- Synthesis, Antileishmanial Activity and In Silico Studies of Aminoguanidine Hydrazones (AGH) and Thiosemicarbazones (TSC) Against Leishmania chagasi Amastigotes
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Background: Leishmaniasis is a worldwide health problem, highly endemic in developing countries. Among the four main clinical forms of the disease, visceral leishmaniasis is the most se-vere, fatal in 95% of cases. The undesired side-effects from first-li
- Alexandre-Moreira, Magna S.,Aquino, Pedro G. V.,Bourguignon, Jean-Jacques,Bri-Card, Jacques,Freitas, Johnnatan D.,Meneghetti, Mario R.,Nascimento, Igor J. S.,Queiroz, Aline C.,Rodrigues, Klinger A. F.,Rodrigues, Raiza R. L.,Santos, Mariana S.,Schmitt, Martine,de Aquino, Thiago M.,Araújo, Morgana V.,Fran?a, Paulo H. B.,Rodrigues, érica E. E. S.,Santos-Júnior, Paulo F. S.,da Silva-Júnior, Edeildo F.,de Araújo-Júnior, Jo?o X.
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p. 151 - 169
(2022/02/05)
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- Synthesis and antitubercular activity of 2-(1H-pyrrol-1-Yl)-5- substituted-1,3,4-oxadiazoles
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A series of 2-(1H-pyrrol-1-yl)-5-substituted-1,3,4-oxadiazole derivatives were prepared and evaluated for their antitubercular activity. These derivatives were synthesized by the reaction of 5-substituted-1,3,4-oxadiazol-2-amines (4a-j) with 2,5- dimethoxytetrahydrofuran in dried acetic acid. Structures of the newly synthesized compounds were confirmed on the basis of physico-chemical and spectral data. All the synthesized compounds were screened for their antitubercular activity using microplate almar blue assay (MABA) method. Compounds have shown moderate to good antitubercular activity against M. tuberculosis H37Rv microorganism.
- Joshi, Shrinivas D.,Dixit, Sheshagiri R.,More, Uttam A.,Kulkarni, Venkatrao H.
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p. 137 - 140
(2019/01/21)
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- Electrochemical synthesis of 2-amino-5-substituted-1,3,4-oxadiazole derivatives and evaluation of antibacterial activity
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Some new 2-amino-5-substituted-1,3,4-oxadiazoles have been synthesized at platinum electrode through the electrochemical oxidation of semicarbazone at room temperature and studied for their antibacterial activity. This is an environmentally benign method in the field of electroorganic synthesis under controlled potential electrolysis in an undivided cell. The electrolysis have been carried out in the acetonitrile solvent and lithium perchlorate is used as a supporting electrolyte. Two platinum plates are used as working as well as counter electrode and saturated calomel electrode as the reference electrode. These compounds have been characterized by microanalyses, IR, Mass, 1H NMR and 13C NMR spectral data. All the compounds have been evaluated for their antibacterial activity against Klebsilla penumoniae, Escherichia coli, Streptococcus aureus and Shigella dysenteriea at 25 and 50 ppm concentrations.
- Kumar, Sanjeev,Pandey
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p. 252 - 258
(2013/05/09)
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- Evaluation of semicarbazones for anticonvulsant and sedative-hypnotic properties
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A series of semicarbazones and thiosemicarbazones were synthesized and evaluated for anti-convulsant activity. Some compounds provided significant protection against Maximal Electroshock (MES) and subcutaneous strychnine induced seizures. Compound 1 was the most active in the series with activity in a dose of 30 mg/kg in the strychnine seizure pattern test and an ED50 of 10 mg/kg in the MES test. Hence it could serve as a prototype molecule for future development. Also compounds with a p-nitrophenyl substitution in place of the amino hydrogen of semicarbazone moiety showed activity in a dose of 30 mg/kg and an ED50 of 83 mg/kg in the MES test.
- Pandeya,Aggarwal,Jain
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p. 300 - 302
(2007/10/03)
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