King Saud University

Mohamed Abdulrahman Al-Omar

Abd El-Galil E Amr

Mashooq Ahmad Bhat

Nagy Mahmoud Hassan Khalifa

Ahmed Mohamed Naglah

Abdulrahman Abdulaziz Almehizia

Kamal E H El-Taher

Ghada S Hassan

Fatmah A Al-Omary

Mohamed M Hefnawy

Nawaf Abdulaziz Alsaif

Khalid A Al-Rashood

Adel S El-Azab

Hussein I El-Subbagh

Hamad M Alkahtani

Mohammad Raish

Ahmad Jomah Obaidullah

Ahmed H Bakheit

Alaa A -m Abdelaziz

Mohammed Mater Alanazi

Abdulrahman M Al-Obaid

Alaa A-m Abdelaziz

Mushtaq Ahmad Ansari

Syed Hidayathulla

Hatem A Abuelizz

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 sulindac derivatives are compounds of the formula: wherein R is one of twenty-five substituted or unsubstituted phenyl substituents; and pharmaceutically acceptable salts thereof. The sulindac derivatives are synthesized by refluxing sulindac hydrazide with appropriately substituted benzaldehydes in the presence of ethanol and catalytic amounts of glacial acetic acid. The sulindac derivatives may be used as active ingredients in pharmaceutical compositions for the treatment of inflammation or inflammatory diseases. The sulindac derivatives may also be used as analgesic and/or gastric sparing agents.

Sulindac derivatives

The naphthyridinyl hydrazine derivatives as potent peripheral analgesic agents are (E)-2-(substituted benzylidene)-1-(2,7-dialkyl-1,8-naphthyridinyl) hydrazines that provide effective peripheral analgesic activity, as demonstrated using the mouse writhing test. The new target compounds include at least one compound that demonstrates higher potency in providing analgesic relief in mice (Protection (%)=81.44) compared to the reference drug acetyl salicylic acid (Protection (%)=78.47). These results demonstrated that the target compound exerts acute analgesic action, suggesting that it may represent an alternative in the development of new therapeutic strategies. Preferably, the (E)-2-(substituted benzylidene)-1-(2,7-dialkyl naphthyridinyl) hydrazine has the formula: wherein Rand Rare alkyl, Ris hydrogen, and Ris NO.

Naphthyridinyl hydrazine derivatives as potent peripheral analgesic agents

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 pyrido[2,3-d]pyrimidine derivatives as anticancer agents include 5-(substituted-phenyl)-2-(3-methyl-5-oxo-2H-pyrazol-1(5H)-yl)-7-(pyridin-3-yl)pyrido[2,3-d]pyrimidin-4(3H)-one derivatives having the formula: where R is hydrogen; 2-halo, 3-halo, or 4-halo (Cl, Br, or F); 2-methoxy, 3-methoxy, or 4-methoxy (OCH); 2-nitro, 3-nitro, or 4-nitro (NO); 4-isopropyl, 4-methyl, or 4-cyano (CN); 2-hydroxy or 3-hydroxy (OH), 3-chloro and 5-chloro; 2-methoxy and 5-methoxy, 3-methoxy and 5-methoxy, or 3-methoxy and 4-methoxy; 3,4,5-trimethoxy; or 2-hydroxy and 4-hydroxy; or a pharmaceutically acceptable salt thereof. The derivatives may be useful in treating various cancers, including hepatic, colon, prostate, breast, and lung cancer.

Pyrido[2,3-d]pyrimidines as anticancer agents

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.

Abietic acid derivatives as anti-tumor agents

Antihepatotoxic agents include dihydropyrimidinone derivatives with 1,4-benzodioxane. The antihepatotoxic agents are compounds having the structural formula represented by Formula 1: wherein each Z independently represents O, N or S; X represents O or S; R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl; and pharmaceutically acceptable salts of these compounds.

Antihepatotoxic agents

A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: 

Dihydropyrimidinone derivatives

A substituted pyrazole derivative includes a compound of the formula: or a pharmaceutically acceptable salt thereof.

Substituted pyrazole derivatives

A pentacyclic triterpenoidal derivative can include 3,11-dioxo-24(phenyl)-urs-12-en-24-one (4), 24-norurs-12-en-24(phenyl)-3,11-dione (5), 3,11-dioxo-24(Phenyl)-urs-1,12-diene-24-one (6), or 24-nor-urs-1,12-diene-24(phenyl)-3,11-dione (7). The pentacyclic triterpenoidal derivative demonstrates highly potent 5-lipoxygenase inhibition activity.

Pentacyclic triterpenoidal derivatives

Oleanolic acid methyl ester derivatives demonstrate potent anti-diabetic activities. In in vitro anti-diabetic testing, the derivatives showed more potency regarding dipeptidyl peptidase-4 (DPP-IV) inhibitor activity, peroxisome proliferator-activated receptors (PPARs) agonist activity, and &#x3b1;-Glucosidase inhibitors activity, as compared to reference standards oleanolic acid and acarbose. In in vivo oral hypoglycemic testing, both acute and sub-acute studies demonstrated that the derivatives had high potency and long duration of action compared to the reference standards pioglitazone, acarbose and oleanolic acid.

Oleanolic acid methyl ester derivatives

The glycyrrhetic acid derivatives can include: The glycyrrhetic acid derivatives can be used to treat inflammation and/or ulcers.

Glycyrrhetic acid derivatives

A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: wherein

The substituted naphthyridinyl hydrazine compounds as anti-liver cancer agents are anti-liver cancer agents that inhibit proliferative pathways of cancer cells, thereby exhibiting potent in vitro and in vivo anticancer activity. The compounds have the formula: wherein Rand Reach are selected independently from hydrogen, mercapto, and C-C-alkyl, preferably methyl, ethyl, propyl, isopropyl or halogen; Rand Reach are selected independently from hydrogen, alkyl or halogen; and Ris selected from substituted or unsubstituted aryl, more preferably from substituted phenyl, naphthyl, and substituted or unsubstituted heteroaryl, more preferably from furyl, pyrrolyl, thienyl, imidazolyl, thiadiazolyl, pyridinyl, pyridazinyl, pyrimidinyl, benzothiazolyl, oxadiazolyl or sugar moities. These agents exert their action through topoisomerase II inhibition.

Substituted naphthyridinyl hydrazines as anti-liver cancer agents

Cyclooxygenase inhibitors include compounds of the formula: where R represents phenyl, nitrophenyl, 2-nitrophenyl, 3-nitrophenyl, 4-nitrophenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 3,4-dimethoxyphenyl, 2-methoxyphenyl, 4-hydroxyphenyl, dimethylaminophenyl, 3-methoxyphenyl, 4-ethoxyphenyl, 2,4,5-trimethoxyphenyl, 3,4,5-trimethoxyphenyl, 2,4,6-trimethoxyphenyl, and 2,4-dimethoxyphenyl, 3-hydroxyphenyl, 4-dimethylaminophenyl, or 2,3,4-trimethoxyphenyl.

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Riyadh, Saudi Arabia

Mohamed Abdulrahman Al-Omar