Background: Hypogonadism is the condition resulting from the failure of testes to produce physiol... more Background: Hypogonadism is the condition resulting from the failure of testes to produce physiological levels of testosterone due to disruption of one or more levels of the hypothalamic-pituitary-gonadal axis. It strongly affects the health of men especially bone strength, muscle mass, hypertension, hyperlipidaemia, diabetes, and asthma. Methods: In a retrospective study, Testosterone and Luteinizing hormone levels were measured in adult males. The subjects were classified as hypogonadal using a new classification system. Results: The subjects with low testosterone levels turned out to be 41%. Secondary hypogonadism was most prevalent amongst the adult males. Compensated hypogonadism was also observed in a large group. Discussion: With this study it became easier for us to classify the subjects as Eugonadal or hypogonadal and to determine the class of hypogonadism as Primary, Secondary or Compensated hypogonadism. As maintaining normal testosterone levels is important for overall h...
A novel serie of escitalopram triazoles (60-88) and a tetrazole (89) have been synthesized and su... more A novel serie of escitalopram triazoles (60-88) and a tetrazole (89) have been synthesized and subjected to a study to establish the inhibitory potential of these compounds toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Some selectivity in inhibition has been observed. The 4-chlorophenyl- (75, IC50, 6.71±0.25μM) and 2-methylphenyl- (70, IC50, 9.52±0.23μM) escitalopram triazole derivatives depicted high AChE inhibition, while 2-fluorophenyl- (76, IC50=4.52±0.17μM) and 4-fluorophenyl- (78, IC50=5.31±0.43μM) have found to be excellent BChE inhibitors. It has also been observed that ortho, meta and para substituted electron donating groups increase the inhibition, while electron withdrawing groups reduce the inhibition. Docking analyses of inhibitors with AChE have depicted the binding energies for 70 and 75 as ΔGbind -6.42 and -6.93kcal/mol, respectively, while ligands 76 and 78 have shown the binding affinity ΔGbind -9.04 and -8.51kcal/mol, respectively, for BChE.
A series of coumarins have been prepared by the Pechmann reaction of different phenols with ethyl... more A series of coumarins have been prepared by the Pechmann reaction of different phenols with ethyl acetoactate as well as malic acid using catalytic amount of sulfuric acid under microwave irradiation for few seconds. Keywords: Pechman reaction, Coumarins, Microwave irradiation
Coumarin and coumarin-3-acetic acid derivatives were synthesized by reacting phenols with malic a... more Coumarin and coumarin-3-acetic acid derivatives were synthesized by reacting phenols with malic acid, ethyl acetoacetate and ethyl acetylsuccinate in appropriate reaction conditions. All synthesized compounds were subjected to test for their antimicrobial activities against variety of gram positive (Bacillus subtilis, Staphylococcus aureus) and gram negative bacterial stains (Shigella sonnei, Escherichia coli) by agar dilution method. Several of them exhibited appreciable good antibacterial activity against the different strains of gram positive and gram negative bacteria. These findings suggest a great potential of these compounds for screening and use as antibacterial agents for further studies with a battery of bacteria.
Background: Indazoleacetic acids and their pharmaceutically acceptable salts have been claimed to... more Background: Indazoleacetic acids and their pharmaceutically acceptable salts have been claimed to be useful as anti-inflammatory, analgesic and antipyretic agents. They are active in the treatment of respiratory diseases such as asthma, bronchitis, allergies and obstructive pulmonary diseases. Objectives: We report herein a feasible study concerned about the design, synthesis, structure and in vitro antimicrobial activity of 3-arylindazole-1-acetic acids derivatives. Series of compounds were synthesized by alkylation of 3-arylindazoles. Method: Synthesized compounds were subjected to study the effect on microbial growth in vitro. All synthesized compounds were found to exhibit antibacterial activities against a range of grampositive (Bacillus subtilis, Staphylococcus aureus) and gram-negative bacteria (Shigella sonnei, Escherichia coli) by broth dilution method. Results: The synthesized compounds exhibited antibacterial activities comparable to fluoroquinolones and some compounds ex...
Background: Hypogonadism is the condition resulting from the failure of testes to produce physiol... more Background: Hypogonadism is the condition resulting from the failure of testes to produce physiological levels of testosterone due to disruption of one or more levels of the hypothalamic-pituitary-gonadal axis. It strongly affects the health of men especially bone strength, muscle mass, hypertension, hyperlipidaemia, diabetes, and asthma. Methods: In a retrospective study, Testosterone and Luteinizing hormone levels were measured in adult males. The subjects were classified as hypogonadal using a new classification system. Results: The subjects with low testosterone levels turned out to be 41%. Secondary hypogonadism was most prevalent amongst the adult males. Compensated hypogonadism was also observed in a large group. Discussion: With this study it became easier for us to classify the subjects as Eugonadal or hypogonadal and to determine the class of hypogonadism as Primary, Secondary or Compensated hypogonadism. As maintaining normal testosterone levels is important for overall h...
A novel serie of escitalopram triazoles (60-88) and a tetrazole (89) have been synthesized and su... more A novel serie of escitalopram triazoles (60-88) and a tetrazole (89) have been synthesized and subjected to a study to establish the inhibitory potential of these compounds toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Some selectivity in inhibition has been observed. The 4-chlorophenyl- (75, IC50, 6.71±0.25μM) and 2-methylphenyl- (70, IC50, 9.52±0.23μM) escitalopram triazole derivatives depicted high AChE inhibition, while 2-fluorophenyl- (76, IC50=4.52±0.17μM) and 4-fluorophenyl- (78, IC50=5.31±0.43μM) have found to be excellent BChE inhibitors. It has also been observed that ortho, meta and para substituted electron donating groups increase the inhibition, while electron withdrawing groups reduce the inhibition. Docking analyses of inhibitors with AChE have depicted the binding energies for 70 and 75 as ΔGbind -6.42 and -6.93kcal/mol, respectively, while ligands 76 and 78 have shown the binding affinity ΔGbind -9.04 and -8.51kcal/mol, respectively, for BChE.
A series of coumarins have been prepared by the Pechmann reaction of different phenols with ethyl... more A series of coumarins have been prepared by the Pechmann reaction of different phenols with ethyl acetoactate as well as malic acid using catalytic amount of sulfuric acid under microwave irradiation for few seconds. Keywords: Pechman reaction, Coumarins, Microwave irradiation
Coumarin and coumarin-3-acetic acid derivatives were synthesized by reacting phenols with malic a... more Coumarin and coumarin-3-acetic acid derivatives were synthesized by reacting phenols with malic acid, ethyl acetoacetate and ethyl acetylsuccinate in appropriate reaction conditions. All synthesized compounds were subjected to test for their antimicrobial activities against variety of gram positive (Bacillus subtilis, Staphylococcus aureus) and gram negative bacterial stains (Shigella sonnei, Escherichia coli) by agar dilution method. Several of them exhibited appreciable good antibacterial activity against the different strains of gram positive and gram negative bacteria. These findings suggest a great potential of these compounds for screening and use as antibacterial agents for further studies with a battery of bacteria.
Background: Indazoleacetic acids and their pharmaceutically acceptable salts have been claimed to... more Background: Indazoleacetic acids and their pharmaceutically acceptable salts have been claimed to be useful as anti-inflammatory, analgesic and antipyretic agents. They are active in the treatment of respiratory diseases such as asthma, bronchitis, allergies and obstructive pulmonary diseases. Objectives: We report herein a feasible study concerned about the design, synthesis, structure and in vitro antimicrobial activity of 3-arylindazole-1-acetic acids derivatives. Series of compounds were synthesized by alkylation of 3-arylindazoles. Method: Synthesized compounds were subjected to study the effect on microbial growth in vitro. All synthesized compounds were found to exhibit antibacterial activities against a range of grampositive (Bacillus subtilis, Staphylococcus aureus) and gram-negative bacteria (Shigella sonnei, Escherichia coli) by broth dilution method. Results: The synthesized compounds exhibited antibacterial activities comparable to fluoroquinolones and some compounds ex...
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