6636-02-8Relevant articles and documents
Synthesis and biological evaluation of some new furoxan derivatives as anti-inflammatory agents
Amir, Mohd,Verma, Jeevan S.,Tariq, Sana,Somakala,Ehtaishamul Haq
, p. 955 - 959 (2019/05/21)
A new series of furoxan derivatives (3a-k) have been synthesized and characterized by their IR, 1H NMR and mass spectral data. All the compounds have been screened for their anti-inflammatory activity. The compounds 3a, 3b, 3f, 3g, and 3i which show significant anti-inflammatory activity have been further studied for their ulcerogenic activities and nitric oxide releasing properties. Furoxan derivative 3-memyl-4-[{2-(2-phenylacetyl)hydrazono}memyl]-furoxan 3f showed greater anti-inflammatory activity comparable to standard drug ibuprofen. The compound also showed reduced, ulcerogenicity and high nitric oxide releasing properties.
Synthesis & characterization of 2-(substituted-phenyl)acetohydrazide analogs, 1,3,4-oxadiazoles, and 1,2,4-triazine Ring Systems: A novel class of potential analgesic and anti-inflammatory agents
Nayak, Prakash S.,Narayana, Badiadka,Fernandes, Jennifer,Sarojini, Balladka K.,Sheik, Sana,Shashidhara, Kenkere S.,Chandrashekhar, Konambi R.,Byrappa, Kullaiah
, p. 547 - 562 (2016/10/12)
The new series of 2-(substituted-phenyl)acetohydrazides analogs, S-alkylated 5-substituted-1,3,4-oxadiazoles-2-thione derivatives and 5-arylidene-3-substituted-1,2,4-triazines have been synthesized in good yields and characterized by IR, NMR, mass spectral and elemental analyses. All the synthesized compounds 4(a-d), 5(a-d), 7(a-b), and 8(a-f) are evaluated for their in vitro DPPH scavenging, antimicrobial activity, in vivo analgesic, anti-inflammatory activities. The results of the anti-inflammatory activity are supported by molecular docking study with mouse COX-1 (PDB ID: 2CZT) and COX-2 (PDB ID: 3LN1) enzymes to predict their putative interactions. Among all the assays conducted, the compounds 5-(4-bromophenyl)-3-(naphthalen-2-ylmethyl)-1,2,4-triazine (4d) and2-{[5-(diphenylmethyl)-1,3,4-oxadiazol-2-yl]sulfanyl}-N-(pyrazin-2-yl)acetamide (8a) have emerged as the most potent molecules.
Design, synthesis and pharmacological evaluation of novel azole derivatives of aryl acetic acid as anti-inflammatory and analgesic agents
Amir, Mohammad,Saifullah, Khalid,Akhter, Wasim
scheme or table, p. 141 - 148 (2011/10/18)
A series of substituted azole derivatives (3a-e, 4a-e and 5a-e) were synthesised by the cyclisation of N1(diphenylethanoyl)-N 4-substituted phenyl thiosemicarbazides under various reaction conditions. These compounds were tested in v
Unusual behavior in the reactivity of 5-substituted- 1H-tetrazoles in a resistively heated microreactor
Gutmann, Bernhard,Glasnov, Toma N.,Razzaq, Tahseen,Goessler, Walter,Roberge, Dominique M.,Kappe, C. Oliver
, p. 503 - 517 (2011/06/28)
The decomposition of 5-benzhydryl-1H-tetrazole in an N-methyl-2- pyrrolidone/acetic acid/water mixture was investigated under a variety of high-temperature reaction conditions. Employing a sealed Pyrex glass vial and batch microwave conditions at 240 °, the tetrazole is comparatively stable and complete decomposition to diphenylmethane requires more than 8 h. Similar kinetic data were obtained in conductively heated flow devices with either stainless steel or Hastelloy coils in the same temperature region. In contrast, in a flow instrument that utilizes direct electric resistance heating of the reactor coil, tetrazole decomposition was dramatically accelerated with rate constants increased by two orders of magnitude. When 5-benzhydryl-1H-tetrazole was exposed to 220 ° in this type of flow reactor, decomposition to diphenylmethane was complete within 10 min. The mechanism and kinetic parameters of tetrazole decomposition under a variety of reaction conditions were investigated. A number of possible explanations for these highly unusual rate accelerations are presented. In addition, general aspects of reactor degradation, corrosion and contamination effects of importance to continuous flow chemistry are discussed.
New potent inhibitors of tyrosinase: Novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site
Ghani, Usman,Ullah, Nisar
scheme or table, p. 4042 - 4048 (2010/08/06)
A series of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides were tailored and synthesized as new potent inhibitors of tyrosinase. The rationale for inhibitor design was based on the active site structural evidence from the crystal structures of bacterial tyrosinase and potato catechol oxidase enzymes. Kinetic and active site binding studies suggested mono-dentate binding of thiadiazole, oxadiazole, and triazole rings to the active site dicopper center of tyrosinase including hydrophobicity contributing to the potent inhibition. Kinetic plots showed mixed-type of inhibition by all 25 compounds. Substitutions at C3 of the triazole ring and C5 of the thiadiazole/oxadiazole rings were found to be playing a major role in the high binding affinity to tyrosinase. The current work may help develop new potent tyrosinase inhibitors against hyperpigmentation including potential insecticides.
PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS
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Page/Page column 11, (2010/03/02)
Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
5-Sulphanyl-4h-1,2,4-triazole derivatives and their use as medicine
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Page/Page column 12-13, (2008/06/13)
The invention concerns novel 5-sulphanyl-4H-1,2,4-triazole derivatives of formula (1), wherein: R1, R2 and R3 represent variable groups and the methods for preparing them by liquid-phase parallel synthesis processes. Said product exhibit good affinity for certain sub-types of somatostatin receptors; they are particularly useful for treating pathological conditions or diseases wherein one (or more) somatostatin receptors is (are) involved. The invention also concerns pharmaceutical compositions containing said products and their use for preparing a medicine.