Hypoglycemic prodrugs of 4-(2,2-dimethyl-1-oxopropyl)benzoic acid

Journal of Medicinal Chemistry

Volumn 42, Issue 1, 1999, Pages 153-163

  Aicher, Thomas D ^a   Bebernitz, Gregory R ^a   Bell, Philip A ^a   Brand, Leonard J ^a   Dain, Jeremy G ^a   Deems, Rhonda ^a   Fillers, William S ^a   Foley, James E ^a   Knorr, Douglas C ^a   Nadelson, Jeffrey ^a   Otero, Dario A ^a   Simpson, Ronald ^a   Strohschein, Robert J ^a   Young, Douglas A ^a  

^a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (1,1 DIMETHYLETHYL) 2 (4 METHYLPHENYL) 1,3 DIOXOLANE; 4 (1 HYDROXY 2,2 DIMETHYLPROPYL)BENZOIC ACID; 4 (2,2 DIMETHYL 1 OXOPROPYL) N METHOXYBENZENE CARBOXIMIDIC ACID; 4 (2,2 DIMETHYL 1 OXOPROPYL)BENZOIC ACID; ANTIDIABETIC AGENT; BENZOIC ACID DERIVATIVE; FOX 988; PRODRUG; SAH 51641; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG DESIGN; DRUG MECHANISM; DRUG POTENCY; DRUG SYNTHESIS; GLUCONEOGENESIS; HYPERGLYCEMIA; INSULIN DEPENDENT DIABETES MELLITUS; MALE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; ORAL DRUG ADMINISTRATION; RAT; REPRODUCTIVE TOXICITY; STREPTOZOCIN DIABETES; TESTIS DISEASE;

ACETOPHENONES; ANIMALS; BENZOATES; BENZOIC ACIDS; DIABETES MELLITUS, EXPERIMENTAL; DRUG EVALUATION, PRECLINICAL; FATTY ACIDS; GLUCONEOGENESIS; HYPOGLYCEMIC AGENTS; LIVER; MALE; OXIDATION-REDUCTION; PRODRUGS; RATS; RATS, SPRAGUE-DAWLEY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TESTIS;

EID: 0033552861     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm980438y     Document Type: Article

References (35)

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31. Normal rats fasted for 6 h were assumed to have a blood glucose of 60 mg/dL, and the percent efficacy was calculated based upon the percent normalization of glucose levels of treated vs control groups. The percent efficacy so calculated was utilized as a tool to be able to qualitatively compare two different experiments in which the diabetic nontreated control groups had blood values of 220 or 170 mg/dL after a 6-h fast. In a representative experiment with FOX 988, the glucose of the untreated diabetic animals was 200 ± 10 mg/dL. The treated animals (140 mmol/ kg) displayed a glucose level of 100 ± 20 mg/dL (p < 0.001). This may actually represent a normalization of glucose. In our table, we represent these data as displaying a 70% efficacy.
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