A series of nitrile derivatives of Petromurin C were synthesized and assessed for their cytotoxic effects on tumor cell lines and inhibitory activity against Mycobacterium tuberculosis (M.tb H37Ra).Bromoalkyl nitriles (Br(CH2)nCN; n=1-5) and (o-, m-, p-) bromomethyl benzonitriles were used as alkylating reagents.The majority of the syntheses consisted of O-alkylated derivatives in which the two NH group were not alkylated, as expected from the treatment of petromurin C with K2CO3 in DMF followed by treatment with alkylating reagents.Similarly, treatment of Petromurin C with NaH in DMF and the treatment with alkylating reagents yielded both OR and bis-NR alkylated structures.In the first method, 7 different O-alkyl Petromurin C derivatives were obtained.The second method yielded 7 different Petromurin-C derivatives containing both Oalkyl and bis-N-alkyl groups.Notably, compounds 1-4 and 7-10 demonstrated selective inhibitory activity against the acute myeloid leukemia cell line MV4-11, with IC50 values ranging from 12.96 to 20.00 M.Compound 15 exhibited a minimum inhibitory concentration (MIC) of 6.25 M against M.tb H37Ra.Importantly, all synthesized compounds showed negligible inhibition (below 50%) against human normal cell lines L-02 and 293T at a concentration of 100 M.These findings suggest that the compounds possess high efficacy and low toxicity, indicating their potential as novel therapeutic agents for the treatment of leukemia and tuberculosis.

A more efficient and environmentally friendly approach has been developed for synthesizing aminophosphonates through the Kabachnik-Fields (K-F), catalyzed by nano-ZnO in a solvent-free environment, utilizing microwave irradiation.Before synthesis, each compound underwent in silico ADMET analysis and molecular docking to assess drug-like characteristics and their potential to inhibit -amylase.The structure of the newly synthesized compounds was validated using spectroscopic analysis, and their in vitro inhibitory effects on -amylase and -glucosidase were assessed.Among the compounds 8g (IC50, 99.20.5 g/mL), 8i (IC50, 101.20.3 g/mL), 8e (IC50, 102.10.4 g/mL) and 8j (IC50, 103.40.4 g/mL) containing anthracen-9-ylamino, phenanthren-9-ylamino, 2-oxo-2H-chromen-6-yl)amino and 2benzoylphenyl)amino moieties respectively, exhibited the highest inhibitory activity on -amylase, superior to the reference compound acarbose (IC50, 104.50.1 g/mL).The remaining compounds demonstrated moderate to good enzyme inhibition.8c bearing with 4-fluorophenyl substituent (IC50, 88.40.7 g/mL), 8e (IC50, 90.00.4g/mL) bearing with 2-oxo-2H-chromen-6-yl substituent and 8d (IC50, 91.10.9 g/mL) bearing with 2-methylbenzo[d]oxazol-5-yl moiety have shown the highest inhibitory activity on -glucosidase than the reference drug, Acarbose ((IC50, 93.10.8 g/mL).The remaining compounds exhibited moderate to good inhibition on the enzyme with IC50 ranging 94.50.9 to 141.40.7 g/mL.

This concise review provides an overview of some synthetic methods utilized for the preparation of 4(3H)quinazolinone and benzotriazepine derivatives, and explores their diverse biological activities.The review highlights the significance of these compounds in medicinal chemistry and discusses selected synthetic approaches employed in their synthesis.Additionally, it examines the range of biological activities exhibited by these derivatives and briefly discusses their potential applications.This succinct review serves as a valuable resource for researchers interested in the synthesis and biological evaluation of 4(3H)-quinazolinone and benzotriazepine derivatives.

It is known that compounds containing sulfur in their structure have a wide range of biological activities, such as antibacterial, antiallergic, antimicrobial, anticancer, and anticonvulsant.In addition, nitrogen-containing heterocyclic compounds are also found in nature and the structure of drugs.Various compounds, such as piperidine and its derivatives, are also widely used in the synthesis of many drugs.Various Schiff bases have been synthesized in drug development studies, and they have been used in clinical applications as drugs and drug candidates.In this context, the synthesis of new thiophene-based Schiff bases containing piperidine rings is aimed.Green chemistry objectives were adhered to in the syntheses.Thiophene-2-carbaldehyde and piperidine derivatives were used as starting compounds, and new compounds containing thiophene-based piperidine were synthesized without adding any catalyst or solvent to the reaction medium.The desired Schiff base compounds were successfully synthesized in high yield and in a short time.

In this study, a synthetic route to access unsymmetrical ditetrazoles was developed.By using this method, the first examples of unsymmetrical thioditetrazole compounds were synthesized.In vitro, antibacterial efficacy studies were carried out for all the thioditetrazoles and their precursor thiotetrazoles against ten bacteria.The synthesized compounds showed a strong antibacterial effect against pathogenic Gram-negative bacteria, especially Escherichia coli, Salmonella typhi and Pseudomonas aeruginosa (up to 23 mm).

In the present study, new oxalamide-based compounds were designed from thalidomide and synthesized easily and with high yields (from 69% up to 93%) by a two-step method.The antiproliferative effects of synthesized 6a-d and 7a-d compounds on (ER+) MCF-7 and (ER-) MDA-MB-231 breast cancer cell line and human fibroblast WI-38 healthy cell line were investigated by the MTT method.The results showed that compound 7d was the most potent candidate against both MCF-7 and MDA-MB-231 cell lines with IC50 = 4.72 µM and 6.37 µM, respectively.To investigate whether antiproliferative effect of the compounds on breast cancer cell lines is dependent on COXs, expressions of COX-1/2 on the MCF-7 cell line were investigated by the Western-Blot technique.Among synthesized compounds, compound 7d increased the expression of both COX-1 and COX-2.The inhibition potential of compounds on COX-1/2 enzymes was investigated by molecular docking compared to inhibitor co-ligand celecoxib in crystal structures of COX-1 (PDB ID: 3KK6) and COX-2 (PDB ID: 3LN1).Docking results indeed showed that compound 7d had a higher binding affinity for both COX-1 and COX-2 active sites.Consequently, the novel oxalamide-based compounds presented here may be important candidate molecules for the development of new COX-dependent antiproliferative agents.

Enantioselective reduction of a new 1-oxotetrahydrocarbazole compound (ethyl 2-(1-oxo-9-tosyl-2,3,4,9tetrahydro-1H-carbazol-2-yl)acetate) through asymmetric transfer hydrogenation by using the commercially available Noyori-Ikariya ruthenium catalyst and HCO2H/Et3N or HCO2H/DABCO as the hydrogen source have been investigated.High enantiomeric excesses (up to 96% ee) and moderate to good yields (24-72%) for corresponding alcohol and lactone compounds have been achieved.Structures of all compounds have been characterized by spectroscopic techniques.

Inhibition of soluble epoxide hydrolase (sEH) is implicated as a new therapeutic approach against inflammatory disorders in the context of metabolic and cardiovascular diseases.In the course of our ongoing research on sEH inhibitors, we synthesized novel piperidine/piperazine amide derivatives of the chromone-2-carboxylic acid, and evaluated their inhibitory properties against human sEH.The chemical structures of the target compounds (2-5, 7-9) were elucidated by means of 1 H-NMR, 13 C-NMR and HRMS spectra.Initial screening of final compounds against sEH at a final concentration of 10 M led to the identification of compound 7, which inhibited sEH activity in a concentration-dependent manner with an IC50 = 1.75 M.Therefore, this chromone-2-amide derivative 7 decorated with benzyl piperidine on the amide side can be regarded as a novel lead structure, which pave the way of developing new analogues with improved inhibitory activities against sEH.

In this research, five novel hydrazone derivatives (2a-e) were obtained for the first time, characterized and investigated for their antioxidant properties, and acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. The target molecules were easily synthesized by the condensation reaction of 2,4dinitrophenylhydrazine (2,4-DNPH) with aryl esters (1a-e) derived from salicylaldehyde as a starting material. These molecules were fully elucidated by some spectroscopic techniques and elemental analysis. Antioxidant activities of newly synthesized molecules were examined by CUPRAC reducing, ABTS and DPPH radical scavenging assays. The IC50 values of the screened molecules were determined in the range of 72.54-221.52 M against AChE and in the range of 8.46-48.28 M against BChE. Among the tested molecules, compound 2e indicated the highest activity against both AChE and BChE. Also, the inhibitory capacities of all tested molecules were compared to the standard molecules galanthamine. On the other hand, In CUPRAC reducing assay, the target molecules exhibited antioxidant activities in the range of 30.29 and 59.43 M. Among these compounds, compound 2b (IC50=30.29 M) showed the closest activity to the standard compounds butylated hydroxytoluene (BHT) (IC50=30.62 M) and butylated hydroxyanisole (BHA) (IC50=34.24 M).