A series of 5-(1,3-benzothiazol-6-yl)-4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazole derivatives was synthesized as transforming growth factor-β (TGF-β) type I receptor (also known as activin-like kinase 5 or ALK5) inhibitors. These compounds were evaluated for their ALK5 inhibitory activity in an...

The title compound, 2-((2-(4-(3-(2,5-Dimethylphenyl)-3-methylcyclobutyl)thiazol-2-yl)hydrazono)methyl)phenol, was characterized by single-crystal X-ray diffraction. In order to calculate molecular geometry along with the infrared, Atoms in Molecules (AIM) analysis and 1H and 13C NMR chemical shi...

A novel one-pot synthesis of sydnones appended to coumarins (4a–r) via thiazole in presence of silica sulfuric acid as a heterogeneous catalyst is discussed. The use of low cost and reusable silica sulfuric acid as catalyst makes this process feasible and convenient. Further, the title compound...

Through a structure-guided rational drug design approach, we have discovered a highly selective inhibitor compound 40 (JSH-150), which exhibited an IC50 of 1 nM against CDK9 kinase in the biochemical assay and achieved around 300–10000-fold selectivity over other CDK kinase family members. In a...

2-amino-4-methylbenzothiazole (AMBT) and one of its derivatives (E)-2-methylbenzo[d]thiazol-2-yl)imino-4-methyl) phenol (MBTP) were used as synergistic pair for the protection of mild steel in 0.5 M HCl. The combination of inhibitors, AMBT-MBTP, adsorbs on electrode surface through chemical and ...

(E)-(4-(2-(benzo[d]thiazol-2-yl)hydrazono)-3-methyl-2,6-diphenylpiperidin-1-yl)(phenyl)methanone [EPHDPM] and its derivatives were synthesized and characterized by FT-IR, 1H NMR, 13C NMR and elemental analysis. The target compound [EPHDPM] was computed using density functional theory (DFT) metho...

New (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones, unsubstituted or carrying fluoro, bromo, methoxy, nitro, methyl and chloro groups on the benzene ring, were synthesized and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria a...

In this study, the synthesis of novel, symmetrical, tetrasubstituted metallo-phthalocyanines (MPc; M = manganese, indium) bearing four 2-(4-methyl-1,3-thiazol-5-yl) ethoxy units has been reported. All of the synthesized compounds have been characterized by using elemental analysis, UV–Vis, FT-I...

Malignant melanoma is an important type of cancer worldwide due to its aggressiveness and poor survival rate. Significant efforts to understand the biology of melanoma and approaches to treat the advanced disease are focused on targeted gene inhibitors. Frequently mutated genes, such as NRAS, B-...

The present article describes the synthesis, in vitro urease inhibition and in silico molecular docking studies of a novel series of bi-heterocyclic bi-amides. The synthesis of title compounds was initiated by benzoylation, with benzoyl chloride (1), of the key starter ethyl 2-(2-amino-1,3-thiaz...

Nowadays, macroalgae are widely discussed as advantageous alternative feedstock for crude bio-oil production using pyrolysis. In the present work, pyrolysis products of Enteromorpha clathrata washed with 7% phosphoric acid, hydrochloric acid and sulfuric acid were studied. In general, washing wi...

Tyrosinase plays a central role in the biosynthesis pathway of melanin pigment and its activity has also been linked to Parkinson's and other neurodegenerative diseases. Melanin functions in the formation of skin color and its unusual levels cause some skin disorders such as pregnancy scar,...

A series of 5,6-diaryl-1,2,4-triazines hybrids bearing a 1,2,3-triazole linker were synthesized by molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, EC-109 and PC-3). The first structure-activity relationship (SAR) fo...

An improved synthesis of (1R,3S)-3-[(tert-butoxycarbonyl)amino]cyclohexanecarboxylic acid from 3-aminobenzoic acid is described utilising milder and more selective conditions. Both a classical salt resolution and an enzymatic approach have been shown to give the desired compound in high selectivity.

The decarboxylation of isatoic anhydrides with disulfides was realized in the presence of sodium dithionite, leading to S-aryl 2-aminobenzothioate derivatives in moderate to excellent yields. Furthermore, the decarboxylation of diphenyldiselenide with isatoic anhydrides was also examined. It was...

We report the synthesis of a series of novel 2′-deoxy-2′,2′-difluoro-5-halouridines and their corresponding phosphoramidate ProTides. All compounds were evaluated for antiviral activity and for cellular toxicity. Interestingly, 2′-deoxy-2′,2′-difluoro-5-iodo- and -5-bromo-uridines showed s...

A cobalt-catalyzed strategy for N-arylmethylation of phosphorylamides was herein achieved with the assistance of azodiisobutyronitrile as the radical initiator and di-tert-butyl peroxide as the oxidant. Both methylarenes and diaryl methanes were compatible under the oxidative conditions, express...

Diaporthin and orthosporin were characterised from the fungus Aspergillus ochraceus D2306. Diaporthin was identified by high-resolution electron impact mass spectrometry and 1H and 13C NMR spectroscopy, from which new spectroscopic assignments were made. Orthosporin was also identified by mass s...

ABSTRACT. 6-Methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole is a high affinity (Ki = 8.2 nM) reversible inhibitor of acetylcholinesterase (AChE). The carbon-11 labeled form was prepared in high (>97%) radiochemical purity and with specific activities of 37 ± 20 GBq/μmol a...

An energetic study of 5-fluoro-2-methylbenzoxazole (FMBO) and of 5-fluoro-2-methylbenzothiazole (FMBT), in condensed and gaseous states, has been performed using calorimetric techniques and computational calculations. The standard (p∘=0.1MPa) molar enthalpies of formation of FMBO and FMBT, in t...