Novel Synthesis and Pharmaceutical Impurities of AntiHypertensive Drugs: A Review

Kumar, A. S. Kiran; Kumar, Rajnish; Saini, Sweety

doi:10.20902/ijctr.2019.130203

Cited by 3 publications

(3 citation statements)

References 12 publications

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“…Conventional methods to produce synthetic nHA are proposed to be the precipitation technique, sol-gel method, hydrothermal synthesis, multiple emulsion method, biomimetic deposition, and electrodeposition methods [36]. Novel approaches such as microwave synthesis and atomiclayer deposition methods have been also proposed, providing the production of nHA with desirable structure and properties [37 -39].…”

Section: Nano-hydroxyapatite Potential As a Phosphorus Fertilizermentioning

confidence: 99%

An Evaluation of Phosphogypsum (PG) -Derived Nanohydroxyapatite (HAP) Synthesis Methods and Waste Management as a Phosphorus Source in the Agricultural Industry

Avşar¹,

Gezerman²

2023

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As a raw material, phosphorus availability in agriculture has been a critical concern in terms of phosphate rock consumption related to a price-dependent supply-demand chain. Novel approaches have been proposed for alternative phosphorus sources in agricultural applications. Although nano-hydroxyapatite (nHA) is a commonly used bioceramic material, its utilization as an alternative phosphorus fertilizer is an emerging field. Phosphogypsum (PG), a by-product of wet process phosphoric acid production, is a promising raw material for nHA production. With an approximate 300 Mton annual accumulation rate of PG puts pressure on the research for introducing alternative strategies for the resource utilization of legacy PG piles in an environment-friendly and cost-efficient manner. Valorization of PG as the calcium and phosphorus precursor in nHA production would both provide an efficient waste management strategy and low-cost raw material. This study gives a brief review of the various synthesis routes on PG-derived nHA and criticizes nHA utilization as a phosphorus fertilizer.

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Section: Nano-hydroxyapatite Potential As a Phosphorus Fertilizermentioning

confidence: 99%

An Evaluation of Phosphogypsum (PG) -Derived Nanohydroxyapatite (HAP) Synthesis Methods and Waste Management as a Phosphorus Source in the Agricultural Industry

Avşar¹,

Gezerman²

2023

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“…Scheme 2 includes subsequently reported important synthetic approaches to synthesize baclofen. For example, Kumar et al 9 recently designed a novel route A of synthesis starting from pchlorobenzaldehyde 2 which on treatment with sodium cyanide, gave cyanohydrin 12 which was further oxidized by using pyridinium chlorochromate to form p-chlorobenzoyl cyanide 13. Compound 13 was further treated with triphenylphosphine acetate to give compound 14, which was further reduced by using Raney nickel to get 1.…”

Section: Scheme 1: Commercial Route Of Synthesismentioning

confidence: 99%

Novel Synthetic Industrial Approach for Efficient Synthesis of Baclofen through C–C Bond Formation

Jagtap,

Raut,

Qureshi

et al. 2023

Synlett

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Baclofen is an active pharmaceutical ingredient (API) used for the treatment of muscle spasticity. We describe our efforts to develop a novel synthetic approach via C-C bond formation and the cost-effective process of Baclofen. The synthesis involved a two-step approach via C-C bond formation using the extensively and commercially available starting material 4-chlorobenzyl cyanide and chloroacetic acid as a reagent in an aprotic solvent, followed by reduction of the nitrile functional group. The synthetic route of baclofen has been demonstrated to be commercially viable, cost-effective, and environmentally friendly. Execution of the developed process led to the isolation of (+) baclofen in an overall yield of 60% at a multi-kilogram scale > 99.5 % HPLC purity. This article also discusses the cost-effectiveness of the process, impurity profiling, material quality, and polymorphic form. Key words Baclofen, polymorph, C- alkylation, Nitrile reduction.

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“…Heterocyclic compounds have been found to have an affinity towards a diverse range of biotargets across several fields [27][28][29]. Both agribusiness and pharmacological research have derived advantages from the utilization of these scaffolds [30].…”

Section: Introductionmentioning

confidence: 99%

The Synthesis, In Vitro Bio-Evaluation, and In Silico Molecular Docking Studies of Pyrazoline–Thiazole Hybrid Analogues as Promising Anti-α-Glucosidase and Anti-Urease Agents

Khan,

Hussain

et al. 2023

Pharmaceuticals

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In the present work, a concise library of benzothiazole-derived pyrazoline-based thiazole (1–17) was designed and synthesized by employing a multistep reaction strategy. The newly synthesized compounds were screened for their α-glucosidase and urease inhibitory activities. The scaffolds (1–17) were characterized using a combination of several spectroscopic techniques, including FT-IR, 1H-NMR, 13C-NMR, and EI-MS. The majority of the synthesized compounds demonstrated a notable potency against α-glucosidase and urease enzymes. These analogues disclosed varying degrees of α-glucosidase and urease inhibitory activities, with their IC50 values ranging from 2.50 to 17.50 μM (α-glucosidase) and 14.30 to 41.50 (urease). Compounds 6, 7, 14, and 12, with IC50 values of 2.50, 3.20, 3.40, and 3.50 μM as compared to standard acarbose (IC50 = 5.30 µM), while the same compounds showed 14.30, 19.20, 21.80, and 22.30 comparable with thiourea (IC50 = 31.40 μM), respectively, showed excellent inhibitory activity. The structure−activity relationship revealed that the size and electron-donating or electron-withdrawing effects of substituents influenced the enzymatic activities such as α-glucosidase and urease. Compound 6 was a dual potent inhibitor against α-glucosidase and urease due to the presence of -CF3 electron-withdrawing functionality on the phenyl ring. To the best of our knowledge, these synthetic compounds were found to be the most potent dual inhibitors of α-glucosidase and urease with minimum IC50 values. Moreover, in silico studies on most active compounds, i.e., 6, 7, 14, and 12, were also performed to understand the binding interaction of most active compounds with active sites of α-glucosidase and urease enzymes.

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Novel Synthesis and Pharmaceutical Impurities of AntiHypertensive Drugs: A Review

Cited by 3 publications

References 12 publications

An Evaluation of Phosphogypsum (PG) -Derived Nanohydroxyapatite (HAP) Synthesis Methods and Waste Management as a Phosphorus Source in the Agricultural Industry

An Evaluation of Phosphogypsum (PG) -Derived Nanohydroxyapatite (HAP) Synthesis Methods and Waste Management as a Phosphorus Source in the Agricultural Industry

Novel Synthetic Industrial Approach for Efficient Synthesis of Baclofen through C–C Bond Formation

The Synthesis, In Vitro Bio-Evaluation, and In Silico Molecular Docking Studies of Pyrazoline–Thiazole Hybrid Analogues as Promising Anti-α-Glucosidase and Anti-Urease Agents

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