Sulfamylurea hypoglycemic agents. 6. High-potency derivatives.

  title={Sulfamylurea hypoglycemic agents. 6. High-potency derivatives.},
  author={Reinhard Sarges and Donald E. Kuhla and Hans E. Wiedermann and Dale A. Mayhew},
  journal={Journal of medicinal chemistry},
  volume={19 5},
Synthetic methods for a series of novel sulfamylurea derivatives have been developed. The hypoglycemic activity of simple 1-piperidinosulfonylureas is greatly enhanced by attaching an acylaminoethyl function in the 4 position of the piperidine ring. Optimum activity is achieved when the acyl radical is 5-chloro-2-methoxybenzoyl, 2-methoxynicotinyl, 5-chloro-2-methoxynicotinyl, 1,2-dihydro-1-methyl-2-ketonicotinyl, 2,3-ethylenedioxybenzoyl, quinoline-8-carbonyl, or 6-chloroquinoline-8-carbonyl… 
12 Citations

An improved synthesis of gliamilide®, a high‐potency sulfamylurea hypoglycemic agent

An efficient synthesis of the sulfamylurea, Gliamilide®, is described, which involves as a key feature the selective reduction of the more basic alkyl-substituted pyridine ring in the

Sulfonylureas and Related Compounds: Chemistry and Structure-Activity Relationships

Over the past 40 years, thousands of sulfonamide derivatives have been synthesized and biologically tested for their hypoglycemic activity. A comprehensive review of the molecular variations and

Scalable synthesis and antibacterial evaluation of 2‐(3‐(N‐(substituted phenyl)sulfamoyl)ureido)benzothiazoles

A new series of 2‐(3‐(N‐(substituted phenyl)sulfamoyl)ureido)benzothiazoles was synthesized via a one‐pot efficient and scalable method, involving the condensation of2‐aminobenzothiazole derivatives, substituted anilines, and chlorosulfonyl isocyanate, and their structures were confirmed from their spectral analyses.

Piperidinsulfonylurinstoffer and -thioureas, their preparation, their use and pharmaceutical compositions containing same

The present invention relates Piperidinsulfonylharnstoffe and -thioureas of the formula I, wherein A, X, R (1), R (2) and R (3) have the meanings indicated in the claims. The compounds of formula I

6 Hypoglycaemic Drugs

Synthesis of sultams and related sulfur heterocycles using the ring -closing metathesis reaction

Maria del Sol Jimenez, Ph. D. Department of Chemistry University of Kansas July 2007 The use of ring-closing metathesis (RCM) for the construction of small, medium and large rings has become a

An Improved Method of Chlorinating 2-alkoxynicotinic Acids

Abstract A novel chlorination process for preparing 5-chloro-2-alkoxynicotinic acids has been developed using commercial 5.25% sodium hypochlorite (Clorox®) as a chlorinating agent.