Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives

Alzheimer’s disease (AD) is the most common form of dementia among the elderly people. Based on the cholinergic hypothesis, loss of cholinergic neurons in AD patients’ brain leads to the decline of acetylcholine (ACh) neurotransmitter level and eventually causes severe dysfunctions in the cholinergic neurotransmission. Thus, increasing the ACh levels is a promising therapeutic approach to restore the substantial impairment of memory and cognitive dysfunctions in AD patients. The search for new cholinesterase inhibitors is still ongoing worldwide. Inspired by the biological significance of pyrimidine-grafted derivatives, especially in cholinesterase inhibition, seventy-four novel pyrimidine embedded derivatives, namely pyridopyrimidines 6(a-l), pyridopyrimidothiones 7(a-l), N-ethyl-pyridopyrimidothiones 8(a-j), N-ethylmorpholino pyridopyrimidothiones 9(a-j), pyrimidinethiols 11(a-l) and thiazolopyrimidines 13(a-r) were synthesized and evaluated for their cholinesterases inhibitory potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)

Cholinesterase Enzymes Inhibitors from the Leaves of Rauvolfia Reflexa and Their Molecular Docking Study

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The comparison between the attitudes of employees and clients towards organizational intelligence (case study: Isfahan General Directorate of Sports and Youth)

This study was conducted in 2013, aiming tocompare the attitudes of employees and clientstowards organizational intelligence of IsfahanGeneral Directorate of Sport and Youth. The current studyis applied in terms of goal, descriptive in terms of natureand survey in terms of data collection. Based on Krejcie &Morgan table for sample size determination from a givenpopulation, 123 samples of employees were selected.Due to the comparison between the attitudes of employeesand clients, 123 clients were also selected throughsimple random method. The measurement tool in thisresearch was standard questionnaire of organizationalmultiple intelligence (Aghahosseini, 2010). To determinethe validity of it, the experts and professors of physicaleducation and sport sciences as well as management andplanning were consulted. Hereby, the content validity ofquestionnaire was confirmed. The reliability of it was alsocalculated through Cronbach’s alpha coefficient as 0.87.The descriptive and inferential statistical methods wereutilized for data analysis using SPSS software in error levelof 0.05. The results of study indicated no significant differencebetween the attitudes of employees and clientstowards organizational intelligence of Isfahan General Directorateof Sport and Youth (P=0.651). According to theemployees, the components of systematic intelligence,emotional intelligence, cooperative intelligence and educationalintelligence were upper than average level exceptoperational intelligence which was less than mean level(P=4.473). According to clients, all components in IsfahanGeneral Directorate of Sport and Youth were upperthan average level but there was no significant differencebetween the attitudes of employees and clients in any ofcomponents of organizational intelligence (P=0.05)

Laparoscopic adrenalectomy: 10-year experience, 67 procedures

Introduction: The purpose of this study was to evaluate the short-term and long-term results of laparoscopic adrenalectomies carried out in our center. Materials and Methods: A total of 67 laparoscopic adrenalectomies were performed during the 10 years between 1995 and 2005 at Shahid Labbafinejad Medical Center. A transperitoneal lateral approach was used in 65 (97.0%) of the patients, and retroperitoneal approach was used in 2 (3.0%). The clinical characteristics and the outcomes were reviewed in a retrospective study. Results: Indications for laparoscopic adrenalectomy in our patients were as follows: pheochromocytoma in 28 patients (41.8%), aldosteroneproducing adenoma in 15 (22.4%), pseudocyst in 6 (9.0%), Cushing syndrome (macronodular adrenocortical hyperplasia) in 5 (7.5%), nonfunctioning adenoma (incidentaloma) in 5 (7.5%), myelolipoma in 2 (3.0%), almost normal adrenal tissue in 2 (3.0%), adrenal cyst in 2 (3.0%), adenocarcinoma in 1 (1.4%), and schwannoma in 1 (1.4%). The mean operative time for unilateral cases was 149.0 ± 36.1 minutes. The mean intraoperative blood loss was 126 ± 36 mL. Conversion rate to open surgery was 7.5%. Reoperation due to hemorrhage was performed in 1 patient. Conclusion: Laparoscopic adrenalectomy is a safe procedure in some adrenal tumors and a reasonable option for selected large adrenal tumors when complete resection is technically feasible and there is no evidence of local invasion

(3E,5E)-1-Acryloyl-3,5-bis­(2,4-dichloro­benzyl­idene)piperidin-4-one hemihydrate

The asymmetric unit of the title compound, C22H15Cl4NO2·0.5H2O, consists of a (3E,5E)-1-acryloyl-3,5-bis­(2,4-dichloro­benzyl­idene)piperidin-4-one mol­ecule and a half-mol­ecule of water (the O atom of the water mol­ecule lies on a twofold axis). The piperidin-4-one ring adopts an envelope conformation. The dihedral angle between the two terminal benzene rings is 8.84 (11)°. In the crystal, mol­ecules are connected by C—H⋯O hydrogen bonds forming supra­molecular chains along the c axis. Furthermore, adjacent chains are inter­connected by the water mol­ecules via O—H⋯O hydrogen bonds

Neurologic complications in percutaneous nephrolithotomy

Percutaneous nephrolithotomy (PCNL) has been the preferred procedure for the removal of large renal stones in Iran since 1990. Recently, we encountered a series of devastating neurologic complications during PCNL, including paraplegia and hemiplegia. There are several reports of neurologic complications following PCNL owing to paradoxical air emboli, but there are no reports of paraplegia following PCNL. Materials and Methods: We retrospectively reviewed the medical records of patients who had undergone PCNL in 13 different endourologic centers and retrieved data related to neurologic complications after PCNL, including coma, paraplegia, hemiplegia, and quadriplegia. Results: The total number of PCNL procedures in these 13 centers was 30,666. Among these procedures, 11 cases were complicated by neurologic events, and four of these cases experienced paraplegia. All events happened with the patient in the prone position with the use of general anesthesia and in the presence of air injection. There were no reports of neurologic complications in PCNL procedures performed with the patient under general anesthesia and in the prone position and with contrast injection. Conclusions: It can be assumed that using room air to opacify the collecting system played a major role in the occurrence of these complications. Likewise, the prone position and general anesthesia may predispose to these events in the presence of air injectio

Targeted Therpeutics for Prostate Cancer, Behind the Scenes of PSMA & Cysteine Protease Trapping Mechanism

In an attempt to increase the residence time of PSMA-targeted theranostics inside the prostate cancer cells and tumors, we designed and prepared a CPTA-PSMATA resembling PSMA-617 by adding a well-known cysteine protease inhibitor (E-64) to the conjugate. Lysosomal proteases, including cysteine, serine, and aspartic families of hydrolytic enzymes, are expressed in high concentrations in the lysosomes and are responsible for the catabolism of proteins inside the cell [165, 278]. We proposed that after successful internalization of the PSMA-targeted conjugates into the cells, they will be conveyed to the endolysosomes. In these endolysosomal compartments, the E-64 moiety will covalently bind to cysteine proteases such as cysteine cathepsins, thereby forming high molecular weight conjugates