Synthesis and Molecular Docking Study of Some New Thiazole-coumarin Molecular Hybrids as Antibacterial Agents.

Background: The emergence of drug-resistant bacteria and multidrug-resistant diseases, both of which are associated with high mortality, has posed a serious global health issue. Thiazoles and coumarins were reported as antimicrobial agents.

Objective: This research paper aims to describe the synthesis of some novel thiazole derivatives bear-ing a coumarin residue as antibacterial agents Methods: The thiazole - coumarin hybrids were synthesized starting from the condensation of 3-acetyl coumarin (1) hydrazine carbothioamide (2) or thisemicarbazide then reacting the resulting products with different p-substituted phenacyl bromides (4a-e), hydrazonoyl chlorides (8a-e), and (11).

Synthesis and In Silico Study of Some New -[1,3,4]thiadiazolimines and -Thiazolimines as Potential Inhibitors for SARS-CoV-2 Main Protease.

A novel series of -[1,3,4]thiadiazolimines, and -thiazolimines, with alkyl linker, were synthesized through general routes from cyclization of 1,1'-(hexane-1,6-diyl)bis(3-phenylthiourea) and hydrazonoyl halides or -haloketones, respectively. Docking studies were applied to test the binding affinity of the synthesized products against the M of SARS-CoV-2. The best compound, , has average binding energy (-7.

Comparative Study of Intralesional Vitamin D3 Injection and Candida Albicans Antigen in Treating Plantar Warts.

Background: Warts, or verrucae, are mucosal human papilloma virus (HPV) infections that are very challenging to treat.

Objective: To compare the safety and efficacy of intralesional injection of vitamin D3 versus intralesional injection of candida albicans antigen for plantar warts.

Methods: Forty patients were included in the study and were divided into two groups (A&B) with 20 patients each.

Facile synthesis and antiproliferative activity of new 3-cyanopyridines.

Background: Pyridines have been reported to possess various pharmacological activities.

Results: Sodium 3-oxo-3-(2-oxo-2-chromen-3-yl)prop-1-en-1-olate () and sodium 3-oxo-3-(3-oxo-3-benzo[f]chromen-2-yl)prop-1-en-1-olate () were prepared and reacted with 2-cyano-'-(1-aryl(heteryl)ethylidene)acetohydrazides to produce 2-oxo-1,2-dihydropyridine-3-carbonitrile derivatives and , respectively, in good yields. Also, reacted with sodium (2-oxocyclopentylidene)methanolate ( or sodium (2-oxocyclohexylidene) methanolate ) to yield 2-oxo-tetrahydro-1-cyclopenta[b]pyridine-3-carbonitriles and 2-oxo-hexahydroquinoline-3-carbonitriles , respectively.

A facile access and evaluation of some novel thiazole and 1,3,4-thiadiazole derivatives incorporating thiazole moiety as potent anticancer agents.

Background: Many heterocyclic compounds containing thiazole or 1,3,4-thiadiazole ring in their skeletons have been reported to possess various pharmacological activities especially anticancer activities.

Results: 4-Methyl-2-phenylthiazole-5-carbohydrazide (2) was used as a synthon to prepare 2-(4-methyl-2-phenylthiazole-5-carbonyl)-N-phenylhydrazinecarbothioamide (3) and 2-(2-(4-methyl-2-phenylthiazole-5-carbonyl)hydrazono)-N'-phenylpropane hydrazonoyl chlorides 5a-c. In addition, thioamide 3 was used as starting material for preparation of a new series of thiadiazole derivatives via its reaction with hydrazonoyl chlorides 5a-c in dioxane using triethylamines as catalyst.

Green Synthesis and Molecular Docking of Thiazolyl-thiazole Derivatives as Potential Cytotoxic Agents.

Method: A series of novel thiazole derivatives were synthesized in a good yield via reaction of 2-(1-(4-methyl-2-phenylthiazol-5-yl)ethylidene)hydrazine carbothioamide with hydrazonoyl halides. The reaction was performed in the presence of DABCO as an organocatalyst in short reaction times, easy workup, good to excellent yields. The structure of the newly synthesized products was elucidated via elemental analysis, spectral data and alternative routes whenever possible.

Synthesis and SAR Study of the Novel Thiadiazole-Imidazole Derivatives as a New Anticancer Agents.

In the present study, a novel series of 2-(2-(3-aryl-5-substituted-1,3,4-thiadiazol-2(3H)-ylidene)hydrazinyl)-4,4-diphenyl-1H-imidazol-5(4H)-one derivatives were designed and prepared via the reaction of the most versatile, hitherto unreported 2-(5-oxo-4,4-diphenyl-4,5-dihydro-1H-imidazol-2-yl)-N-phenylhydrazinecarbothioamide with the appropriate hydrazonoyl halides. In addition, some thiazole derivatives were prepared. The structures of the newly synthesized compounds were established based on spectroscopic evidences and their alternative syntheses.

Synthesis, Characterization and Molecular Docking of Novel Bioactive Thiazolyl-Thiazole Derivatives as Promising Cytotoxic Antitumor Drug.

Reactions of ethylidenethiocarbohydrazide with hydrazonoyl halides gave 1,3-thiazole or 1,3,4-thiadiazole derivatives according to the type of hydrazonoyl halides. Treatment of ethylidenethiosemicarbazide with hydrazonoyl halides and dimethylacetylene dicarboxylate (DMAD) afforded the corresponding arylazothiazoles and 1,3-thiazolidin-4-one derivatives, respectively. The structures of the synthesized products were confirmed by IR, ¹H-NMR, (13)C-NMR and mass spectral techniques.

Design and Synthesis of Imidazopyrazolopyridines as Novel Selective COX-2 Inhibitors.

The usefulness of non-steroidal anti-inflammatory drugs (NSAIDs) is hampered by their gastrointestinal side effects. Non-selective cyclooxygenases inhibitors interfere with both COX-1 and COX-2 isozymes. Since COX-1 mediates cytoprotection of gastric mucosa, its inhibition leads to the undesirable side effects.