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- Title
Evaluation of Physicochemical Properties of Glacial Acetic Acid Mediated Solvent Free One Pot Synthesis of malonylurea and Its Chloroacetylated Derivatives.
- Authors
Chahal, Piyush; Singh, Ranjeet; Kumar, Kuldeep
- Abstract
Barbiturates or malonylureas are an important class of heterocyclic scaffold because they possess a wide range of therapeutic and pharmacological properties. Barbiturates and its derivatives include a wide range of pharmacological activities such as anticonvulsant, antianxiety, analgesic, sedative, antidepressive and hypnotic agents. In 1864 Adolf von Bayer developed malonylurea. Barbiturates are basically a closed-chain ureic compound, whose nucleus is malonylurea. Malonyurea is a combination of urea and malonic acid, an acid derivative taken from apples. A series of compounds of malonylurea and its chloroacetylated derivatives have been synthesized and its physicochemical parameters were evaluated in order to determine the potency of the compounds for good CNS activity. This solvent-free reaction mediated by glacial acetic acid was found to be very efficient with high yield. The structures were confirmed on the basis of TLC, IR and 1HNMR and CHN elemental studies. The log P values of two of the compounds shows that compounds have the potential to be CNS active and all other parameters like nonvalue, non-value, nviolations, and number of rotatable bonds also lies in the ranges that are required for bloodbrain barrier penetration. This synthesis provides a new hope that the free chloro group in this structure can be utilized for further substitution of various heterocyclic rings which possess potent CNS activity.
- Subjects
ACETIC acid; MALONIC acid; QUINAZOLINONES; ANTIDEPRESSANTS; FREE groups; ACID derivatives
- Publication
International Journal of Pharmacy & Life Sciences, 2019, Vol 10, Issue 6, p86
- ISSN
0976-7126
- Publication type
Article