Keywords: 5-amino-1,3,4-thiadiazole-2-thiol derivatives, diuretic activity, saluretic/natriuretic/carbonic anhydrase inhibition indexes, SAR,

Pregnant Wistar rats were each injected once ip with various doses of 2-amino-l,3,4-thiadiazole hydrochloride (ATDA) at days 1-16 of gestation (sperm day = day 0). The optimal teratogenic dose was determined to be 100 mg/kg and this dose was employed throughout the experiment, At autopsy at day 20 resorptions and malformations were found in all litters from treated females. Two periods of incre...

We report on the interaction of Lewis acids with narrow band gap conjugated copolymers containing donor and acceptor units. Examination of the widely used poly[(4,4-bis(2-ethylhexyl)cyclopenta-[2,1-b:3,4-b']dithiophene)-2,6-(diyl-alt-benzo[2,1,3]thiadiazole)-4,7-diyl] (1) shows weaker binding with B(C(6)F(5))(3) when compared with a small molecule that contains a cyclopenta-[2,1-b:3,4-b']dithio...

Saisentong, as a thiadiazole fungicide, is widely used in China. The structure of saisentong shows a closer relationship to N, N-methylene-bis (2-amino-1, 3, 4-thiadiazole) (Bis-A-TDA), which is a teratogen. A few studies have shown that some of the thiadiazole fungicides act as endocrine disruptors via disturbance in thyroid hormone homeostasis. Little is known about the effect of pubertal exp...

Tyrosine kinase receptor and protein kinases drawn much attention for the scientific fraternity in drug discovery due to its important role in different cancer, cardiovascular diseases and other hyper-proliferative disorders. Docking studies of pyrazole derivatives with tyrosine kinase and different serine/threonine protein kinases were employed by using flexible ligand docking approach of Auto...

Sulfones are one of the most important classes of agricultural fungicides. To discover new lead compounds with high antibacterial activity, a series of new sulfone derivatives were designed and synthesized by introducing the aroxymethyl moiety into the scaffold of 1,3,4-oxadiazole/thiadiazole sulfones. Antibacterial activities against three phytopathogens (Xanthomonas oryzae pv. oryzae, Ralston...

BACKGROUND Cutaneous Leishmaniasis (CL) is endemic in many tropical and subtropical regions of the world. Due to the prolonged duration of therapy, adverse effect and resistance to current drugs in the treatment of CL, the discovery of novel, efficient, and safe leishmanicidal drugs is required. The aims of the present study was to synthesis of new compounds based on the active compounds of 5-(...

A series of 2-(p-substituted benzylidene)-3-(5-ethyl-1, 3, 4-thiadiazol-2-yl) thiazolidin-4-ones were synthesized by the reaction of Schiff’s bases of N-(p-substituted benzylidene)-5-ethyl-1, 3, 4-thiadiazole-2-amines with thioglycolic acid in 1, 4-dioxane as solvent and studied for their in vitro antibacterial activity. Reaction of thiosemicarbazide with propanoic acid in presence of concentra...

HIE-124 is the new member of ultra-short acting hypnotics drug family. In this research, thiadiazole can act as the bio-isosteric replacement of thiazole in synthesized compounds as HIE-124 derivatives. HIE-124 drug, in which the heterocyclic thiazole ring replaced to thiadiazole, will be presented. Thiadiazolodiazepines were synthesized by a two-step reaction starting from the amino thiadiazol...