Synthesis, human carbonic anhydrase I and II inhibition, and in silico studies of 2-ethoxy-6-formylphenyl [1,1'-biphenyl]-4-sulfonate derived thiosemicarbazones.

This study describes the synthesis and biological evaluation of 2-ethoxy-6-formylphenyl [1,1'-biphenyl]-4-sulfonate-based thiosemicarbazones 5(a-s) as potential inhibitors of human carbonic anhydrase isoforms hCA I and hCA II. Among the synthesized compounds, 5 k exhibited potent inhibition, with IC values of 89.25 nM and 54.

Design, Synthesis, In Vitro, and In Silico Studies of 5-(Diethylamino)-2-Formylphenyl Naphthalene-2-Sulfonate Based Thiosemicarbazones as Potent Anti-Alzheimer Agents.

Alzheimer's disease (AD) is known as one of the more devastating neurodegenerative diseases diagnosed in older people. Cholinesterase inhibitors (ChEI) can be used as an effective palliative treatment for AD. An extensive range of new biologically active 4-(diethylamino) salicylaldehyde-based thiosemicarbazone derivatives 5(a-u) was synthesized and evaluated as inhibitors of cholinesterase (ChE) and monoamine oxidase (MAO) enzymes.

Synthesis, Anti-Alzheimer Evaluation and In Silico Study of 4-Methoxyphenyl)Sulfonyl Indole Hybrid Thiosemicarbazones.

Alzheimer's disease (AD) is a multifaceted neurological disorder linked to behavioral, psychological, and language abnormalities as well as memory loss. A series of 1-[(4-methoxyphenyl)sulfonyl]-1H-indole-3-carbaldehyde-based thiosemicarbazones 5(a-v) had been synthesized and screened for their potential against AD. The compounds were tested for their inhibitory effects against cholinesterases (AChE and BChE) and monoamine oxidase A (MAO-A).

Design, synthesis, in-vitro and in-silico studies of novel N-heterocycle based hydrazones as α-glucosidase inhibitors.

Diabetes mellitus has dominated the globe as a chronic health condition and has become a major global health concern. The inhibition of the key metabolic enzymes of carbohydrates digestion including α-amylase and α-glucosidase are the promising targets for the treatment of diabetes via delaying glucose absorption. Therefore, nitrogen containing saturated heterocycle (pyrrolidinyl, piperidinyl and N-methylpiperazinyl) based hydrazones derivatives 5-23 were synthesized through two step reactions and evaluated for their anti-diabetic potential.

Design, synthesis, in vitro, and in silico studies of 4-fluorocinnamaldehyde based thiosemicarbazones as urease inhibitors.

Clinically significant problems such as kidney stones and stomach ulcers are linked to the activation of the urease enzyme. At low pH, this enzyme gives an ideal environment to Helicobacter pylori in the stomach which is the cause of gastric ulcers and peptic ulcers. In recent work, we have developed a library of 4-fluorocinnamaldehyde base thiosemicarbazones and assessed them for their potential against urease enzyme.

Design, synthesis, QSAR modelling and molecular dynamic simulations of N-tosyl-indole hybrid thiosemicarbazones as competitive tyrosinase inhibitors.

Tyrosinase is an enzyme crucial for the progression of melanogenesis. Immoderate production of melanin may be the cause of hyperpigmentation and darkening leading to skin diseases. Tyrosinase is the most researched target for suppressing melanogenesis since it catalyzes the rate-limiting stage of melanin production.