Design and synthesis of novel 1,3,4-thiadiazole thioglycosides as promising antimicrobial potent structures.

Thiosemicarbazide was used as a key starting material for the building of a diversity of novel heterocyclic moieties. The heterocyclization reaction of thiosemicarbazide derivatives with carbon disulfide in basic conditions afforded novel heterocyclic 1,3,4-thiadiazolethiolate derivatives. 1,3,4-thiadiazole-2-thiol was successfully reacted with protected α-D-gluco- and galacto-pyranosyl bromides in dimethylformamide at room temperature to give the matching 1,3,4-thiadiazole -glycosides in good yields.

Crystal structure of 5-(β-d-gluco-pyran-osyl-thio)--(4-methyl-phen-yl)-1,3,4-thia-diazol-2-amine.

In the structure of the title compound, CHNOS, the bond lengths at the linking sulfur atom are significantly different [1.7473 (17) and 1.811 (2) Å], and the angle at the exocyclic nitro-gen atom is wide at 128.

Crystal structures of three homologues with increasing ring size: 2-meth-oxy-4-(thio-phen-2-yl)-5,6,7,8-tetra-hydro-quinoline-3-carbo-nitrile, 2-meth-oxy-4-(thio-phen-2-yl)-6,7,8,9-tetra-hydro-5-cyclo-hepta-[]pyridine-3-carbo-nitrile and 2-meth-oxy-4-(thio-phen-2-yl)-5,6,7,8,9,10-hexa-hydrocyclo-octa[]pyridine-3-carbo-nitrile.

The title compounds, CHNOS (), CHNOS (), and CHNOS (), form a homologous series in which the size of the saturated ring increases from six- to eight-membered (with four, five and six methyl-ene groups respectively). For and , the central (CH) moieties are all displaced to the same side of their ring, and the CH-CH-CH angles are much wider than the standard value; a database search indicates that these are general features of such ring systems. For , the thio-phene ring lies with the sulfur atom on the opposite side of the C-C bond to the cyano group, in contrast to and .

Crystal structure of 2-amino-5,6,7,8-tetra-hydro-7,7-dimethyl-4-(naphthalen-2-yl)-5-oxo-4-chromene-3-carbo-nitrile.

In the title compound, CHNO, both six-membered rings of the fused heterocyclic system display envelope conformations; the two carbon atoms bearing the methyl groups and the naphthyl substituent both lie outside the planes of the other atoms of each ring. In the crystal, the amino group forms hydrogen bonds of the types N-H⋯O=C and N-H⋯N≡C, leading to the formation of a double layer structure propagating parallel to the plane. Weak C-H⋯O and C-H⋯π inter-actions may reinforce the layers.

Anticolitic activity of prodigiosin loaded with selenium nanoparticles on acetic acid-induced colitis in rats.

Ulcerative colitis (UC) is a chronic autoimmune inflammatory disease associated with extensive mucosal damage. Prodigiosins (PGs) are natural bacterial pigments with well-known antioxidant and immunosuppressive properties. In the current study, we examined the possible protective effect of PGs loaded with selenium nanoparticles (PGs-SeNPs) against acetic acid (AcOH)-induced UC in rats.

Chlororesistoflavins A and B, Chlorinated Benzopyrene Antibiotics Produced by the Marine-Derived Actinomycete sp. Strain EG32.

As part of a collaborative biomedical investigation of actinomycete bacteria isolated from sediments collected along the northern coast of Egypt (Mediterranean Sea), we explored the antibacterial metabolites from a bacterium identified as a sp., strain EG32. HPLC analysis and antibacterial testing against methicillin-resistant (MRSA) resulted in the identification of six compounds related to the resistoflavin and resistomycin class.

Rhamnolipids Nano-Micelles as a Potential Hand Sanitizer.

COVID-19 is a pandemic disease caused by the SARS-CoV-2, which continues to cause global health and economic problems since emerging in China in late 2019. Until now, there are no standard antiviral treatments. Thus, several strategies were adopted to minimize virus transmission, such as social distancing, face covering protection and hand hygiene.

New Route to the Synthesis of Benzamide-Based 5-Aminopyrazoles and Their Fused Heterocycles Showing Remarkable Antiavian Influenza Virus Activity.

This study describes a new route to the synthesis of novel benzamide-based 5-aminopyrazoles and their corresponding pyrazolo[1,5-]pyrimidine and pyrazolo[5,1-][1,2,4]triazine derivatives. Benzamide-based 5-aminopyrazoles were prepared through a reaction of benzoyl isothiocyanate with malononitrile in KOH-EtOH followed by alkylation with alkyl halides and then a reaction with hydrazine. In an attempt to react benzoyl isothiocyanate with ethyl cyanoacetate in KOH-EtOH followed by alkylation with methyl iodide at room temperature and then a reaction with hydrazine has resulted in the formation of 3-ethoxy-5-phenyl-1-1,2,4-triazole.

Mersaquinone, A New Tetracene Derivative from the Marine-Derived sp. EG1 Exhibiting Activity against Methicillin-Resistant (MRSA).

New antibiotics are desperately needed to overcome the societal challenges being encountered with methicillin-resistant (MRSA). In this study, a new tetracene derivative, named Mersaquinone (), and the known Tetracenomycin D (), Resistoflavin () and Resistomycin () have been isolated from the organic extract of the marine sp. EG1.

Heliomycin and tetracinomycin D: anthraquinone derivatives with histone deacetylase inhibitory activity from marine sponge-associated sp. SP9.

Several actinomycetes strains were isolated from different marine sponges collected from the Red Sea shore in Egypt. The efficiency of their crude extracts to inhibit histone deacetylase (HDAC) enzyme was investigated in the nuclear extract of Hela cell line. The crude extract corresponding to sp.

Marine actinomycete crude extracts with potent TRAIL-resistance overcoming activity against breast cancer cells.

Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is a promising anticancer agent, as it can kill tumor cells selectively. In our search of bioactive natural products to overcome TRAIL-resistance, we isolated 47 actinomycete strains from different sediments and seawater samples collected from the Red Sea coast in Egypt and found four crude extracts (EGY1, EGY3, EGY24 and EGY34) displaying TRAIL sensitizing activity in the resistant breast cancer cell line MDA-MB-231. None of these crude extracts exhibited cytotoxic effect on normal mouse embryonic fibroblasts (MEF), with the exception of EGY34.