamase-producing Escherichia coli is comparable to piperacillin/tazobactam, though it is less effective against SHV-type β-lactamases.

7-APRA is a semisynthetic intermediate of the cephalosporin class of antibiotics. It exhibits antibacterial activity and is primarily used in the synthesis of other cephalosporin antibiotics, such as Cefaclor and Cefprozil.

<p>Griseofulvic Acid ((±)-Griseofulvic acid) is a metabolite of the antifungal agent Griseofulvin. It induces protein aggregation and tubulin polymerization in cell-free assays.</p>

Antibacterial agent 113 targets multiple bacteria including P. aeruginosa and E. coli, showing efficacy at MIC 15625 μM.