• Aamer Saeed

      Articles written in Journal of Chemical Sciences

    • Sodium borohydride reduction of aromatic carboxylic acids via methyl esters

      Aamer Saeed Zaman Ashraf

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      A number of important aromatic carboxylic acids precursors, or intermediates in the syntheses of natural products, are converted into methyl esters and reduced to the corresponding primary alcohols using a sodium borohydride-THF-methanol system. The alcohols are obtained in 70–92% yields in 2–5 hours, in a pure state. This two-step procedure not only provides a better alternative to aluminum hydride reduction of acids but also allows the selective reduction of esters in presence of acids, amides, nitriles or nitro functions which are not affected under these conditions.

    • Recent developments in synthetic chemistry and biological activities of pyrazole derivatives

      MUHAMMAD FAISAL AAMER SAEED SARWAT HUSSAIN PARSA DAR FAYAZ ALI LARIK

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      Pyrazole, a five-membered heterocycle containing two nitrogen atoms, is extensively found as a core framework in a huge library of heterocyclic compounds that envelops promising agro-chemical, fluorescent and biological potencies. Attributed to its several potential applications, there is a rise in the significance of designing novel pyrazoles, disclosing innovative routes for synthesizing pyrazoles, examining different potencies of pyrazoles, and seeking for potential applications of pyrazoles. This review consists of two parts. The firstpart provides an overview on the recent developments in synthetic approaches to pyrazoles, which is related to the new or advanced catalysts and other ‘environment-friendly’ procedures, including heterogeneous catalytic systems, ligand-free systems, ultrasound and microwave-assisted reactions. The second part focuses on the recently reported novel biological affinities of pyrazoles. This systematic review covers the published studies from 1990 to date. It is expected that this review will be helpful in future research and for new thoughts in thequest for rational designs for developing more promising pyrazoles

    • N-(5-acetyl-4-methylthiazol-2-yl)arylamide derivatives as multitarget- directed ligands: design, synthesis, biochemical evaluation and computational analysis

      RABAIL UJAN HAFIZ MOHAMMAD KASHIF MAHMOOD PERVAIZ ALI CHANNAR SYEDA ABIDA EJAZ SHOMAILA SAEED AAMER SAEED AMNA SAEED MAMOONA RAFIQ KASHIF ALI CHANNAR HAFIZ ABDUL BARI INDHER HAMMAD ISMAIL

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      In the present study, we are reporting the synthesis of a total eight derivatives of N-(5-acetyl-4-methylthiazol-2-yl) Arylamide derivatives (3a-h). The products obtained in good to excellent yield representsdrug-like molecules with a well-developed structure-activity relationship. All the synthesized compoundswere further subjected to chemical characterization (NMR, FTIR and elemental analysis) and further testedfor biological activities (antioxidant, antibacterial, antifungal and α-glucosidase). The anti-oxidant propertiesof compound 3h (IC50 ± SEM = 141.9 ± 1.12 μg/mL) were found maximum in comparison to the rest of thederivatives. The antibacterial results showed the compounds 3d and 3h as a significant bacterial inhibitor. Thesignificant fungicidal activity was observed by compound 3a with the zone of inhibition up to 24 mm whichin comparison with the results of positive control (Terbinafine). When the effect was observed on α-glucosidaseactivity, the highest enzyme inhibition activity was observed by 3h (IC50 ± SEM 134.4 ± 1.01 lμ/mL) followed by 3c (IC50 ± SEM = 157.3 ± 1.11 lμ/mL). The results were further supported by moleculardocking studies and the chemical stability of the derivatives was also performed by density functional theory(DFTs) calculations. The data revealed that most of the derivatives are multi-target ligands and can be used aslead molecules for the synthesis of derivatives for their further evaluation at molecular targets for thetreatment of specific diseases.

      Synopsis This article reports the synthesis of a total of eight derivatives of N-(5-acetyl-4-methylthiazol-2-yl) Arylamide derivatives. The products obtained in good to excellent yield represents drug-like molecules with a well-developed structure-activity relationship.

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