thiourea and benzisothiazole

thiourea has been researched along with benzisothiazole* in 2 studies

Other Studies

2 other study(ies) available for thiourea and benzisothiazole

Article	Year
Ureas/thioureas of benzo[d]isothiazole analog conjugated glutamic acid: synthesis and biological evaluation. Archiv der Pharmazie, 2013, Volume: 346, Issue:5 A series of urea and thiourea derivatives of glutamic acid conjugated to 3-(1-piperazinyl)-1,2-benzisothiazole were synthesized, spectroscopically characterized, and evaluated for their in vitro antiglycation and urease inhibitory activities. Preliminary screening of the synthesized compounds 1-35 showed significant results. Amongst these, compounds 17-21 and 30-35 bearing fluoro and methoxy substituents, respectively, exhibited inhibitory potency greater than the reference standards. Hence, they may serve as new lead compounds for further development. Topics: Enzyme Inhibitors; Glutamic Acid; Glycation End Products, Advanced; Structure-Activity Relationship; Thiazoles; Thiourea; Urea; Urease	2013
tert-Butyl 1,5-bis(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)-1,5-dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent H+/K(+)-ATPase inhibitors. Bioorganic & medicinal chemistry letters, 2013, Jul-15, Volume: 23, Issue:14 Amino acids are known to possess variable efficacy against ulceration. Considering the good antiulcer activity of amino acids, a series of urea/thiourea derivatives of glutamic acid conjugated benzisothiazole analogue 3a-u with various substituents on aryl ring were synthesized, spectroscopically characterized and evaluated for in vitro H(+)/K(+)-ATPase inhibition. Majority of the compounds possessed potency compared to that of omeprazole, a reference drug. In particular, methoxy derivatives 3p-u were the most active compounds possessing a significant 15-fold increase for para substituent thus, contributing positively to gastric H(+)/K(+)-ATPase inhibition. Topics: Animals; Anti-Ulcer Agents; Carbamates; Gastric Mucosa; Glutamic Acid; H(+)-K(+)-Exchanging ATPase; Proton Pump Inhibitors; Sheep; Thiazoles; Thiourea; Urea	2013

Article

Year

Ureas/thioureas of benzo[d]isothiazole analog conjugated glutamic acid: synthesis and biological evaluation.

Archiv der Pharmazie, 2013, Volume: 346, Issue:5

A series of urea and thiourea derivatives of glutamic acid conjugated to 3-(1-piperazinyl)-1,2-benzisothiazole were synthesized, spectroscopically characterized, and evaluated for their in vitro antiglycation and urease inhibitory activities. Preliminary screening of the synthesized compounds 1-35 showed significant results. Amongst these, compounds 17-21 and 30-35 bearing fluoro and methoxy substituents, respectively, exhibited inhibitory potency greater than the reference standards. Hence, they may serve as new lead compounds for further development.

Topics: Enzyme Inhibitors; Glutamic Acid; Glycation End Products, Advanced; Structure-Activity Relationship; Thiazoles; Thiourea; Urea; Urease

2013

tert-Butyl 1,5-bis(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)-1,5-dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent H+/K(+)-ATPase inhibitors.

Bioorganic & medicinal chemistry letters, 2013, Jul-15, Volume: 23, Issue:14

Amino acids are known to possess variable efficacy against ulceration. Considering the good antiulcer activity of amino acids, a series of urea/thiourea derivatives of glutamic acid conjugated benzisothiazole analogue 3a-u with various substituents on aryl ring were synthesized, spectroscopically characterized and evaluated for in vitro H(+)/K(+)-ATPase inhibition. Majority of the compounds possessed potency compared to that of omeprazole, a reference drug. In particular, methoxy derivatives 3p-u were the most active compounds possessing a significant 15-fold increase for para substituent thus, contributing positively to gastric H(+)/K(+)-ATPase inhibition.

Topics: Animals; Anti-Ulcer Agents; Carbamates; Gastric Mucosa; Glutamic Acid; H(+)-K(+)-Exchanging ATPase; Proton Pump Inhibitors; Sheep; Thiazoles; Thiourea; Urea

2013