Syed Z. Ahmed

Synthesis of deuterium-labeled atorvastatin and its metabolites for use as internal standards in a LC/MS/MS method developed for quantitation of the drug and its metabolites in human serum

D5-labeled isotopomers of atorvastatin, atorvastatin lactone and its hydroxy metabolites were synthesized as internal standards for use in a LC/MS/MS method developed for the simultaneous quantitative determination of atorvastatin and its hydroxy metabolites in human serum. d5-Atorvastatin and d5-atorvastatin lactone were prepared from d5-aniline whereas their corresponding hydroxy metabolites were synthesized using d5-benzaldehyde. Copyright

Aryl cyanoguanidine potassium channel openers

Abstract To investigate whether potassium channel openers cromakalim ( 1 ) and pinacidil ( 2 ) share common pharmacophoric features, the combination compound 6a was prepared and evaluated for biological activity. The potent vasorelaxant/antihypertensive activity displayed by 6a and some of its analogs suggest cromakalim ( 1 ) and pinacidil ( 2 ) may shrare common pharmacophoric features.

(cis)-3-methyl-1,5-benzothiazepine-4-ones: potent analogs of the calcium channel blocker diltiazen

Abstract 3-Methyl analogs of the calcium channel blocker diltiazem are reported. The title compounds were prepared from readily available amino thiophenols by a six step sequence which involves setting up the desired 2,3-cis-stereochemistry through decarboxylation under acidic conditions. To our knowledge, there are the most potent analogs of diltiazem reported to date.

Benzopyranyl-cyanoguanidine potassium channel openers

Abstract To further investigate whether potassium channel operators cromakalim (1) and pinacidil (2) share common pharmacophoric features, the cyanoguanidine analog 4a of cromakalim (1) was prepared and evaluated for biological activity. the potent vasorelaxing activity displayed by 4a and some of its analogs support the hypothesis that cromakalim (1) and pinacidil (2) share common pharmacophoric features.

The discovery of a novel calcium channel blocker related to the structure of potassium channel opener cromakalim

Abstract During our studies aimed at the identification of novel analogs of the potassium channel opener cromakalim ( 3 ), we serendipitously observed pyranoquinoline 4 to possess pure calcium channel blocking activity. The results of the studies conducted to confirm the calcium channel blocking mechanism of 4 are reported in this paper.

Trimethylaluminum promoted synthesis of cyanoguanidines

Abstract Synthesis of cyanoguanidines from N-cyano-O-phenylisoureas and relatively nonbasic amines (e.g., aniline) using trimethylaluminum is reported.