Current Medicinal Chemistry - Volume 30, Issue 37, 2023

Oteseconazole was approved by the US FDA in April 2022. It is the first approved selective and orally bioavailable CYP51 inhibitor for the treatment of patients with recurrent Vulvovaginal candidiasis. Herein, we describe its dosage, administration, chemical structure, physical properties, synthesis, mechanism of action, and pharmacokinetics.

Sulfonamides, with the general formula R-SO2NR1R2, have attracted great attention since the early discovery of sulfonamide-containing antibacterial drugs. The combinations of certain sulfonamides and other drug molecules to form sulfonamide hybrids are being used to develop novel formulations with greater effectiveness and in a huge range of therapeutic applications such as antimicrobial, antifungal, anti-inflammatory, antitubercular, antiviral, antidiabetic, antiproliferative, carbonic anhydrase inhibitor, antimalarial, anticancer and other medicinal agents. Part C of this review presents recent advances in designing and developing multicomponent sulfonamide hybrids containing more than one biologically active heterocycle, such as coumarin, indole, pyridine, pyrimidine, pyrazole, triazole, oxazole, oxadiazole, triazine, quinazoline, and thiadiazol. This review aims to highlight the status of the hybridization technique in synthesizing biological and computational studies of novel sulfonamide hybrids that were designed and presented between 2016 and 2020.

The epicardial adipose tissue, which is referred to as fats surrounding the myocardium, is an active organ able to induce cardiovascular problems in pathophysiologic conditions through several pathways, such as inflammation, fibrosis, fat infiltration, and electrophysiologic problems. So, control of its volume and thickness, especially in patients with diabetes, is highly important. Incretin-based pharmacologic agents are newly developed antidiabetics that could provide further cardiovascular benefits through control and modulating epicardial adiposity. They can reduce cardiovascular risks by rapidly reducing epicardial adipose tissues, improving cardiac efficiency. We are at the first steps of a long way, but current evidence demonstrates the sum of possible mechanisms. In this study, we evaluate epicardial adiposity in physiologic and pathologic states and the impact of incretin-based drugs.

Background: NR2F1-AS1 is a long non-coding RNA (lnc RNA) that is involved in different biological processes. It plays an integral role in the pathophysiology of human diseases, especially tumorigenesis and progression. Therefore, it may be a promising target for numerous tumor biotherapeutics. The current review study aimed to show the pathophysiological activities and processes of RNA NR2F1-AS1 in cancer cells. Methods: The contents of the present review were based on information obtained from PubMed. In the data search, “NR2F1-AS1” was chosen as the first keyword, whereas “cancer” was chosen as the second keyword. This review selected and summarized studies published between 2019-2021, concerning the biological functions and mechanisms of NR2F1-AS1 in the development of tumorigenesis. Results: It was found that NR2F1-AS1 regulates a variety of biological activities such as proliferation, invasion, migration, and apoptosis. It acts as an oncogene because it is abnormally expressed and promotes the progression of cancer in a variety of malignancies, including esophageal squamous cell carcinoma, non-small cell lung cancer, breast cancer, neuroblastoma, endometrial cancer, thyroid cancer, and gastric cancer. However, it was evident that NR2F1-AS1 inhibits the progression of cancer in cervical squamous cell carcinoma. Conclusion: NR2F1-AS1 is a potential new biomarker and therapeutic target for the treatment of different cancers.