Current Issue : April - June Volume : 2013 Issue Number : 2 Articles : 8 Articles
1, 3, 4 – Oxadiazole mainly based on a Heterocyclic ring system. In the structure of oxadiazole there are two nitrogen fused with oxygen. Oxadiazole have accelerated interest in various field like medicinal chemistry, polymer industry etc. Heterocyclic compounds have been an interesting area for the study of synthesis and biological activity of novel oxadiazole derivatives for a long time. Oxadiazole are the major compound of heterocyclic nucleus for the development of new drugs and the drugs of oxadiazole were the first effective chemotherapeutic agent to be employed systemically for the prevention & cure of bacterial infection. The heterocyclic compound has been known for several years and investigations in field have been identified due to the large no. of uses & application in most diverse area. Literature survey reveals that the compound are well known to have a no. of broad spectrum biological activities like as antibacterial, anti-inflammatory, anticonvulsant, anticancer, ant tubercular, anti-diabetic, anthelmintic, analgesic etc. Therefore, the synthesis of new 2, 5-di-substituted 1, 3,4oxadiazole derivatives that possess a promising biological activity for the future development to get safer & effective compounds....
Indanone scaffold play important role in the field of medicinal chemistry with so many pharmacological activities such as anti-inflammatory, anticonvulsants, antimicrobial, antiviral, antidiabetic and anticancer activity. The potency of these clinically useful drugs in treatment of microbial infections and other activities encouraged the development of some more potent and significant compounds. There has been considerable interest in development of a promising target for new drug development. Indanone is one such pharmacophore having different pharmacological activities. They are intermediates of many marketed drugs. A number of indanone scaffolds have been synthesized and evaluated for different biological activities. Here we have introduced different indanone scaffold which possess different biological activities depends on its types and position of substituted functional groups. This review is summarized to know about the chemistry of different indanone scaffold along with their pharmacological activities....
Drug discovery is a lengthy and costly process which aims at bringing in a novel therapeutic molecule for the treatment of various diseases. In the present study, various chalcone oxide derivatives were designed to inhibit soluble epoxide hydrolase enzyme (sEH). Lipinski’s rule of five and absorption, distribution, metabolism, elimination and toxicity (ADMET) properties of the compounds were calculated using molinspiration server and Accord for excel software respectively. All 60 compounds have passed the Lipinski’s rule of five and only 14 compounds showed considerable ADMET properties. These 14 compounds were subjected to molecular docking studies using AutoDock 4.2 in order to rationalize the possible interactions between test compounds and the active site of human soluble epoxide hydrolase enzyme (1ZD3). Binding energy, intermolecular energy and inhibition constant were the main parameters taken into consideration in this study. The binding energies ranged from -7.46 to -6.44 Kcal/mol and the structural activity relationship of these compounds was also studied. Based on the docking studies, ((4-acetamido)-(4’-hydroxy)-3’-(morpholino)-sulphonyl) (2E)-1, 3-diphenylprop-2-oxirane-1-one compound was synthesized and structural properties was studied....
Some novel heterocyclic derivatives such as Triazolothiazines, Triazoloxazines, Isoxazoles and Pyrazoles were synthesized from various Chalcones. The synthesized compounds have been characterized by TLC, Elemental analysis, IR and 1HNMR Spectroscopy. These compounds were screened for their Analgesic, Antibacterial and Antifungal activities....
A series of 5-mercapto-1,2,4-triazole derivatives have been synthesized and evaluated for antimicrobial, anti-tubercular and anti-inflammatory activities. The newly synthesized compounds have been characterized by IR, 1H NMR and CHN analysis. All the compounds have shown promising antimicrobial, antitubercular and anti-inflammatory activities when compared with standard drug Norfloxacin, Streptomycin, and Diclofenac sodium respectively....
“2-Benzylidene-2,3-dihydro-1H-inden-1-one” derivatives, is a bicyclic carbonyl compound possessing interesting biological activities i.e., mast cell stabilizing, anticoagulant, acetyl choline esterase inhibition, anti-inflammatory, anti-cancer, anti-malarial and antibacterial activities. Benzylidene substituted 9 Indanone derivatives have been synthesized. The structures of the newly synthesised compounds were established by spectroscopic interpretation (1H NMR, 13C NMR, Mass and IR spectra) studies. Melting range of the synthesised compounds, percentage yield, Rf value, molecular formula, molecular weights were established. After final structural confirmation the synthesized compounds were evaluated for antithrombotic activity....
The pyrazolone ring is an important structural moiety found in numerous pharmaceutically active compounds. This is mainly due to the ease preparation and the important versatile biological activity. When pyrazolones were discovered, they were mostly useful as a anti-inflammatory and analgesic but in recent times, they are known to exhibit antioxidant, anticancer, antibacterial and several other pharmacological actions like antifungal, protein-kinase inhibitor, anti inflammatory, analgesic, antipyretic, anticancer, anticonvulsant, ant diabetic, plant growth regulator ,and herbicidal. These derivatives were withdrawn from the market because of their adverse effects such as agranulocytosis, skin rashes and blood dyscrasis. So, structural modification of pyrazolones is necessary to minimize the side effect and to improve its therapeutic application. But, recently it again gain place in market due to their versatile actions especially in cardiovascular diseases. This review emphasized the recent researches in pyrazolones in various diseases and disorders....
Thiophene is a five member heterocyclic ring with general formula C4H4S. Thiophene moiety have attracted great attention in medicinal field due to its diversified biological activities such as anti microbial activity, anti fungal activity, anti tubercular activity, anti oxidant activity, local anaesthetic activity, 5-HT1A receptor antagonist, 5-HT6 receptor antagonist, anti-inflammatory activity, analgesic activity, anti cancer activity, anti convulsant activity, anti allergy, Phosphodiesterase IV inhibitors, anti histaminic activity and many more. Various synthetic methods have been developed to synthesize this novel heterocyclic nucleus. In this review we have focused on some widely known named as well as general and miscellaneous synthetic methods, chemical properties and diversified pharmacological activities of thiophene nucleus....
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