Kuldeep Singh Patel

Bio: Kuldeep Singh Patel is an academic researcher. The author has contributed to research in topics: Schiff base & Dry-powder inhaler. The author has an hindex of 3, co-authored 6 publications receiving 62 citations.

Synthesis of some coumarinyl chalcones and their antiproliferative activity against breast cancer cell lines

Abstract: A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R1, R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

Design, synthesis and biological evaluation of some novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones as antimalarial agents

Abstract: A novel series of 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones were designed, synthesized and screened for antiplasmodial activity. Eleven compounds of the series exhibited micromolar potency against chloroquine sensitive and chloroquine resistant strains. The most potent compound 4-hydroxy-3-(3-(4-nitrophenyl)acryloyl)-2H-chromen-2-one showed inhibitory potency (IC50) of 3.1 and 4 μg/ml against chloroquine sensitive and chloroquine resistant strains, respectively. A structure activity relationship study was performed by correlating the effect of substituents with the antimalarial activity of the title compounds. The novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones reported here should be good lead for further development of antimalarial agents that can overcome resistance.

Design, synthesis and biological evaluation of some schiff base ligand as antimalarial agents.

Abstract: Schiff base ligand AA-1, was derived from ethylenediamine and salicylaldehyde for the development of pharmaceuticals and it was followed by complexation of ligand with Ni (II) metal ion 2. The data of elemental analyses, molar conductance, 1H-NMR, IR, EI-MS was used for the corroboration of structural features of Schiff base AA1 and its complex AA2 along with the data obtained from single X-ray crystallography. The magnetic moment and UV spectral data was employed to proposed square planar geometry to the complex which was strongly supported by the Single-Crystal X-Ray diffraction studies. On the basis of conductivity data, it was suggested that the complex AA2 has non-electrolytic nature. The results of biological activities showed that the The most potent compound AA-5 showed inhibitory potency (IC50) of 2.1 mg/ml and 3mg/ml against chloroquine sensitive and chloroquine resistant strains respectively.The results of antibacterial activity showed that the ligand AA-1 exhibits moderately active while complex AA-2 exhibits good activity for chloroquine sanstive and resistant.

Design, in vitro evaluation and in vivo studies of novel delayed release tablets of pantoprazole

Abstract: In an effort to reduce production costs, a simple, direct compression delayed release formulation consisting of pantoprazole was investigated. Pantoprazole is a proton pump inhibitor belongs to group of benzimidazole. It is very efficient for the treatment of gastric and duodenum ulcers. Even in solid state pantoprazole is sensitive to heat, humidity, light and especially to substances containing an acidic group. For such types of drugs, enteric coating added to the formulation tends to avoid the stomach's acidic exposure, delivering them instead to a basic pH environment where they do not degrade, and give their desired action. Subcoating is desirable to protect the enteric coating. Opadry and Acryl-EZE systems have been utilized for subcoating and enteric coating respectively. Delayed-release tablets with good physical, mechanical and technological properties were obtained with use of different combinations of diluents, binders, superdisintegrants and lubricants. A comparative kinetic study of the present tablets and commercial tablets was established. The value for the similarity factor (f2 = 71.6) suggested that the dissolution profile of the present two delayed-release oral dosage forms are similar. Hixon–Crowell (erosion) kinetic profiles were achieved

Liposome: A Novel Aerosol Carrier of Doxophylline in Treatment of Chronic Asthma & Chronic Obstructive Pulmonary Disease

Abstract: The aim of the present research work is to develop liposomal dry powder inhaler of doxophylline by double hydration method to increase the entrapment efficiency of this hydrophilic drug. In this formulation, PVP coated mannitol and the mannitol were used as a cryoprotectant and a carrier respectively. Doxophylline, a new methylxanthine derivative, chemically designated as 7-(1,3-dixolan-2-yl-methyl) theophylline, is a more potent bronchodilator than theophylline, which is associated with a wide range of adverse effects accounting for poor compliance and high dropout rates. Powder inhaler formulation of the drug was characterized by angle of repose, compressibility index and in vitro aerosolization properties using Anderson cascade impactor including fine particle dose (212.9 + 7.2), fine particle fraction (21.69 + 1.21), % dispersibility (62.34 + 3.5) and % emission (72.1 + 0.13) at a flow rate of 28.3 lit/m for 10 seconds using 10 capsules for each determinations. The optimized formulations were subjected to stability studies at 2-8 o C, RT, and 40 o C for 3 months. The stability studies of LDPI were determined in terms of their visual appearance (surface characteristics and colour changes) and PDRE. The in vivo study was carried out by gamma scintigraphy and that showed better retention of doxophylline in liposomal formulation as compared to the controlled release formulation.

Ruthenium-catalyzed direct oxidative alkenylation of arenes through twofold C–H bond functionalization

Abstract: Significant progress has been accomplished in direct olefinations through twofold C–H bond functionalization of arenes and heteroarenes employing readily accessible, selective and relatively inexpensive ruthenium catalysts. Particularly, ruthenium(II) complexes have allowed challenging direct double C–H/C–H bond alkenylations of arenes with ample scope. These catalysts set the stage for step-economical C–H/C–H bond functionalization with electron-rich as well as electron-deficient arenes and heteroarenes, and, thereby, provide versatile access to diversely decorated styrenes.

Current Developments of Coumarin Compounds in Medicinal Chemistry

Abstract: Coumarin compounds represent an important type of naturally occurring and synthetic oxygen-containing heterocycles with typical benzopyrone framework. This type of special benzopyrone structure enables its derivatives readily interact with a diversity of enzymes and receptors in organisms through weak bond interactions, thereby exhibit wide potentiality as medicinal drugs. So far, some coumarin-based drugs such as anticoagulant and antineurodegenerative agents have been extensively used in clinic. Coumarin-containing supramolecular medicinal agents as a new increasing expansion of supramolecular chemistry in pharmaceutical science have also been actively investigated in recent years. Coumarin-derived artificial ion receptors, fluorescent probes and biological stains are growing quickly and have a variety of potential applications in monitoring timely enzyme activity, complex biological events as well as accurate pharmacological and pharmacokinetic properties. This review provides a systematic summary and insight of the whole range of medicinal chemistry in the current developments of coumarin compounds as anticoagulant, antineurodegenerative, anticancer, antioxidative, antibacterial, antifungal, antiviral, antiparasitic, antiinflammatory and analgesic, antidiabetic, antidepressive and other bioactive agents as well as supramolecular medicinal drugs, diagnostic agents and pathologic probes, and biological stains. Some rational design strategies, structure-activity relationships and action mechanisms are discussed. The perspectives of the future development of coumarinbased medicinal chemistry are also presented.

Recent advances in positional-selective alkenylations: removable guidance for twofold C–H activation

Abstract: The transition metal-catalyzed transformation of otherwise inert C–H bonds into substituted alkenes offers a versatile tool for the synthesis of value added olefinic molecules. Recent developments in the directing group assisted C–H activation approach ensured high levels of positional selectivity. A vast number of coordinating groups have been utilized in directed C–H alkenylation, which are often not removable after the desired transformation. However, the concept of easily removable or traceless directing group strategy overcomes this limitation and enables site-selective C–H alkenylation of relevance to academia and the practitioners in industry. Various easily removable or transformable directing groups utilized in the transition metal-catalyzed oxidative C–H alkenylations are discussed in this review until February 2017.

Advances in Chalcones with Anticancer Activities

Abstract: Chalcones are naturally occurring compounds exhibiting broad spectrum biological activities including anticancer activity through multiple mechanisms. Literature on anticancer chalcones highlights the employment of three pronged strategies, namely; structural manipulation of both aryl rings, replacement of aryl rings with heteroaryl scaffolds, molecular hybridization through conjugation with other pharmacologically interesting scaffolds for enhancement of anticancer properties. Methoxy substitutions on both the aryl rings (A and B) of the chalcones, depending upon their positions in the aryl rings appear to influence anticancer and other activities. Similarly, heterocyclic rings either as ring A or B in chalcones, also influence the anticancer activity shown by this class of compounds. Hybrid chalcones formulated by chemically linking chalcones to other prominent anticancer scaffolds such as pyrrol[2,1-c][1,4]benzodiazepines, benzothiazoles, imidazolones have demonstrated synergistic or additive pharmacological activities. The successful application of these three pronged strategies for discovering novel anticancer agents based on chalcone scaffold has resulted in many novel and chemically diverse chalcones with potential therapeutic application for many types of cancer. This review summarizes the concerted efforts expended on the design and development of anticancer chalcones recorded in recent literature and also provides an overview of the patents published in this area between 2007 and 2014 (WO2013022951, WO201201745 & US2012029489).