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Synthesis of steroidal thiadiazoles from steroidal ketones.

Syntheses of steroidal heterocycles containing a five-membered N,S- heterocycle attached at the 6,7 positions of the B ring are reported. 5Alpha-cholestane-6-one (1), its 3beta-acetoxy- (2) and 3beta-chloro- (3) analogues reacted with semicarbazide and aqueous sodium acetate in refluxing ethanol to yield 5alpha-cholestan-6-one-semicarbazone 1a and its 3-beta-acetoxy and 3beta-chloro derivatives 2a and 3a, respectively. The reactions of 1a, 2a and 3a with thionyl chloride in dichloromethane at low temperature afforded the cyclized thiadiazole 4 and its 3beta-acetoxy- and 3beta-chloro analogues

Steroids and related products. LIII. The synthesis of 11-oxa steroids. V. The synthesis of 17-ethynyl-11-oxatestosterone.

The synthesis of 17-ethynyl-11-oxatestosterone, both from 11-oxa-5 alpha-pregnane-3,20-dione and, via a 3,17-dioxygenated 9-oxo 9,12-seco 11-nor 5 alpha-androstane-12-oic ester, from 3 beta-acetoxy-17-hydroxy-5 alpha-pregnan-12-one--two products available from hecogenin--is reported. The new hormone analogue shows significant progestational activity in the Clauberg test and relatively weak activity in a post-coital antifertility assay.

Steroids in organ transplantation: Immunosuppression and tolerance.

Organ transplantation has evolved significantly since the first successful kidney transplant in the 1950s, but corticosteroids remain a mainstay of immunosuppressive therapy. This review addresses the emerging and expanding role of corticosteroids as adjunct therapeutic agents in transplantation with particular emphasis on their immunosuppressive and tolerance inducing properties. The progression of current immunosuppressive strategies, including the combined use of steroids, calcineurin inhibitors, and mTOR inhibitors have also been discussed. The review highlights the mechanisms underlying g…

Thrombotic complications of glucocorticoids and anabolic steroids.

Glucocorticoids and anabolic-androgenic steroids are used for medical and nonmedical purposes. There are thrombotic risks associated with both classes of steroids. Glucocorticoid therapy has been shown to increase the relative risk of venous thromboembolism. Glucocorticoids are also associated with arterial events. The mechanisms involve the exacerbation of cardiovascular risk factors and its effects on coagulation, platelet function, and endothelial integrity. Anabolic-androgenic steroids use similarly predisposes users to both venous thromboembolism and arterial thromboses. It is driven by a…

When and How Much? Steroids in Sepsis.

Patients with septic shock may have lack of endogenous steroid synthesis or insufficient corticosteroid activity. This forms the basis for exogenous steroid administration to patients with septic shock, though the timing, dose, and duration have varied among clinical studies over the last several decades. More recent evidence from large randomized clinical trials has overall supported use of hydrocortisone in those with septic shock, particularly when refractory or severe. The aim of this article is to guide clinical practice regarding steroid administration in septic shock from an evidence-ba

Revisiting the use of steroids in oncology.

Glucocorticoids are cornerstone agents in oncology due to their potent anti-inflammatory, immunosuppressive, and antitumor properties. Glucocorticoids exert direct cytotoxic effects in hematologic malignancies such as lymphomas, acute lymphoblastic leukemia, and multiple myeloma by inducing apoptosis. Their role is primarily supportive in solid tumors, although glucocorticoid receptor signaling may influence tumor progression in cancers like breast and prostate. They are routinely employed to reduce cerebral edema, manage chemotherapy-induced nausea and vomiting, relieve spinal cord compressio

Role of Prophylactic Steroids in Differentiation Syndrome.

Acute promyelocytic leukemia (APML) is defined as a balanced chromosomal translocation between chromosomes 15 and 17 t(15;17)(q24;q21), whic … ffusion are the most common manifestations of DS. Early recognition and prompt initiation of corticosteroids are key factors in the management of DS. As soon as ATRA/ATO therapy is started, prophylactic treatment with steroids has been recommended to minimize the severity of DS. It is proposed that ATRA/ATO should be stopped or held once the signs and symp …

Psychiatric morbidity among men using anabolic steroids.

OBJECTIVE: The purpose of this study was to investigate the psychiatric morbidity among men with abuse of anabolic steroids. METHODS: The design is a retrospectively matched cohort study. Five hundred and fourty-five males, who tested positive for anabolic steroids in Danish fitness centers during the period January 3, 2006 to March 1, 2018, were matched with 5450 randomly chosen male controls. Data was cross-referenced with seven national registers pertaining to information about education, employment status, and psychiatric comorbidity. Main outcomes and measures were prescription of psycho…

Current use and abuse of anabolic steroids.

Common abuse of anabolic androgenic steroids (AAS) is no longer confined to high performance athletes, as it has spread among the general population. Epidemiological data about the abuse of these substances show that it is a common practice in young populations. Its use is based on the desire to increase muscle mass and strength, as well as improving physical performance. The ease of acquisition of this type of substances has developed a "sophisticated" knowledge of steroid pharmacology based on subjective and anecdotal analysis with no adverse event information, which translates into a public…

Anabolic steroids-induced delirium: A case report.

INTRODUCTION: Anabolic steroids are commonly used by athletes, body builders, and young adults to improve muscle strength. Deleterious effects of anabolic steroids on physical health are well-established. Psychiatric aspects are of particular importance and include psychosis, delirium, mania, depression, and aggression. We describe the case of a young gentleman who was managed as a case of androgenic steroid induced delirium. PATIENT CONCERN: A 33-year-old gentleman presented with increased aggression, hostility, and destructive impulses. He was a regular user of testosterone propionate, test…

Safety of Intranasal Steroids: an Updated Perspective.

PURPOSE OF REVIEW: Intranasal corticosteroid sprays have been available as over-the-counter (OTC) medications since 2013. As such, clinicians need to be up-to-date with the risks and the safety of INS, as patients may have concerns and detailed questions. The following is a review of the recent medical literature regarding the safety profile, adverse reactions, and special populations using INS. RECENT FINDINGS: The latest research on intranasal steroid sprays (INS) continue to confirm that INS rarely have significant local side effects, such as severe and persistent epistaxis. Recent studies

Intravitreal steroids for macular edema in diabetes.

BACKGROUND: Diabetic macular edema (DME) is secondary to leakage from diseased retinal capillaries with thickening of central retina, and is an important cause of poor central visual acuity in people with diabetic retinopathy. Intravitreal steroids have been used to reduce retinal thickness and improve vision in people with DME. OBJECTIVES: To assess the effectiveness and safety of intravitreal steroid therapy compared with other treatments for DME. SEARCH METHODS: We searched the Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE, and Embase on 15 May, 2019. We also searched …

Hepatoprotective steroids from roots of Cynanchum otophyllum.

Seven undescribed C21 steroids, namely cynanchin A-G, together with thirteen known analogues, were isolated from the roots of cynanchum otophyllum. Their structures were elucidated by 1D, 2D NMR and MS spectra, as well as chemical methods. Meanwhile, all of isolates were tested for their anti-hepatic fibrosis activity. Among them, compounds 4-6, 10-12 and 14-17 showed moderate or significant inhibitory effects for the proliferation of hepatic stellate cells (HSCs) induced by transforming growth factor-β1 (TGF-β1) in vitro.

Пресечение оплодотворения Аденовирусом кардиотоническими стероидами.

UNLABELELED: Зависимость аденовируса от оборудования для скрещивания всего генома перед РНК, потенциально делает его уязвимым для модуляторов скрещивания РНК, таких, как дигоксин и цифроксин. Оба препарата сократили урожайность четырех человеческих аденовирусов (HAdV-A31, -B35 и -C5 и изолируемый вид D конъюнктивитов) по меньшей мере на 2 - 3 бревен, затронув один или несколько шагов, необходимых для воспроизведения генома. Незамедлительно ранние уровни содержания белка в E1A не затрагиваются лекарствами, но синтез отсроченного белка E4orf6 и крупного гексона протеина капсида скомпрометирован.

Совпадение в аннотации оригинала
UNLABELLED: The dependence of adenovirus on the host pre-RNA splicing machinery for expression of its complete genome potentially makes it v … humans, there are few well-tolerated therapies. In this report, we demonstrate that two cardiotonic steroids already in use in humans, digoxin and digitoxin, are potent inhibitors of multiple adenovirus species. A synthetic derivative of the cardiotonic steroid convallotoxin was even more potent than digoxin and digitoxin when tested with HAdV-C5. These dr …

Effect of inhaled steroids on laryngeal microflora.

Conclusions As is known, this study is the first study to evaluate the effect of inhaled steroids on laryngeal microflora. The data support that ICS usage causes changes in the larynx microflora. Purpose The aim of this study was to determine the alteration in larynx microbial flora of the patients treated with ICS comparing the culture results of a control group. In addition, laryngeal microflora was compared to the smears obtained from the vallecula and pharynx. Materials and methods The study included 39 patients (mean age = 45.56 ± 12.76 years) who had been using a corticosteroid inhaler a…