Synthesis of novel phenacyl derivatives of alkyl piperidine as cytotoxic agents via simple and single step reaction procedure is going to be reported here. Twelve new compounds were successfully synthesized in moderate yield and in solid form. Their synthesis was confirmed by TLC, melting point, CHN analysis and through different spectral studies such as UV, IR, Mass and proton NMR. The advantages of this synthetic route are simple operation, mild reaction conditions and good yields. These newly synthesized derivatives were extensively explored for their cytotoxicity by brine shrimp lethality assay.
The present study concerns behavioral, biochemical and hematological effects of new synthesized adrenergic related compound 1-(3, 4-dihydroxyphenyl)-2-(4-methylpiperidin-1-yl) ethan-1-one, which have similar structural activity to adrenergic receptor agonist. With intraperitoneal injection in rats, stimulatory activity in home cage, anxiolytic effect in light and dark and locomotors activity in open field were significantly increased. Biochemical effects of glucose and cholesterol were checked by kit (CHOD-PAP) method were significantly decreased. Liver enzymes including, Alkaline Phosphatase (ALP) and SGOT were markedly decreased but, Alanine aminotransferase (ALT) level was markedly increased. In hematological study, after administration of compound hemoglobin (Hb) level was significantly increased in test group of rats. Results indicate that new adrenergic related antidepressant compound not only enhanced the stimulation, locomotion and released depression and anxiety but also, this antidepressant compound show more effectiveness in depression to prevent diabetes and heart diseases.
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
A variety of piperidines (2-12, 14-26) with variable substituents at N-atoms have been synthesized and evaluated as urease inhibitors. The synthesized compounds showed varying degree of urease inhibitory activity ranging from 31.97 to 254 microM. The size and electron-donating or -withdrawing effects of substituents influence the activity, which lead to the formation of urease inhibitors.
INTRODUCTION: Human 16w-density lipoprotein (LDL) and high-density lipoprotein (HDL) are . two of the major carriers of cholesterol in human blood. Plasma level of LDL has been suggested to have a direct correlation with the deposits of cholesterol in plaques on arterial walls and subsequent atherosclerosis.2’3 There appears to be a positive correlation between LDL and inverse relationship between HDL cholesterol and risk of developing coronary •artery disease.4’5 The cholesterol concentration of HDL represents approximately 25% of total serum cholesterol in normal ind ividuaLs and less than 20% in those with coronary artery disease.6’7.A wide variety of agents have been reported to be effective in hypercholesterolemic condition such as, Clofibrate, Nicotinic acid and its derivat ive etc. MATERIAL AND METHODS: All experiments are carried out on healthy rabbits weighing 1. 5-2.0 kg. Rabbits are classified into the following four groups, each group comprised of 4 rabbits: The details of the groups and their treatment with drugs has already been described elsewhere (Saify etal 1 O)• In brief for the determination of HDL cholesterol chemical kit (Cat No. 400971 and Cat No. 231347) and for LDL cholesterol chemical kit (Cat No. 124931) of Boehringer Mannheim was used. RESULT: Results are summarized in Table 1,2,3 and 4. Table 1 shows the level of serum HDL cholesterol (mg/100 ml) in all the 4 groups of rabbit before the treatment with dru, i.e., for 120 days.Nicotinic acid, derivative treated group (Grou pB) also shows a progressive decrease in serum HDL and LDL cholesterol level starting from the 5th day through .20th day though statistically not significant except on 15 and 20th days (<.01) DISCUSSIONS: The goal of serum lipid lowering in HLP is prevention of atherosclerosis eomplications. This effect is believed to operate through an influence on the serum lipoprotein levels of the developm ent of atheroma. The complications of the atherosclerosis may result, in acute myocardial infarction, angina pectoris, and sudden death. A more direct way of measuring the effect of the lipid lowering treatment would determine the concentration of lipoprotein, i.e., LDL & HDL before and after treatment1 1.In these studies it 1s suggested that low dose of aspirin (100 mg/day) may be of value in thrombotic condition ansi may act as anti1ipo proteinemic agent where the infrequent use of 300mg aspirin may be of no value.
The idea of this study is based on the marvelous fact of nojirimycin and deoxy nojirimycin, naturally occurring from piperidine class and having their role as alpha glucosidase inhibitors. In the present work some hydroxyl piperidine analogues have been synthesized and analysed for their hypoglycemic effect through glucosidase inhibition owing to the structural resemblance with nojirimycin. The activity was done by spectral absorbance analysis using acarbose as standard. Two analogues (I & IV) were found to pose excellent activity having 87.4 and 54.7% inhibition respectively, hence strengthening the idea of studying piperidine analogiues as glucosidase inhibitors due to structural similarity with nojirimycin.
Two series of variably N-substituted biperidines were synthesized by condensing various acid chlorides, alkyl halides and anhydrides with 1,4-bipiperidine. The new compounds were tested as tyrosinase inhibitors and a structure–activity relationship (SAR) study was carried out. Potent inhibition was observed in the case of the 4′-methylbenzyl substitution on this atom (IC50 = 1.72 μM) with this compound being a lead for future drug design. Additionally, calculations of the important QSAR molecular descriptors were done on the biperidine analogues after their 2 ps molecular dynamics (MD) simulations using molecular mechanics force field (MMFF) approaches. Using MD simulations potential and total energies were calculated for the energy minimized models of bipiperidine and the most active analogs 2, 3, 4, 6, 8 and 10.
Background: Diabetes is co-morbid with various metabolic and psychological disorders. Diabetes and depression are both chronic conditions with allied adverse and complicated outcomes.
Objectives: The current study was designed and planned accordingly to elucidate the associated frequency of depression with DM (Diabetes Mellitus) type 2 and prescribing practice of doctors depending on the distressing reality and threatening figures.
Methodology: A prototype prospective study was monitored in different public and private sector hospitals and clinics of outpatient settings in Karachi after taking approval from the Ethical Review Board of Hamdard University. In this context, seven hundred patients having diabetes were covered in the study and their data were analyzed through the Statistical software version 20. Beck Depression Inventory (BDI) was the preferred approach to evaluate the depression level.
Results: The outcome of the study established the fact of high prevalence for the co-morbidity of stress, anxiety and depression among patients with diabetes in Karachi, specifically among age bracket from forty to sixty years. Unfortunately, 80% (544) of diabetic patients in the study were suffering from depression and anxiety, while only 22.05% (120) patients were taking antidepressants and they were not counseled for the root cause of the disease. Severe depression (BDI score=38) was present in 100 subjects, moderate depression (BDI score=27) in 200 subjects, and mild depression was present in 175 of subjects. Being a patient of DM is itself a strong reason for contracting a depressive disorder. The result highlight improper treatment of depression in diabetic patients.
Conclusion: However, the current situation demands to follow proper treatment through effective and appropriate drugs to treat the disease from progressing. Moreover, efforts should be undertaken to strengthen the healthcare system where practitioners, either doctors, pharmacists or nurses are liable for patient care in both the physical and psychological domains.
In the context of our previous communication on phytochemical studies of the ethanolic extract of flowers of Alstonia scholaris of Pakistan origin, these have resulted in the isolation of two new triterpenoids. One is of the oleanane type, alstoprenyol, 3-β-hydroxy-28-β-acetoxy-5-olea triterpene (1), the other is of ursane type, alstoprenylene 3β-acetate-24-nor-urs-4,12,2′-triene ester triterpene (2) and together with four known triterpenes, α-amyrin acetate (3), α-amyrin (4), lupeol acetate (5) and 3β-hydroxy-24-nor-urs-4,12,28-triene triterpene (6) were isolated. The structures of 1–6 were elucidated with the aid of extensive NMR spectroscopic studies.
Terpenes in general and triterpenes in particular showed anti-inflammatory activity and act as immunomodulators in nutraceutical agents. Antiinflammation, a useful and attractive approach in experimental oncology, helps to investigate the inflammation preventive potential of natural products and synthetic entities. During the course of our research work in natural product chemistry and synthesis of novel structures in the field of heterocyclic chemistry, we found interesting results. In natural product betulinic acid, α-amyrin acetate, lupeol acetate, oleanolic acid, ursolic acid and their derivatives showed interesting potential analgesic and anti-inflammatory activity. In this review specific reference has been made to novel classes and newly discovered compounds in the literature, which exhibited required activities. Indomethacine is a potent synthetic compound, which becomes the basis of novel anti-inflammatory agents. Shen postulated a receptor theory which indicates the physical parameters responsible for anti-inflammatory activity. Attempt has been made to cover almost all the anti-inflammatory agents which fall under the various chemical structural classes of compounds showing required activity. The objective of this review is to compile relevant data on the mechanism of action of terpenes isolated from active ethnomedicinal plants to examine the role terpenoids have in medicinal plants used against inflammatory diseases, especially those in which an immune response is implicated. In addition, a selection of several structurally related compounds has been compiled in order to analyze the possible structural characteristics and relationships between the different types of structures found in triterpenoids. The selection of active species was made on the basis of their immunomodulatory activity, and their role in the resolution of diseases in which the immune system is implicated to examine the mechanism by which they are useful as ethnopharmacological medicines. These terpenes include ursolic acid, oleanolic acid, betulinic acid. This review discusses in detail the preclinical studies conducted with triterpenes and provides an insight into its mechanism of action.
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