4-(4-Chlorophenyl)thiazol-2-amines as pioneers of potential neurodegenerative therapeutics with anti-inflammatory properties based on dual DNase I and 5-LO inhibition.

Eleven new 4-(4-chlorophenyl)thiazol-2-amines were synthesized and, together with nine known derivatives, evaluated in vitro for inhibitory properties towards bovine pancreatic DNase I. Three compounds (18-20) inhibited DNase I with IC values below 100 µM, with compound 19 being the most potent (IC = 79.79 µM).

Synthesis and DNase I inhibitory properties of new benzocyclobutane-2,5-diones.

Eight new benzocyclobutane-2,5-diones (-) were synthesized, and their inhibitory properties against bovine pancreatic DNase I were examined . Compounds - were synthesized using photocycloaddition of duroquinone with various phenyl-substituted ethylenes in the presence of 18W compact fluorescent lamp (visible light). Two compounds, 1,3,4,6-tetramethyl-7-phenylbicyclo[4.

Rutin as Deoxyribonuclease I Inhibitor.

DNase I inhibitory potential of water extract of nine Hypericum species (H. umbellatum, H. barbatum, H.

Synthesis, Antimicrobial Activity and in silico Studies on Eugenol Eters.

The results presented herein represent our continued study based on the modification of phenolic functionality in molecules originated from natural sources by acylation. A small focused library of nineteen eugenyl esters, with four of which are new compounds, is reported. All compounds were subjected to in vitro antimicrobial testing.

Synthesis and DNase I inhibitory properties of some 4-thiazolidinone derivatives.

Twelve new thiazolidinones were synthesized and, together with 41 previously synthesized thiazolidinones, evaluated for inhibitory activity against deoxyribonuclease I (DNase I) in vitro. Ten compounds inhibited commercial bovine pancreatic DNase I with an IC below 200 μM and showed to be more potent DNase I inhibitors than crystal violet (IC  = 365.90 ± 47.

Synthesis and DNase I inhibitory properties of some 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidines.

A series of six novel and six known thieno[2,3-d]pyrimidin-4-amines 2-13 were synthesized, and further were used as a starting material for preparation of a small series of eight novel thieno[2,3-d]pyrimidin-4-phthalimides 14-21. Eight compounds, five amine and three phthalimide derivatives, inhibited bovine pancreatic DNase I with an IC below 200 µM, being more effective than referent inhibitor crystal violet. Phthalimide derivatives 16, 18 and 19 exhibited higher DNase I inhibitory activity compared to their amine precursors 7, 10 and 11.

Benzimidazoles as novel deoxyribonuclease I inhibitors.

Inhibitory potential of 19 benzimidazoles against bovine pancreatic deoxyribonuclease I (DNase I) was investigated in vitro. Three compounds inhibited DNase I with IC below 100 μM and proved to be more potent DNase I inhibitors than crystal violet (IC  = 351.82 ± 29.

Ascorbic acid as DNase I inhibitor in prevention of male infertility.

Apoptotic and/or ROS-induced DNA fragmentation in sperm cells may contribute to the development of male infertility. As the known dietary antioxidant, ascorbic acid prevents ROS production and protects sperm cells from DNA damage. Here, we found that ascorbic acid has the ability to inhibit DNase I, one of the main endonucleases involved in DNA fragmentation during apoptosis.

Synthesis, Antimicrobial Activity and in silico Studies on Thymol Esters.

Derivatisation of parent structure in terpenoids often results in enhancement of biological activity of newly obtained compounds. Thymol, a naturally occurring phenol biosynthesized through the terpene pathway, is a well known biocide with strong antimicrobial attributes and diverse therapeutic activities. We have aimed our study on a single modification of phenolic functionality in thymol in order to obtain a small focused library of twenty thymyl esters, ten of which were new compounds.

An overview of recent dipeptidyl peptidase-IV inhibitors: linking their structure and physico-chemical properties with sar, pharmacokinetics and toxicity.

Dipeptidyl peptidase-IV (DPP-IV) (EC 3.4.14.

Deoxyribonuclease inhibitors.

Deoxyribonucleases (DNases) are a class of enzymes able to catalyze DNA hydrolysis. DNases play important roles in cell function, while DNase inhibitors control or modify their activities. This review focuses on DNase inhibitors.