In the current work, aromatic amines and alkyl halides have been converted to the corresponding azides 2a‒d and 4a-d by the reaction with sodium nitrite and sodium azide respectively for amines and sodium azide for halides. Then, dipropargyl ether derivative of D-mannose 8 has been synthesized from diacetone mannose that has been obtained by the treatment of D-mannose (5) with dry acetone in the presence of sulfuric acid. Then, aldol condensation has been used to prepare diol 7 from the mannose diacetonide 6. The reaction of compound 7 with propargyl bromide in alkaline media has been afforded dipropargyl
... Show MoreA group of derivatives for compounds 2-Amino-3-carboxy-4,5,6,7-tetra hydrobenz -othiophene bearing different heterocyclic moieties such as Schiff bases. B-Lactum, 4-thiazolidinone.1,3-oxazepan. The newly synthesized derivatives have been supported by spectral data FT-IR, H1-NMR. All the synthesized compounds were screened for their antimicrobial activities against gram-positive and gram-negative bacteria as reference.
Primary amide derivatives as histone deacetylase inhibitors (HDACIs) are very rare. This paper describes the synthesis of primary amide derivatives (compounds 6 and 7) that have the requirements to be histone deacetylase inhibitors of the zinc-binding type. Both of them exhibited good cytotoxicity against the tested cancer cell lines with much lower cytotoxicity against normal cell line.
Abstract Bilastine, a second-generation antihistamine, is commonly prescribed for managing allergic rhinoconjunctivitis and urticaria due to its prolonged action. However, its therapeutic potential is constrained by poor water solubility and low oral bioavailability. This study aimed to enhance bilastine dissolution and patient compliance by formulating a nanosuspension-based orodispersible film (ODF). An anti-solvent precipitation method was employed to produce nanosuspension using different hydrophilic stabilizers (Soluplus®, Poloxamer 188, and PEG 6000). The influence of formulation parameters, such as the stabilizer ratio, the anti-solvent ratio, stirring speed, and the stabilizer type, on particle size and polydispersity index (PDI)
... Show MoreRegulatory T (Treg) cells are one of the major immunosuppressive cell types in cancer and a potential target for immunotherapy, but targeting tumor-infiltrating (TI) Treg cells has been challenging. Here, using single-cell RNA sequencing of immune cells from renal clear cell carcinoma (ccRCC) patients, we identify two distinct transcriptional fates for TI Treg cells, Fate-1 and Fate-2. The Fate-1 signature is associated with a poorer prognosis in ccRCC and several other solid cancers. CD177, a cell surface protein normally expressed on neutrophil, is specifically expressed on Fate-1 TI Treg cells in several solid cancer types, but not on other TI or peripheral Treg cells. Mechanistically, blocking CD
Highly Modified Asphalt (HiMA) binders have garnered significant attention due to their superior resistance to rutting, fatigue cracking, and thermal distress under heavy traffic loads and extreme environmental conditions. While elastomeric polymers such as Styrene- Butadiene-Styrene (SBS) have been extensively used in HiMA applications, the potential of plastomeric polymers, including Polyethylene (PE) and Ethylene Vinyl Acetate (EVA), remains largely unexplored. This study aims to evaluate the performance of reference binder (RB) modified with plastomeric HiMA asphalt in comparison to SBS-modified binders and determine the optimal polymer dosage for achieving an optimal balance between rutting resistance and fatigue durability. The experi
... Show MoreBackground: Semen contamination is a detrimental factor in decreasing fertility. Seasonal changes may affect the contamination, too. Objectives: This study was designed to detect semen contamination in ovine and caprine during different seasons. Methods: Six fully mature male sheep and goats were subjected to electro-ejaculator collection twice monthly from February 1, 2022, to January 31, 2023 (Spring, February 1, 2022-April 30, 2022; Summer, May 1, 2022, July 31, 2022; Autumn August 1, 2022, October 31, 2022; Winter November 1, 2022, January 31, 2023), for studying the seasonal effect. A total of 288 semen samples were collected from both species (36 samples from each per season). All samples were subjected to bacterial isolatio
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