Synthesis of new coumarin derivatives with suspected anticoagulant activity

Objectives: To synthesize three series of new coumarin derivatives and to screen their anticoagulant activity in rabbits in order to define in more exact terms the structural features that responsible for the anticoagulant activity of coumarins. Methods: the first series was synthesized by esterification the 7-hydroxycoumarin with benzoic acid, salicylic acid and 5-amino salicylic acid to give derivatives I-III; the second series was synthesized by the formation of amide linkage between 6-aminocoumarin and benzoic acid, salicylic acid and 5-amino salicylic acid to give derivatives IV-VI while the third series was synthesized by esterification the coumarin-6-carboxylic acid with phenol, resorcinol and m-chlorophenol to give derivatives VII-IX. The anticoagulant activity of these derivatives (I-IX) was investigated in rabbits via Quick's one-stage method; the initial effect of each derivative on the prothrombine time for five rabbits before and after oral administration was measured. Results: The chemical structure of these derivatives was characterized by physical and spectroscopic techniques as FTIR, UV and 13C-NMR spectra. Depending on prothrombin time measurements, derivatives II and VIII showed a significant anticoagulant activity through increasing the prothrombine time while the other derivatives showed an insignificant anticoagulant activity. Conclusion: This study proposed that the coumarin derivatives contained an ester linkage at position 6 or 7 separated from a hydroxyl group by short carbon side chain may show anticoagulant activity

Synthesis and in vitro kinetic study of novel mutual azo prodrug for inflammatory bowel disease

Background: Inflammatory bowel disease (IBD) refers to idiopathic inflammatory diseases of the intestine, principally ulcerative colitis and Crohn’s disease. IBD is characterized by chronic inflammation in the mucosal membrane of large intestine. 5- ASA is the gold standard for the treatment of IBD and when searched for a better 5- ASA prodrug, a novel mutual azo prodrug was designed and synthesized. Methods: A mutual prodrug was synthesized by coupling p-phenetidine with salicylic acid. The stability of this prodrug in HCl buffer, in phosphate buffer and in rat fecal matter were monitored. Results: The chemical structure of mutual prodrug was characterized by physical and spectroscopic techniques using FTIR, UV/Visible, 1H-NMR and 13C-NMR spectra. In vitro kinetic studies in HCl buffer (pH 1.2) showed negligible release of 5-ASA and p-phenetidine, whereas in phosphate buffer (pH 7.4) only (22.04 %) release was observed over a period of (6 hr.). In rat fecal matter, the hydrolysis of mutual prodrug was almost complete (77.96 %), with a half-life of 182.67 min, following zero order kinetics. Conclusion: The mutual prodrug was split in colon by the action of bacterial azoreductase into 5-ASA and p-phenetidine that constitute two anti-inflammatory compounds with different mechanisms of action. Therefore, this mutual prodrug is a promising colon specific prodrug for IBD and worthy of further study

Synthesis and kinetic studies of mutual azo prodrugs of 5-aminosalicylic acid with sulfamethoxazole and trimethoprim as models for colon targeting

In this study, two mutual azo prodrugs were synthesized for colon targeting in a treatment of colonic diverticular disease. The first was synthesized by coupling sulfamethoxazole with salicylic acid; the second was synthesized by coupling one mole of trimethoprim with two moles of salicylic acid. In vitro kinetic studies of these mutual prodrugs in hydrochloric acid buffer (pH 1.2) and in phosphate buffer (pH 7.4) were monitored. Hydrolysis of these mutual prodrugs was established in rat fecal matter. The release of 5-aminosalicylic acid and sulfamethoxazole or trimethoprim from these mutual prodrugs was almost complete and it followed first order kinetics. The prodrug approach to drug physico-chemical properties modification based on enzyme specifications may offer a new approach for improving drug product efficacy and reducing most of its adverse effects

Electrochemical detection of sulfite in food samples

In various pharmaceutical and food industries, sulfite is utilized for the inhibition of nonenzymatic and enzymatic browning. Also, in brewing industries, it acts as an antioxidizing and antibacterial agent. Several toxic and adverse reactions, including vitamin deficiency, hypersensitivity, and allergic diseases, have been attributed to sulfite ingestion that may cause dysbiotic oral and gut microbiota events. Thus, the content of sulfite in foods must be controlled and monitored, and it is essential to find a specific, reproducible, and sensitive method to detect sulfite. Some analytical solutions are being tested to quantify sulfite. However, due to their advantage over traditional techniques, electroanalytical techniques are attracting much attention because they are simple, fast, affordable, and sensitive to implement. In addition, by the electrode modification, the morphology and size can be controlled, resulting in the miniaturization to be used in portable electrochemical devices. Therefore, the present review addressed some articles on the electrooxidation of sulfite from real samples using various electrochemical sensors

Synthesis of new metoclopramide derivatives and in vitro evaluation of their human cholinesterases protection against Chlorpyrifos

Objective: The purpose of this study was to synthesize three new derivatives of metoclopramide by diazotization and replacement reactions and then to quantify in vitro their protection effects on blood cholinesterases using chlorpyrifos as a potent inhibitor. methods: The three new metoclopramide derivatives were synthesized via Sandmeyer reaction, the chemical structures of these derivatives were identified by physico-chemical and spectroscopic (U.V. and FTIR) techniques. Results and conclusion: The results of in vitro evaluation of their human cholinesterases inhibition and protection against chlorpyrifos indicated that the (OH) functional group binds to cholinesterase (ChE) at the same organophosphorous (OP) binding site and shows some competition and protection ability but not to a significant degree, while the (Cl and I) functional groups bind to the ChE at site differs from OP binding site, as well as the (I) functional group has more selectivity for enzyme moiety and binds more strongly than the (Cl) group, so that shows more ChE inhibiting abilit

An overview of the uses of propolis for oral health

Propolis is a gummy agent exploited from bees, which has anti-inflammatory, antibacterial, anti-allergic, wound healing, antidiabetic, and antiviral effects against various injuries and diseases. It also produces antifungal, antitumor and local anesthetic effects. The aim of the review was to review research findings on the role of propolis in oral health. This study was conducted by reviewing published articles on the use of propolis in oral health. To this end, Persian electronic databases such as Google, SID and Magiran as well as English databases such as PubMed and WOS were searched for articles published from 1979 onwards, 140 papers were retrieved, 21 articles were excluded, and 119 articles were included in final review. So far, propolis has been studied for the treatment of surgical wounds, intracanal irrigation, inhibition of the decay process, treatment of periodontitis and dentin hypersensitivity, and potential antifungal and antibacterial activities in the canal with a mostly satisfactory efficacy. Propolis has been reported to improve surgical wounds and produce anti-decay, anti-dentin hypersensitivity and anti-aphthous ulcer properties, and to be useful as a tooth-storing medium after tooth extraction, an intracanal irrigant and a mouthwash. substances highly useful properties of propolis, it can be argued that in the future, the substance will play a substantial role in dental science are necessary to isolate its compounds and identify their beneficial effects

Phosphate ion removal from synthetic and real wastewater using MnFe2O4 nanoparticles: a reusable adsorbent

The purpose of this study was to eliminate phosphate (P) from wastewater using MnFe2O4 nanoparticles. BET, TGA/DTG, FTIR, SEM, TEM, VSM, XRD and EDX/Map analyses were used to determine the MnFe2O4 surface properties. The specific surface area of the adsorbent was 196.56 m2/g and VSM analysis showed that the adsorbent has a ferromagnetic property. The maximum P sorption efficiency using MnFe2O4 (98.52%) was achieved at pH 6, temperature of 55 °C, P concentration of 10 mg/L, time of 60 min, and sorbent dosage of 2.5 g/L, which is a significant value. Also, the thermodynamic study indicated that the P sorption process is spontaneous and endothermic. Moreover, the utmost sorption capacity of P using MnFe2O4 was 39.48 mg/g. Besides, MnFe2O4 can be used for up to 6 reuse cycles with high sorption efficiency (>91%). Also, MnFe2O4 was able to remove phosphate, COD, and BOD5 from municipal wastewater with considerable removal efficiencies of 82.7%, 75.8%, and 77.3%, respectively.Campus Lima Centr

Synthesis of efficient cobalt–metal organic framework as reusable nanocatalyst in the synthesis of new 1,4-dihydropyridine derivatives with antioxidant activity

Efficient cobalt–metal organic framework (Co-MOF) was prepared via a controllable microwave-assisted reverse micelle synthesis route. The products were characterized by SEM image, N2 adsorption/desorption isotherm, FTIR spectrum, and TG analysis. Results showed that the products have small particle size distribution, homogenous morphology, significant surface area, and high thermal stability. The physicochemical properties of the final products were remarkable compared with other MOF samples. The newly synthesized nanostructures were used as recyclable catalysts in the synthesis of 1,4-dihydropyridine derivatives. After the confirmation of related structures, the antioxidant activity of derivatives based on the DPPH method was evaluated and the relationship between structures and antioxidant activity was observed. In addition to recyclability, the catalytic activity of Co-MOF studied in this research has remarkable effects on the synthesis of 1,4 dihydropyridine derivatives

Synthesis of Bioactive Yttrium-Metal–Organic Framework as Efficient Nanocatalyst in Synthesis of Novel Pyrazolopyranopyrimidine Derivatives and Evaluation of Anticancer Activity

Novel Yttrium-metal–organic framework (Y-MOF) was synthesized under optimal conditions of microwave with a power of 20 W, the temperature of 30 degrees of centigrade, and time duration of 10 min. The products were characterized by SEM (morphology and size distribution), TGA (thermal stability), BET technique (surface area), and FTIR (characterization of the related group). The Yttrium-metal–organic framework (Y-MOF) synthesized in this study, after identifying and confirming the structure, was used as an efficient and recyclable catalyst in the synthesis of new pyrazolopyranopyrimidine derivatives. Following the study of the properties and applications of Y-MOF, its anticancer properties on breast cancer cells based on the MTT method were evaluated, and significant results were observed. In addition, the anticancer properties of the pyrazolopyranopyrimidine derivatives were investigated

An investigation of the effect of smoking, alcohol, and drug use on male infertility

Background: Infertility in men has increased in recent years. Numerous physical, chemical, biological, and social factors are known to play a role in reducing semen quality, in between, there are high-risk behaviors that affect the quality of semen. In this paper, the effects of three factors: smoking, alcohol consumption, and drugs have been investigated. Methods: This case-control study was performed from June to September 2021 on 500 people, 250 people with normal semen quality and 250 people with defective semen quality. The data collection tool was a questionnaire made by researchers and semen test results. Finally, the collected data were analyzed by descriptive method with SPSS software. For quantitative variables, mean and standard deviation (SD) were used, while frequency and percentage reports were used for qualitative variables. Results: Drug use had a significant relationship with the shape and motility of sperm (B = -0.675, P = 0.005). The chance of natural semen decreases by 0.506 times with an increase of one drug use unit; moreover, the older the age of onset of drug use, the more the semen disorders (B = 0.514, P = 0.002).. Conclusion: Smoking and alcohol consumption were not identified as factors affecting semen quality, but there was a significant relationship between drug use and age of onset and semen disorders