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Answer added in Carboxylic Acids4 Please suggest the best method to convert heteroaryl carboxylic acid to respective hydrazide.Try 1 mmol ethyl-ester with hydrazin hydrate 98% in excess (1:5), in the presence of 2 ml of absolute ethanol, at room temperature (24 h) (stirring)
Publications (18) View all
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Article: New anti-inflammatory thiazolyl-carbonyl-thiosemicarbazides and thiazolyl-azoles with antioxidant properties as potential iNOS inhibitors.
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ABSTRACT: The objective of this study was to investigate the anti-inflammatory and antioxidant activity of new thiazolyl-carbonyl-thiosemicarbazides and thiazolyl-azole derivatives as potential iNOS inhibitors. The in vivo anti-inflammatory effects of the new thiazole compounds were studied in a turpentine oil induced inflammation model. Their anti-inflammatory activity was assessed by evaluating the acute phase bone marrow response, phagocytes' activity, NO synthesis and antioxidant capacity. The new thiazole compounds have anti-inflammatory effects by lowering bone marrow acute phase response and oxidative stress. The best anti-inflammatory and antioxidant effect was found for thiazolyl-carbonyl-thiosemicarbazides Th-1-8, thiazolyl-1,3,4-oxadiazole Th-20 and thiazolyl-1,3,4-thiadiazole Th-21. Virtual screening of thiazole derivatives against the oxygenase domain of chain A from 2Y37 revealed that all twenty-two compounds bind the active site of inducible nitric oxide synthase (iNOS). Based on the virtual screening and on the results obtained above, the activity may be due to their capacity to reduce the NO synthesis by blocking the bind of L-Arg in the active site of iNOS, the compounds binding the synthase by hydrogen bonds between the NH (2 and/or 4) of thiosemicarbazide fragment (Th-2-8) or N2/N3 from azole cycles and by the thiol function (Th-9-22).Archives of Pharmacal Research 03/2013; · 1.59 Impact Factor -
Article: SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME NEW 2-HYDRAZONE-THIAZOLINE-4- ONES
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ABSTRACT: A new series of 2-hydrazone-thiazoline-4-ones 3a-d and 2-hydrazone-5-arylidene-thiazoline-4-ones 4a-h, 5a-f and 6a-b were synthesized starting from various thiosemicarbazones by the Hantzsch condensation with chloroacetic acid. The newly synthesized compounds were screened for their antimicrobial activity against 4 strains of bacteria: Staphylococcus aureus (ATCC 29213), Bacillus subtilis (ATCC 60511), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 10145) and one fungal strain: Candida albicans (ATCC 10231). The compounds 3a-c demonstrated a good inhibitory activity against E. coli. The results of the antifungal screening showed that the 2-hydrazon-thiazolin-4-ones 3c, 3d and 4b presented an excellent activity against Candida albicans.Farmacia 12/2012; 60(6). · 0.67 Impact Factor -
Article: 2. Ioana A. Ionut, Brindusa Tiperciuc, Ovidiu Oniga, Beata Szefler, Raluca Maties, Correlating study on physico-chemical and biological properties of thiosemicarbazone and thiadiazoline derivatives, Studia UBB Chemica, 3, 2012, 109-119
Studia UBB Chemica. 01/2012; 3:109-119. -
Article: 2. Brindusa Tiperciuc, Valentin Zaharia, Ioana Colosi, Cristina Moldovan, Ovidiu Crisan, Adrian Pirnau, Laurian Vlase, Mihaela Duma, Ovidiu Oniga, Synthesis and evaluation of Antimicrobial Activity of Some New Hetaryl-Azoles Derivatives Obtained fromn 2-Aryl-4-methylthiazol-5-carbohydrazydes and isonicotinic Acid Hydrazide, J. Heterocyclic Chem., 2012, 49, 1407, 1414
Journal of Heterocyclic Chemistry 01/2012; 49:1407-1414. · 1.22 Impact Factor -
Article: 1. Dagobert Tazoo, Ovidiu Oniga, D. Scott Bohle, Zhijie Chua, Etienne Dongo, General Two-Step Preparation of Chalcones Containing Thiazole, Journal of Heterocyclic Chemistry, 2012, 49, 768-773
Journal of Heterocyclic Chemistry 01/2012; 49:768-773. · 1.22 Impact Factor
