Studies on 16,17-Pyrazoline Substituted Heterosteroids as Anti-Alzheimer and Anti-Parkinsonian Agents Using LPS Induced Neuroinflammation Models of Mice and Rats

Alzheimer’s disease (AD) and Parkinson’s disease (PD) are the most common forms of neurodegenerative disorders. Dehydroepiandrosterone (DHEA) has been reported as a neuroprotective steroid useful in the therapeutic management of neurodegenerative disorders such as AD and PD. Herein we report the synthesis and evaluation of a new series of 16,17-pyrazolinyl DHEA analogues <b>2</b>–<b>4a</b>–<b>d</b> as neuroprotective agents using LPS-induced neuroinflammation animal models. Treatment with the pyrazoline substituted steroids considerably improved the LPS-induced learning, memory and movement deficits in animal models. Suppression of biochemical parameters of oxidative and nitrosative stress, acetylcholinesterase activity, and TNF-α levels was also observed. 16,17-Pyrazolinyl steroids <b>2c</b>–<b>4c</b> substituted with a 4-pyridyl moiety at the 5-position of the heterocyclic ring were found to be the most potent agents and produced neuroprotective effects better than standard drugs celecoxib and dexamethasone. Of these pyrazoline substituted steroids, the <i>N</i>-acetyl analogue <b>3c</b> displayed neuroprotective effects better than <i>N</i>-phenyl (<b>4c</b>), which in turn showed potency more than <i>N</i><b>-</b>unsubstituted analogue <b>2c</b>

Crystallization Engineering in Aza-Steroid: Application in the Development of Finasteride

Novel and robust crystallization approach based on solid solution formation was developed for the purification of finasteride. This is an unprecedented approach that describes the use of pure finasteride <b>1</b> to purify different lots of finasteride <b>1</b> (impure) contaminated with dihydrofinasteride <b>2</b>