King Saud University

Abdulrahman Abdulaziz Almehizia

Mohamed Abdulrahman Al-Omar

Abd El-Galil E Amr

Ahmed Mohamed Naglah

Nawaf Abdulaziz Alsaif

Mohammed Mater Alanazi

Ahmad Jomah Obaidullah

An ursolic acid derivative can have the following structural formula: The ursolic acid derivative exhibits potent selective calcium channel blocker activities and may be used to treat a disease or condition for which calcium channel regulation is useful.

Ursolic acid derivatives

The sulfonylurea derivatives of oleanolic acid include compounds replacing the 5-chloro-2-methoxybenzoic acid moiety found in glibenclamide with oleanolic acid. The resulting triterpenoidal sulfonylurea derivatives are compounds having the following formula: or a pharmaceutically acceptable salt thereof. The derivatives are synthesized by condensation of 3-oxo-Olean-12-en-28-oic acid with 4-(2-aminoethyl)benzenesulfonamide to form an intermediate product, followed by reaction with cyclohexyl isocyanate or 4-methylcyclohexyl isocyanate to give 3a or 3b, respectively. The sulfonylurea derivative compounds were screened for their oral hypoglycemic activity in vivo using the alloxan-induced diabetic mouse model and proved more potent than either glibenclamide or oleanolic acid.

Sulfonylurea derivatives of oleanolic acid

The abietic acid derivatives as anti-tumor agents are derivatives of abietic acid in which the hydroxyl entity (&#x2014;OH) of the carboxyl entity is replaced by an electronegative substituent, which may be C6H5-O&#x2014;, C6H5-S&#x2014;, or C6H5-NH&#x2014;, and a hydrogen atom on one of the rings is replaced by a hydroxyl (&#x2014;OH) substituents, the derivatives having the formula: wherein X is O, S, or NH. The derivatives are formed by formation of an intermediate lactone from abietic acid, followed by reaction of the lactone with phenol, thiophenol, or aniline. All of the derivatives exhibited potent 5&#x3b1;-reductase inhibitor activity, both in vitro and in vivo, and anti-tumor activity with regard to two prostate cancer cell lines&#x2014;LNCaP and PC-3. The intermediate lactones are also derivatives of abietic acid that exhibit anti-tumor activity.

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Riyadh, Saudi Arabia

Abdulrahman Abdulaziz Almehizia