Search

Purines are nitrogenous heterocyclic compounds characterized by the presence of two fused rings: pyrimidine and imidazole. Their significance is underscored by their widespread occurrence in natural products as the metabolic processes of all living organisms heavily rely on purines and their synthetic derivatives. Furthermore, purines exhibit considerable bioactivity, highlighting their importance in biological systems. Given their unique structural characteristics and ability to yield a diverse array of bioactive molecules, purines have attracted substantial attention from researchers. This review illustrates the recent methods for the synthesis of purines from diaminomaleonitrile, urea derivatives, imidazole, and pyrimidine derivatives reported from 2019 to 2024. Additionally, it elucidates the various chemical modifications applied to the purine nucleus, including benzoylation, alkylation, halogenation, amination, selenylation, thiolation, condensation, diazotization, coupling reactions, and other miscellaneous reactions. Moreover, this review discusses several biological evaluations, including the mechanisms of action of purine derivatives as anticancer, antimicrobial, anti-inflammatory, antiviral, antioxidant, and anti-Alzheimer agents. This review aims to assist researchers in synthetic organic and medicinal chemistry toward the development and enhancement of novel methodologies for the synthesis of new purine molecules while supporting biologists in the identification of new targets for bio-evaluation., Competing Interests: The author declares no conflicts of interest., (This journal is © The Royal Society of Chemistry.)

Background: To the best of our knowledge, there is a gap in the review of literature about the most suitable varicocelectomy technique in isolating and ligating adherent periarterial vein(s). Consequently, leaving the artery intact or ligating it together with the adherent vein may pose a challenge. We conducted a comparative prospective study to assess the outcomes of the three techniques namely Fisch, sclerotherapy and microvaricoclectomy (MSV)., Results: The patients who underwent MSV showed the longest operative time (66.29 ± 2.78 min), followed by Fisch technique (56.94 ± 3.07 min) then sclerotherapy (55.45 ± 1.99). Thus, the difference in the operative time between the three techniques was statistically significant (P < 0.001). Regarding the postoperative right vein diameter, MSV group showed the largest diameter (2.14 ± 0.15 mm), followed by Fisch technique (2.13 ± 0.15 mm) then sclerotherapy (1.75 ± 0.42 mm). Regarding the postoperative left vein diameter, MSV group showed again the largest diameter (2.17 ± 0.21 mm), followed by Fisch technique (2.14 ± 0.15 mm) then sclerotherapy (1.75 ± 0.42 mm). Moreover, the patients who underwent sclerotherapy showed the highest postoperative progressive sperm motility percent (25.27 ± 4.00%), followed by Fisch technique (21.56 ± 7.30%) then MSV group (19.85 ± 6.33%). Post hoc pair wise comparisons revealed that sclerotherapy and Fisch technique had a significantly higher effectiveness in reducing operative time than MSV. Additionally, it revealed that sclerotherapy technique had a significantly higher effectiveness in reducing postoperative vein diameters measurement than MSV and Fisch technique. Post hoc pair wise comparisons revealed that sclerotherapy technique had a significantly higher effectiveness in improving the postoperative progressive sperm motility percent than MSV. Patients who underwent the 3 techniques demonstrated statistically significant differences between baseline and post-operative vein diameter, reflux duration, sperm concentration, progressive sperm motility, progressive motile count/ejaculate and sperm abnormal forms., Conclusion: The 3 techniques showed significant improvement in the semen parameters after 3 months in the studied patients. However, sclerotherapy technique showed a significantly higher effectiveness in improving the postoperative progressive sperm motility percent compared to MSV., Competing Interests: Declarations. Ethics approval and consent to participate: All procedures performed were in accordance with the ethical standards of the institutional and national research committee and with the 1964 Helsinki Declaration and its later amendments or comparable ethical standards. The study was approved by the local ethical committee. Consent for publication: All authors agree to sign any required consent for publication. Competing interests: The authors declare no competing interests., (© 2025. The Author(s).)

Herein, novel thiazolo[4,5- b ]quinoxalin-2-ones 2-6 and thiazolo[4,5- b ]quinoxalin-2(3 H )-imines 7-9 were synthesized and characterized using elemental analysis, IR spectroscopy, and 1 H/ 13 C NMR to confirm their structures. The efficacy of the newly designed thiazolo-quinoxalines 2, 3, 4, 5, 7, 8, and 9 against the cotton leafworm S. litura (2nd and 4th instar larvae) was evaluated, and results revealed insecticidal activity with variable and good mortality percentages. A SAR study was also discussed. Additionally, compound 3 exhibited the highest insecticidal activity, with mortality% values ranging from 86% ± 7.21% to 97% ± 1.52% and from 66.00% ± 6.24% to 86.33% ± 6.90% at concentrations of 625-2500 mg L -1 against the 2nd and 4th instar larvae, respectively. The probit analysis revealed that the thiazolo[4,5- b ]quinoxalin-2(3 H )-one derivative 3, after 5 days of treatment, exhibited LC 50 values of 141.02 and 366.73 mg L -1 for the 2nd and 4th instar larvae, respectively. The LT 50 values ranged from 0.52 to 1.92 days for the 2nd larval instar and from 1.95 to 2.47 days for the 4th larval instar. The corresponding toxicity index (TI) values were 86.21% for the 2nd instar and 78.47% for the 4th instar larvae. The mode of action of compound 3 was assessed through physiological, histological, and SEM analyses on the 4th larval instar. The physiological bioassay revealed a significant increase in total carbohydrate and protein levels compared to the control group. However, the enzymatic study showed a significant decrease ( P < 0.05) in the levels of aspartate aminotransferase (AST/GOT), alanine aminotransferase (ALT/GPT), and alkaline phosphatase (AlP), while acetylcholinesterase (AChE) levels significantly increased. SEM analysis revealed malformations in the external body, while histological examination demonstrated severe damage to the gut epithelium and regenerative cells in the midgut tissues., Competing Interests: The authors declare no conflicts of interest., (This journal is © The Royal Society of Chemistry.)

Hepatocellular carcinoma (HCC) ranks as the third most prevalent reason for cancer-related death on a global scale. Tyrosine kinase inhibitors (TKIs) continue to be the primary treatment option for advanced hepatocellular carcinoma. A series of fluoro-11H-indeno[1,2-b]quinoxaline derivatives as an HCC drug targeting the VEGFR2/AKT axis was designed and synthesized. The novel compounds were investigated against HepG-2 and HuH-7 liver tumor cell lines. Compound 5 was the most active derivative against HepG-2 and HuH-7 cell lines with IC 50  = 0.75 ± 0.04 and 3.43 ± 0.16 μM, respectively, in contrast to Sorafenib which shows IC 50 values of 5.23 ± 0.31 and 4.58 ± 0.21 μM, respectively. IC 50 values on normal liver cells (THLE-2) show that all tests are more selective than Sorafenib, prompting further research. The most promising cytotoxic compound has virtually equal VEGFR2 inhibition efficacy to Sorafenib. The total VEGFR2 and p-VEGFR2 inhibitory effects were subsequently evaluated, showing 38.32 % and 77.64 % attenuation, respectively. Compound 5 also reduced total and phosphorylated AKT concentrations in HepG-2 cells by 55.29 % and 78.01 %, respectively. Furthermore, Compound 5 upregulated BAX and caspase-3 and downregulated Bcl-2 to promote apoptosis. Hybrid 5 stops HepG-2's cell cycle at the S phase 48.02 % higher than untreated. Docking experiments assessed AKT and VEGFR2 binding patterns., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Inc. All rights reserved.)

Background: Infraorbital ethmoidal air cells (IOEAc) are ethmoidal cells that pneumatizes inferior to the orbital floor and lateral to a line parallel to the lamina papyracea. Studies have shown considerable anatomical variation with different extensions in humans. Objectives: To identify and categorize the anatomical variations of the IOEAc creating a new, comprehensive variation classification system. Patients and methods: All included 1260 computed tomography of the nose and paranasal sinuses were reviewed to detect the presence or absence of IOEAc. All cases with IOEAc were evaluated for bilaterality, multiplicity, and shape and categorized according to its extensions to the maxillary infundibulum and its relations to the entire length of the inferior orbital wall. Results: IOEAc were identified in 173 (13.7%) scans. Bilaterality was observed in 99 patients (57.2%), while 50 patients (28.9%) had unilateral air cells on the right and 24 patients (13.9%) had unilateral air cells on the left. They were classified into 5 categories that were subclassified into subtypes. With 173 cases distributed as 26%, 17.9%, 3.5%, 9.8%, 24.9%, 10.4%, 2.3%, 1.7%, and 3.5% among the 5 categories, respectively. Conclusions: The new classification system provides a comprehensive classification of the described anatomical variations of the IOEAc. It allows the description and categorization of variants identified in past and future studies. It is applicable to current clinical practice., Competing Interests: Declaration of Conflicting InterestsThe author(s) declared no potential conflicts of interest with respect to the research, authorship, and/or publication of this article.