Research Journal of Pharmacy and Technology

Pankaj Kumar ¹, Jennifer Fernandes ¹, Abhishek Kumar ¹

Affiliations
1 Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, Nitte University, Paneer, Deralakatte-575018, Mangalore, Karnataka, IN

Abstract

In order to develop relatively small molecules as pharmacologically active molecules, a series of oxazolidinones having benzo thiazinen moieties and their derivatives were synthesized, and characterized by IR, ¹H NMR and Mass spectral studies. Oxazolidinones were prepared from R-glycidylbutarate and Para bromo aniline. Various substituted oxazolidinones benzo thiazinen were prepared by simple reflux in the presence of acetonitrile. Treatment of these oxazolidinones benzo thiazinen deravatives with methanesulfonyl gives its sulphonates derivatives on further treatment with sodium azide and tri phenyl phosphine in acetic anhydride to give its acetamide derivatives. All the newly synthesized compounds were evaluated for antibacterial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa.

Keywords

Oxazolidinones, Benzothiazinen, Antibacterial, Antifungal.

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K. Ishwar Bhat ¹, Abhishek Kumar ¹

Affiliations
1 Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, Nitte University, Paneer, Deralakatte-575018, Mangalore, Karnataka, IN

Abstract

A novel series pyrazoline derivatives have been developed as chemotherapeutic agents and have found wide clinical applications such as antibacterial, anticancer, antifungal and antitubercular agents. Chalcones are known to exhibit interesting pharmacological activities like anti-inflammatory, antileishmanial, antibacterial, antitumor, antimalarial and antitubercular activity. A series of pyrazoline derivatives [Substituted 1,5-diphenyl-3-(m-tolyl)-4,5-dihydro-1H-pyrazole] were prepared from chalcones by the reported method, characterized by IR, ¹H NMR and mass spectra. The synthesized compounds were evaluated for antitubercular and cytotoxic activity studies. Most of the compounds have exhibited promising antitubercular and cytotoxic activities.

Keywords

Chalcones, Pyrazolines, Antitubercular Activity, Cytotoxic Activity.

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K. Ishwar Bhat ¹, Abhishek Kumar ²

Affiliations
1 Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, Nitte University, Paneer, Deralakatte-575018, Mangalore, Karnataka, IN
2 Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences Paneer, Deralakatte, Mangalore 575018, Karnataka, IN

Abstract

A series of novel 4-(4-nitrophenyl)-6-phenyl substituted pyrimidine-2-thiol (PM₁-PM₆) have been synthesized by refluxing 1-(4-nitrophenyl)-3-phenyl substituted prop-2-en-1-one in presence of thiourea and glacial acetic acid. 1-(4-nitrophenyl)-3-phenyl substituted prop-2-en-1-one were prepared by condensing 4-nitroacetophenone with substituted benzaldehydes in presence of 20% NaOH as base. The structures of newly synthesized compounds were characterized by IR, ¹H NMR and mass spectroscopic studies. Newly synthesized compounds were screened for their anti-inflammatory and cytotoxic studies. Few of the compounds exhibited excellent anti-inflammatory compared to the standard drug diclofenac sodium. Some compounds have shown moderate cytotoxic activities.

Keywords

Chalcones, Pyrimidine, Cytotoxic Activity, Anti-Inflammatory Activity.

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Pankaj Kumar ¹, Abhishek Kumar ¹, Jean Sandra Pinto ¹, G. Akshata ¹, Bhashini ¹

Affiliations
1 Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, Nitte University, Paneer, Deralakatte-575018, Mangalore, Karnataka, IN

Abstract

The appearance to antimicrobial resistance to the antimicrobial agent has become a matter of high concern for health care professionals since last ten years. It will an effort to establish new pyrimidine derivatives as improved antimicrobial agent. In this particular series of novel substituted pyrimidine derivatives (PK1-PK5) were synthesized by simple condensation reaction between different substituted aldehydes and 3 acetyl -2,4-dimethyl pyrrole in presence of a strong ethanolic base to yield the pyrrolyl chalcones. The final synthesized pyrimidine derivative is prepared by the cyclization of pyrrolyl chalcones with urea in presence of KOH as base. The structures of the final synthesized compounds were characterized by IR, mass and ¹H NMR spectra. The synthesized compounds were screened for their antibacterial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosaby cup plate method. Most of the compounds exhibited promising antibacterial activity.

Keywords

3 Acetyl -2, 4-Dimethyl Pyrrole, Pyrrolyl Chalcones., Pyrimidine, Antibacterial.

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Pankaj Kumar ¹, Abhishek Kumar ¹, S. Deeksha ¹, G. Nireeksha ¹, Shalet D’souza ¹

Affiliations
1 Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, Nitte University, Paneer, Deralakatte-575018, Mangalore, Karnataka, IN

Abstract

The appearance to antimicrobial resistance to the antimicrobial agent has become a matter of high concern for health care professionals since last ten years. It will an effort to establish new phenylpropenone pyrrolyl; chalcones as improved antimicrobial agent. In this particular series of novel substituted phenylpropenone pyrrol (AP1-AP5) were synthesized by simple condensation reaction between different substituted aldehydes and 3 acetyl -2,4-dimethyl pyrrole in presence of a strong ethanolic base to yield the chalcones. The structures of the final synthesized compounds were characterized by IR, mass and ¹H NMR spectra. The synthesized compounds were screened for their antibacterial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa by cup plate method. Most of the compounds exhibited promising antibacterial activity.

Keywords

3 Acetyl -2,4-Dimethyl Pyrrole, Phenylpropenone Pyrrol., Antibacterial.

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K. Ishwar Bhat ¹, Ranee Kumari ¹, Abhishek kumar ¹, Pankaj Kumar ¹

Affiliations
1 Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, Mangalore-575018, Karnataka, IN

Abstract

The novel series of substituted flavanones were synthesized by reacting various 2-hydroxy chalcones. The intermediate 2-hydroxy chalcones were synthesized by Claisen-Schmidt condensation reaction. Flavanones were prepared by refluxing 2-hydroxychalcones in ethanol in presence of conc. H2SO4. All the synthesized compounds (RF1-RF9) were assigned on the basis of IR, 1H-NMR and MASS spectral data. These synthesized compounds were evaluated for their antioxidant activity by two different methods, DPPH and nitric oxide method. The compounds RF1, RF2, RF6, and RF7, RF8 showed very good activity when compared to the standard.

Keywords

2-Hydroxy Chalcones, Flavanones, Antioxidant, DPPH, Nitric Oxide.

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Abhishek Kumar ¹, Pankaj Kumar ¹, Shravya H ¹, Aravind Pai ²

Affiliations
1 Nitte (Deemed to be University), NGSM Institute of Pharmaceutical Sciences (NGSMIPS) 1Department of Pharmaceutical Chemistry, Mangalore,, IN
2 Manipal Academy of Higher Education, Manipal College of Pharmaceutical Sciences (MCOPS) 2Department of Pharmaceutical Chemistry, Manipal,, IN

Abstract

Major classes of plant metabolites that display a diversity of bioactivities are the Coumarin derivatives. At present, majority of the clinical anti-coagulant agents are coumarins, namely dicoumarol, acenocoumarol and warfarin. The victims who consume coumarins are antidotes should be kept under observation for unfavorable reaction. Phenprocoumon and warfarin, the Vitamin K adversaries, are the front-line oral anti-coagulants for prime and peripheral inhibition of cerebral embolism in victims with atrial fibrillation. Vitamin K adversaries have the capacity of reducing the risk of stroke exceptionally, but their usage is curbed due to some major disadvantages, such as the risk of intracranial and gastrointestinal bleeding, the requirement for systematic laboratory tests for therapy adjustment, interactions with a number of drugs and nutrients, and narrow therapeutic window. At present, latest oral anti-coagulants, namely direct factor Xa inhibitors (e.g., apixaban, rivaroxaban) and direct thrombin inhibitors (e.g., dabigatran), are evolved and tried out in clinical experiments. For the inhibition of cerebral embolism in victims with atrial fibrillation, Rivaroxaban and Dabigatran are currently validated. The role of blood clotting in challenging areas such as the therapeutic potentials of influence over coagulation and the pathogenesis of illness of uncertain etiology shows its biologic and pathologic importance. With growing tempo, acquiring from numerous disciplines – physical, biochemical, physiologic, biochemical, pathologic and clinical, progression has happened swiftly. Adequate proficiency has become handy for over 2 decades in order to grant comprehensive therapeutic requisition. Extensive usage of anti-coagulants and the possibility of their augmentation as vascular and thrombo-embolic sickness have been becoming important as serious medical problems, thereby making re-examination of ample guiding essentials needful.

Keywords

Coumarin, Anti-coagulant, Vitamin K, Blood clotting, Coagulation.

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Pankaj Kumar ¹, Abhishek Kumar ¹, Jean Sandra Pinto ¹, Sachin A. Kumbar ¹, Nanditha Bhat ¹, Prashant Nayak ²

Affiliations
1 Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, IN
2 Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, IN

Abstract

The α,β unsaturated ketone 3-(2,4-dimethyl-1H-pyrrol-3-yl)-1-phenylprop-2-en-1-onederivatives were treated with benzene-1,2-diamine to obtain 2-(2,4-dimethyl-1H-pyrrol-3-yl)-4-phenyl-2,3-dihydro-1H-benzo[b][1,4]diazepine derivatives. These synthesized compound were characterized by IR, 1H NMR, and mass spectroscopy. These synthesized molecules were evaluated for invitro antimicrobial activity. All The synthesized compounds, showed potent anti-microbial activity as compare to reference drug. In these study the synthesized were docked with Type IIA topoisomerases 2XCT using glide dock program and binding affinity were predicted for the synthesized compounds. The compound AP8 and AP9 have shown more active as per binding energy.

Keywords

Benzodiazepines, Antimicrobial, Docking, Topoisomerases, o-Phenylenediamine.

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