3 research outputs found

    3D QSAR STUDIES ON PYRROLOPYRIMIDINES AS SELECTIVE P-GLYCOPROTEIN ANTAGONIST

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    Objective: The present study is wrought to design the 3D QSAR models on pyrrolopyrimidines as p-glycoprotein inhibitors for the treatment of a wide variety of diseases. Methods: A dataset comprising of 33 pyrrolopyrimidine derivatives have been divided into training set and test set. A three dimensional pharmacophore hypotheses were built from training set (24 compounds) using hydrogen bond acceptor, hydrophobic and aromatic features. Results: The proposed model possesses high value of regression coefficient (0.9334) and was validated by using test set predictions. The squared predictive correlation coefficient of 0.985 was observed between experimental and predicted activity values of test set molecules. Conclusion: The nature of fitness and the distance between pharmacophoric features explain the inhibitory activity of pyrollopyrimidines. The proposed pharmacophoric models possess as potential for the design of novel p-glycoprotein inhibitors

    A REVIEW ON THE VARIOUS BIOLOGICAL ACTIVITIES OF THIADIAZOLE

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    Thiadiazole and their derivatives have been studied colossally because of their wide range of biological activity. They are found to be effectual as antibacterial, antimalarial, antiviral, antiinflammatory, anticancer and antianthelminthic agents. Distinct biological activities, such as antibacterial, anti-inflammatory, and antiviral have been consort with 1, 3, 4-thiadiazole derivatives. The substituted 1, 3, 4 Thiadiazole nucleus is particularly ubiquitous, and found in some marketed drugs such as acetazolamide, Methazolamide and antibacterial such as Sulphamethazole, antibiotic like Cefazoline. The synthesis of 1, 3, 4 Thiadiazole derivatives has allured widespread attention due to their diverse biological activities, including antimicrobial, anti-inflammatory, analgesic, and antianthelmintic. These reviews focused on various biological activities consorted with thiadiazole nucleus.Â
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