Archiv der Pharmazie

Five new immunomodulators 1a–1e were synthesized by using a trans-4-alkyl-substituted cyclohexane to replace the flexible C8 alkyl chain of fingolimod. They show therapeutic effects on the DNFB-induced DTH reaction and inhibitory effects on antigen-specific T-cell proliferation.

This study shows how and to what extent the position of side chain substituents affects telomerase activity. Four series of compounds containing an anthraquinone-linked moiety and symmetrical or asymmetrical aminoacyl residues were synthesized and evaluated for their inhibitory effects towards telomerase and hTERT expression.

Among these new compounds, compound IIh is the most potent inhibitor of AChE and BuChE with an IC₅₀ value of 66 ± 0.71 µg/mL and 48.75 ± 2.48 µg/mL, respectively.

A new series of benzo[6,7]cyclohepta[1,2-d]triazolo[4,3-a]pyrimidines 8a–l was synthesized via reaction of heterocyclic thione 4 or its methyl derivatives 10 with hydrazonoyl halides 5a–l. Also, reaction of compound 4 with a mixture of chloroacetic acid and aromatic aldehyde derivatives gave benzo[6,7]cyclohepta[1,2-d]thiazolo[3,2-a]pyrimidin-3-ones 12–14. All the newly synthesized products were screened against 5α-reductase and showed activities with good ED₅₀ for all compounds.

New bisphosphonates and bisphosphonic acids were synthesized and screened for anti-tumor activity. The results indicate that this moiety is an essential factor in developing the total pharmacological properties for the synthesized compounds whereas the type of the substituents attached to the quinoline nucleus determines and controls the potency.

Regioisomers of fluoronitrobenzothiazolo pyrazoline were synthesized and their activity on the Mycobacterium tuberculosis H37Rv strain was compared to the standard drugs streptomycin and pyrazinamide. The results revealed that the introduction of an NO₂ group at the “5-position” of the benzothiazole ring (12a–f) increased the antitubercular activity.

A novel series of pyrazole derivatives were synthesized and tested for their in vivo anti-malarial activity using mice infected with chloroquine sensitive P. berghei and P. falciparum. Compound 8b (R¹ = Cl, R² = COOH) was the most active with an IC₅₀ of 0.0326 ± 0.014  µM. This finding was supported by the docking results performed for the active compounds. The acute toxicity studies of the active compounds revealed that they have a good safety profile.

New synthesized pyrazolopyridine derivatives were screened for their antioxidant properties. Some of the tested compounds as 1, 14, 15, 23, 26, 29a, 30 and 32 have the ability to protect DNA from the damage induced by bleomycin.

Novel biphenylpyrimidines showing substituted benzylthio groups were synthesized and evaluated for their antibacterial and antifungal activity. All synthesized compounds have significant biological activity against the tested microorganisms. Compounds 8a, 8b, 8c, 8e, 8f, 8i, and 8j exhibited good antimicrobial activity.