- Synthesis of Novel 1-(5-(Benzylsulfinyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene)-thiourea/urea Derivatives and Evaluation of Their Antimicrobial Activities
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A new series of 1-(5-(benzylsulfinyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene)-thiourea/urea derivatives (1a–j) were designed and synthesized. For the first time, (i) a new process was developed for N-methylation of 1,3,4-thiadiazole moiety using dimethyl carbonate an environmentally benign reagent in presence of N,N,N′,N′-tetramethylethylenediamine and (ii) the sulfide was selectively oxidized to sulfoxide in higher yield by using chlorine (g) in aqueous acetic acid media under mild reaction condition. The synthesized compounds (1a–j) were investigated for their antimicrobial activities. The tested compounds (1a–j) were exhibited moderate to excellent antibacterial activities against both Gram-positive and Gram-negative bacterial strains. The same compounds exhibited good antifungal activities against selected fungal strains. Particularly, the compounds 1b, 1d, 1h, and 1i were proved to be promising leads exhibiting both antibacterial and antifungal activities compared with standard drugs, ciprofloxacin, and fluconazole. The presence of 1,3,4-thiadiazole moiety has a significant role in the display of antimicrobial activity. In addition, the presence of both sulfinyl and thiourea or urea functionalities has enhanced the activity as per obtained antimicrobial activity data.
- Mannam, Madhava Rao,Srimurugan,Kumar, Pramod,R. S. Prasad
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p. 2179 - 2191
(2019/08/01)
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- Compositions and methods for the suppression of carbonic anhydrase activity
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The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing or modulating carbonic anhydrase activity in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of glaucoma, epileptic seizures, Idiopathic intracranial hypertension (pseudotumor cerebri), altitude sickness, cystinuria, periodic paralysis and dural ectasia, congestive heart failure, drug induced edema, diuretic, intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia.
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Page/Page column 27
(2016/04/05)
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- A kind of 1, 3, 4-thiadiazole derivatives, preparation method and application (by machine translation)
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This invention has offered a kind of 1, 3, 4-thiadiazole derivatives, preparation method and application, with the infrared spectrum and nuclear magnetic resonance to characterize its structure, the SRV testing machine evaluation as 150 SN oil additive basis of the friction-reducing and resistance to extreme pressure performance. The result shows that: the synthesized compound has good lubricating performance, can effectively improve the extreme-pressure performance of the lubricating oil with the antifriction performance, it is a kind of excellent performance of the lubricating oil additive. The compounds are in the 5 [...] amino -2 the [...] mercapto -1, 3, 4-thiadiazole as raw materials for synthesis, the reaction process is simple, and easy to realize, the higher the yield of the product, on the production cost can meet the requirement of industrial production. Furthermore, the present invention 1, 3, 4-thiadiazole compounds when used as lubricating oil additive, friction-reducing and extreme pressure resistance is good, can be used as a lubricating oil of the friction-reducing and resistance to extreme pressure additive. (by machine translation)
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Paragraph 0038; 0039; 0040; 0041
(2016/11/02)
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- COMPOSITIONS AND METHODS FOR SUPPRESSION OF CARBONIC ANHYDRASE ACTIVITY
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Provided are the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for treating or preventing or modulating carbonic anhydrase activity in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral admimstration, syrup, or injection. Such compositions may be used to treatment of glaucoma, epileptic seizures, Idiopathic intracranial hypertension (pseudotumor cerebri), altitude sickness, cystinuria, periodic paralysis and dural ectasia, congestive heart failure, drug induced edema, diuretic, intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia.
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Paragraph 0096; 0097
(2013/12/03)
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- Synthesis of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives and evaluation of their antidepressant and anxiolytic activity
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Recently a series of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives bearing different substituents were synthesized and screened pharmacologically in order to evaluate their central nervous system activity. The purpose of this study was to evaluate the effects of the title compounds on CNS activity by varying the substituents in the thiadiazole moiety. It was found that some of these compounds possess marked antidepressant and anxiolytic properties comparable in efficiency to the reference drugs Imipramine and Diazepam. The most potent compound 3k was further investigated to complete its pharmacological profile with respect to undesired side effects. Behavioral results showed that 3k is a very promising compound, characterized by a mixed antidepressant-anxiolytic activity accompanied by a therapeutic dose range that is essentially 2 orders of magnitude less than that at which side effects such as sedation and amnesia are evident.
- Clerici,Pocar,Guido,Loche,Perlini,Brufani
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p. 931 - 936
(2007/10/03)
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