Current Issue : October - December Volume : 2011 Issue Number : 4 Articles : 7 Articles
A new series of substituted benzimidazole derivatives were synthesized based by N-Mannich reaction. Compound B1-B22 synthesized from benzimidazole and 2-mercapto benzimidazole by reacted with formaldehyde and appropriate amine like 5-amino tetrazole, 2-amino pyrazine, Morpholine, Piperidine, aniline, 4-fluro aniline, 4-amino benzoic acid, Isoniazid, diphenylamine, Trietylamine in ethanol. New 22 compounds synthesized based upon Mannich base reaction from the review of literature and characterized by their physical and spectral (IR, PMR and Mass) data. All the compounds have been screened for antituberculosis activities by most of these compounds have shown promising antituberculosis activity.\...
Indoxole an indole derivative is effective against carrageenin-induced edema in intact and adrenalectomized rats and in mice and gerbils. In the present study, an attempt was made to investigate anti-inflammatory activity of I3C (indole-3-carbinol) analogue and its metal complexes. Indeed, the paradox that copper can play both anti-inflammatory and pro-oxidant roles is related to the nature of the biological molecules bound to the metal in vivo. The copper, vanadium and zinc complex were formed with I3C (indole-3-carbinol) ligand. Effect on carrageenan induced mice paw edema, Acetic acid induced writhing, COX-2 inhibition in vitro models were performed to study the anti-inflammatory activity. To summarize the anti-inflammatory activity of I3C analogue and its metal complexes it was observed that copper complex showed highest activity in reduction of edema in carrageenan induced paw edema, protection against acetic acid induced writhing and COX-2 inhibition in vitro followed by zinc, vanadium complexes than plain I3C ligand....
In the past few decades, medicinal chemistry research towards potent and selective antagonists of human adenosine receptors (namely, A1, A2A, A2B, and A3) has been evolving rapidly. These antagonists are deemed therapeutically beneficial in several pathological conditions including neurological and renal disorders, cancer, inflammation, and glaucoma. Up to this point, many classes of compounds have been successfully synthesized and identified as potent human adenosine receptor antagonists. In this paper, an overview of the structure-activity relationship (SAR) profiles of promising nonxanthine pyrazolo derivatives is reported and discussed. We have emphasized the SAR for some representative structures such as pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidines; pyrazolo-[3,4-c] or -[4,3-c]quinolines; pyrazolo-[4,3-d]pyrimidinones; pyrazolo-[3,4-d]pyrimidines and pyrazolo-[1,5-a]pyridines. This overview not only clarifies the structural requirements deemed essential for affinity towards individual adenosine receptor subtypes, but it also sheds light on the rational design and optimization of existing structural templates to allow us to conceive new, more potent adenosine receptor antagonists....
A new series of substituted benzimidazole derivatives have been synthesized and the structures of these compounds have been established on the basis of spectral analysis. All the compounds have been screened for anticancer activities by most of these compounds have shown promising anticancer activity....
An optimized synthetic route to prepare ring-locked retinoid 1a has been developed. We fully describe a purification protocol that provides isomerically pure 1a in support of on-going proof of concept studies for the development of therapeutic agents to treat human ADRP. Additionally, we have found that isomerically pure 1a can be stored in amber vials under argon at- 20�°C for use over time (up to six months) without degradation. Thus, enabling 1a to be an accessible and valuable biological tool....
A large variety of 2-substituted benzimidazoles have been found to possess anti-inflammatory, antimicrobial, anticancer, antihistaminic, antispasmodic, antihypertensive, antidiabetic, antiasthamatic and antitubercular activities. A number of 2- substituted benzimidazole derivatives have been synthesized and tested for their antifungal activities. The chemical structures of the newly synthesized compounds were characterized via IR, 1HNMR and elemental analysis. All the products were screened for antifungal activity against C. albicans, A. niger, A. fumigatus, P. notatum. The results of preliminary biological tests showed that of these compounds possess good antifungal activities with known standard drug ketoconazole....
Two series of fused tetrahydro-�Ÿ-carboline hydantoin and tetrahydro-�Ÿ-carboline thiohydantoin derivatives with a pendant 2,4-dimethoxyphenyl at position 5 were synthesized, and chiral carbons at positions 5 and 11a swing from R,R to R,S, S,R, and S,S. The prepared analogues were evaluated for their capacity to inhibit phosphodiesterase 5 (PDE5) isozyme. The R absolute configuration of C-5 in the �Ÿ-carboline hydantoin derivatives was found to be essential for the PDE5 inhibition. Chiral carbon derived from amino acid even if of the S configuration (L-tryptophan) may lead to equiactive or more active isomers than those derived from amino acid with the R configuration (D-tryptophan). This expands the horizon from which efficient PDE5 inhibitors can be derived and may offer an economic advantage. The thiohydantoin derivatives were less active than their hydantoin congeners....
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