SYNTHESIS AND BIOLOGICAL SCREENING OF BENZIMIDAZOLE DERIVATIVES
We have most of the compounds were very active biological agents, chalcones and pyrazole derivatives were synthesized.
Synthesis and biological evaluation of ticagrelor derivatives as ..
Manjunatha AK, et al. synthesized a series of oxadiazole derivatives (25) shows anti-inflammatory activity using paw edema induced by carrageenan as the method with diclofenac sodium as the reference. In addition these compounds also containing 4-Cl, 4-NO2, 4-F and 3-Cl groups were more active than diclofenac sodium, the compound R=4-F showed maximal analgesic activity .
Ouyang X, et al. synthesized some 1,3,4-oxadiazoles derivatives and evaluated them for their ability to inhibit tubulin polymerization and to arrest mitotic division of tumour cells. Among the synthesized compounds, compound 83 showed potent activity .
Synthesis and antimicrobial activity of Ibuprofen derivatives
This optically active 5-aryl oxazolines were synthesized by coupling of the amino alcohol with either the acids or the nitriles. These oxazoline derivatives were evaluated for their antiproliferative activity against the human lung carcinoma cell line NCI-H460 and the MDR positive human colon adenocarcinoma cell line HCT-15and thier anticancer activity of was evaluated in the syngeneic M5076 murine ovarian sarcoma flank tumor model.
Anti malarial Malaria is a very infectious disease, and malaria infection results in over 300 million clinical cases and 1.5–2.7 million deaths worldwide per year. Most of these cases are caused by Plasmodium falciparum, the most virulent human malaria species. 2-oxazolines have long been recognized for their potent biological activity and cost effective. Oxazoline derivative 69 as a potential anti-malarial agent has been investigated by E. E. Gordey et al 42.
Synthesis and Biological Activities of Transition Metal Complexes ..
N2 - New analogues of n-butylphthalide (NBP) bearing various lengths of alkyl and different substitution at the two-position of phthalide were designed and synthesised. Preliminary evaluation and prediction of ACD LogP software indicate that the derivatives display significant improvement in water solubility than NBP does. Further biological analysis showed that NBP analogues specifically inhibit platelet aggregation induced by arachidonic acid but have no effect on that induced by adenosine 5-diphosphate. Especially compounds 1 and 3 were stronger than classical anti-platelet drug, aspirin, and equal potent with NBP, respectively. These findings provide an alternative approach to the development of NBP analogues with anti-platelet aggregation activity with good water solubility for the intervention of ischemic stroke.
However, 1,3,4-oxadiazole and 1,2,4-oxadiazole are better known, and more widely studied by researchers because of their many important chemical and biological properties. Among heterocyclic compounds, 1,3,4-oxadiazole has become an important construction motif for the development of new drugs. Literature survey revealed that a minor modification in the structure can result in qualitative as well as quantitative changes in the activity, convinced us to begin on the synthesis of various new 1,3,4-oxadiazole derivatives with the aim of having improved activity and lesser toxicity. The synthesis of novel 1,3,4-oxadiazole derivatives and investigation of their chemical properties and biological behaviour has accelerated in the last two decades. In recent years the number of scientific studies with these compounds has increased considerably. Considering the period from 2002 to 2012, the Scifinder Scholar database records 2,577 references to 1,3,4-oxadiazole, demonstrating its relevance for heterocyclic chemistry .
Synthesis and biological activity of aspirin ..
synthesis of ticagrelor and its derivatives has been ..
09/01/2017 · Synthesis and Evaluation of Diorganotin(IV) and Triorganotin(IV) Derivatives of Aspirin, ..
characterization and antibacterial activity ..
synthesis and biological screening of benzimidazole derivatives html full text
Metal Complexes Based on Acetylsalicylic Acid ..
Synthesis and biological evaluation of n-butylphthalide derivatives as anti-platelet aggregation ..
Synthesis, Biological Evaluation and QSAR Studies of …
INTRODUCTION: Benzimidazoles and its derivatives represent one of the most biologically active classes of compounds, possessing a wide spectrum of activities and these are well-documented in literature. They show selective neuropeptides YY1 receptor antagonists 1, potent inhibitors of TIE-2 and VEGFER-2 tyrosine kinase receptors 2, agents 3, gamma-amino butyric acid (GABA) agonists, and 5-HT3 antagonists 4.
-5-substituted phenylisoxazoles derivatives have been ..
The study of the chemistry of Mannich bases is interesting in many aspects; Mannich bases are important intermediates in organic synthesis. Also these molecules are biologically interesting. Many Mannich bases exert potential antibacterial, antifungal, antiviral, antimalarial and antitumor activities. Hence these bases are important for drug discovery. This work was aimed to synthesis of a panel of ketonic and phenolic Mannich bases, elucidation of structures of the targeted molecules via sensitive analytical tools, and evaluation of the synthesized molecules for their antimicrobial activity. Nine Mannich bases were synthesized via a general synthesis protocol. The structures of the synthesized molecules were deduced on the basis of their spectral data (UV,IR,1HNMR and MS). The targeted Mannich bases were screened for their antibacterial and antifungal activities against six standard human pathogens and significant results were obtained. This work could be beneficial for researchers in the field of organic synthesis. It could also be of interest for those who are involved in drug design.
synthesis, docking and antioxidant activity of some …
ABSTRACT:The synthesis of benzimidazoles derivative involves subsequent synthesis of 4-(2-chloro-ethoxy)-benzaldehyde, 4 methyl benzaldehyde followed by benzimidazoles derivative by reaction between amines derivatives and o-phenylenediamine in dimethyl farmamide (DMF) as solvent in the presence of iodine as a catalyst. Iodine is a commercial and environmentally benign catalyst. The yield of all benzimidazole derivatives was found to be in the range of 75 – 94%. The purity of the compounds was ascertained by melting point and TLC. The synthesized compounds were characterized by using IR,1H NMR, and MASS spectral data together with elemental analysis. The synthesized benzimidazole compounds were screened for analgesic and anticonvulsant activity in albino rat (100-200gm) by using Writhing test and maximal electroshock (MES). Out of all compound studied only PS-3, PS-4, PS-5 and PS-6 showed significant analgesic activities and response against MES test.
Characterization and Evaluation of Anti ..
Jain N, et al. synthesized a series of 2-(3,4,5-trihydroxyphenyl)-5-aryl-1,3,4-oxadiazole derivatives (44). All the synthesized compounds were subjected to antimicrobial and anti-fungal activity. Antimicrobial activity was carried out against Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus at a concentration of 100 μg/ml. Streptomycin was used as standard. Anti-fungal activity was performed against Aspergillus niger with test compounds at a concentration of 100 μg/ml. Ketaconazole was the standard drug .
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