RESUMEN
A new series of 3-(4-substituted phenyl)-1-(4-(4,6-dimethyl-6H-1,3-thiazin-2-yl)phenylsulfonyl)-1-substituted urea (5a-o) was synthesized by an effectual route via sulfonylcarbamates and explores the novel site for substitution in sulfonylurea as well as the way of thiazine can be prepared. The molecules were established by elemental analysis and spectroscopic viz. IR, (1)H NMR, (13)C NMR and MS techniques. All the fifteen derivatives were shown very prominent oral hypoglycemic effect at the dose of 40 mg/kg body weight (p.o.) in respect of standard drug glibenclamide and control. The hypoglycemic effect was studied using oral glucose tolerance test in normal and NIDDM in STZ-rat model. The compounds 5a, 5d, 5f, 5i, 5k and 5n were dominant out of fifteen derivatives for blood glucose lowering activity (more than 80%) when comparing with NIDDM control. These derivatives were either containing simply phenyl ring (5a, 5f and 5k) on to the second amine of sulfonylurea (R' = H) or nitro group at the para position in compound 5d, 5i and 5n (R' = NO2 ) to produce significant oral hypoglycemic effect. Other structural activity relationship is also observed regarding the heteroaromatic and substituted aromatic group at R and R' position respectively.
RESUMEN
Filariasis is result of parasitic infection caused by three specific kinds of round worm. Lymphatic filariasis is found in under developed region of South America, Central Africa, pacific and Caribbian. It has been found for centuries, with main symptoms as elephant like swelling of the arms, legs and genitals. It is estimate that 120 millions peoples in the world have lymphatic filariasis. The spread of diseases and the challenge encountered in its management are discussed along with a review on drugs against filariasis in this article. Detail on clinical effect of drugs on the infection, safety profile, status in clinical practices and drug resistances are also covered.
