PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agent

SYNTHESIS AND ANTI-INFLAMMATORY ACTIVITY OF SOME NOVEL 1,5 BENZODIAZEPINE DERIVATIVES

ABSTRACTObjective: The objective of the study is to synthesize some novel 1,5-benzodiazepine derivatives from chalcones. The structures of the newlysynthesized compounds were characterized by elemental analysis, infrared, H nuclear magnetic resonance, and mass spectroscopic studies. All titledcompounds were screened for their anti-inflammatory activity.1Methods: In this study, a series of novel 2-(substituted phenyl)-3-styryl-2,3-dihydro-1H-benzo [b] [1,4] diazepine (1-12) has been synthesizedfrom 1,5-(disubstituted phenyl)-2,4-pentadien-1-one (1a-12a). 1,5-(disubstituted phenyl)-2,4-pentadien-1-one was prepared by condensingcinnamaldehyde with various aromatic ketones in the presence of 20% NaOH as base. Different 1,5-(disubstituted phenyl)-2,4-pentadien-1-one oncyclisation with o-phenylene diamine in the presence of NaOH as base resulted in 2-(substituted phenyl)-3-styryl-2,3-dihydro-1H-benzo [b] [1,4]diazepine derivatives. The final synthesized benzodiazepine derivatives were screened for their anti-inflammatory activity using carrageenaninducedratpawedema method.Results: The compounds 4, 5, 7, 9, 10, 11, and 12 containing 4-nitrophenyl, 4-chlorophenyl, 3-nitro phenyl, 4-fluorophenyl, 4-bromophenyl, and3-chlorophenyl benzodiazepine derivatives exhibited significant anti-inflammatory activity compared with the standard diclofenac sodium Thepresence of electron withdrawing groups such as nitro, chloro, fluoro, and bromo resulted in increased anti-inflammatory activity.Conclusion: This study reports the successful synthesis of 1,5-benzodiazepine derivatives with moderate yields and most of the synthesizedcompounds showed significant anti-inflammatory activity.Keywords: Chalcones, 1,5-benzodiazepines, Anti-inflammatory activity

PYRAZOLINES AS POTENT ANTITUBERCULAR AND CYTOTOXIC AGENTS

Objective: Pyrazolines are known to exhibit different biological and pharmacological properties such as anticancer, antibacterial, antifungal and antitubercular activities. Chalcones with an enone group between two aromatic rings exhibit remarkable pharmacological activities such as antiinflammatory, antibacterial, antitumor, antifungal, and antimalarial activity. A series of pyrazolines from chalcones have been synthesized and evaluated for antitubercular and cytotoxic activity studies.Methods: Chalcones [3-substituted phenyl-1-(p-tolyl)prop-2-en-1-one] were synthesized from various substituted aldehydes and 4-methyl acetophenone and cyclized into pyrazolines [5-substituted phenyl-3-(p-tolyl)-4,5-dihydro-1H-pyrazole] using hydrazine hydrate. Antitubercular and cytotoxic activity studies were carried out.Results: Antitubercular and cytotoxic activity studies of synthesized pyrazoline revealed that some compounds have showed promising activity.Conclusion: The observed results proved that pyrazolines are found to be interesting lead molecules for further synthesis as antitubercular and cytotoxic agents

SYNTHESIS, IN SILICO PHYSICOCHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES OF SOME PYRAZOLINE DERIVATIVES

Objectives: Nitrogen containing heterocyclic compounds plays an important role in medicinal chemistry. Among them, five-membered ring pyrazolines have found to possess many biological and pharmacological activities like anticancer, antitubercular, antimicrobial, anti-inflammatory etc. Objective is to determine the physicochemical and drug like properties of the synthesized pyrazolines by in silico methods and to screen their antidiabetic and antioxidant activities.Methods: Chalcones were synthesized from naphthaldehydes by condensing with various substituted acetophenones in ethanol and cyclized into pyrazolines using semicarbazides/thiosemicarbazides by conventional and microwave oven synthesis. The physicochemical and drug like properties were determined by using computational tools. Antidiabetic activity was evaluated by alpha amylase inhibition assay method. Antioxidant activity studies were done by DPPH and nitric oxide method.Results: Pyrazolines were synthesized from chalcones. Microwave irradiated synthesis of chalcone was carried out to get higher yield with less reaction time period as compared to conventional method. The synthesized pyrazolines produces yield around 68% (conventional) and 85% (microwave). In silico studies showed considerable values satisfying all the parameters of physicochemical and Lipinski's rule of five properties.  Among the compounds tested for antidiabetic and antioxidant studies, some showed promising activity.Conclusion: Physiochemical and drug like properties revealed that these compounds have good bioavailability and druglikeness properties. So these compounds are found to be interesting lead molecules for further synthesis as antidiabetic and antioxidant agents.Keywords: Chalcones, pyrazolines, in silico physicochemical properties, biological activities.Â

Synthesis and pharmacological study of some novel thiazolidinones

A series of some novel thiazolidinones derivatives were synthesized and evaluated for their pharmacological activities. Thiazolidinones were synthesized from p-nitro aniline in four steps. First Schiff’s bases (V1- 8) were prepared by reacting the N4 -(4-nitrophenyl) thiazole-2,4-diamine (3) of p-nitro aniline derivatives with different aromatic aldehydes. Cyclocondensation of the Schiff’s bases with thioglycolic acid in presence of anhydrous zinc chloride resulted in the formation of the corresponding thiazolidinone (VD1-8) analogues. The structures of the newly synthesized compounds have been established on the basis of their spectral data. The synthesized selected compounds were evaluated for their anti-inflammatory and analgesic activity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Synthesis and pharmacological study of some novel thiazolidinones

A series of some novel thiazolidinones derivatives were synthesized and evaluated for their pharmacological activities. Thiazolidinones were synthesized from p-nitro aniline in four steps. First Schiff’s bases (V1- 8) were prepared by reacting the N4 -(4-nitrophenyl) thiazole-2,4-diamine (3) of p-nitro aniline derivatives with different aromatic aldehydes. Cyclocondensation of the Schiff’s bases with thioglycolic acid in presence of anhydrous zinc chloride resulted in the formation of the corresponding thiazolidinone (VD1-8) analogues. The structures of the newly synthesized compounds have been established on the basis of their spectral data. The synthesized selected compounds were evaluated for their anti-inflammatory and analgesic activity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Synthesis and pharmacological study of some novel thiazolidinones

A series of some novel thiazolidinones derivatives were synthesized and evaluated for their pharmacological activities. Thiazolidinones were synthesized from p-nitro aniline in four steps. First Schiff’s bases (V1- 8) were prepared by reacting the N4 -(4-nitrophenyl) thiazole-2,4-diamine (3) of p-nitro aniline derivatives with different aromatic aldehydes. Cyclocondensation of the Schiff’s bases with thioglycolic acid in presence of anhydrous zinc chloride resulted in the formation of the corresponding thiazolidinone (VD1-8) analogues. The structures of the newly synthesized compounds have been established on the basis of their spectral data. The synthesized selected compounds were evaluated for their anti-inflammatory and analgesic activity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Long-term Farming System Comparison Trial in India

Background: Developing sustainable farming system on large scale is very important for sustainable development of global agriculture. Scientific information about organic vs. conventional agriculture in the tropics is sparse

CYTOTOXIC AND ANTIMICROBIAL STUDIES OF SOME SUBSTITUTED PYRAZOLINE DERIVATIVES DERIVED FROM ACETYL HYDRAZINES

Objectives: Several pyrazoline derivatives have been developed as chemotherapeutic agents and have found wide clinical applications such as anticancer [4], antibacterial [4], antifungal [4], antitubercular [4] agents. Chalcones with an enone system between two aromatic rings exhibit interesting pharmacological activities such as anti-inflammatory, antileishmanial, antibacterial, antifungal, antitumour, antimalarial and anti-tubercular activity. To synthesize series of pyrazolines from chalcones and to evaluate the antimicrobial activities of the synthesized compounds.Methods: Chalcones were synthesized from various substituted aldehydes condensing with various substituted acetophenones and cyclized into Pyrazolines using aryloxy acetyl hydrazines. Antimicrobial and Antitubercular activity studies were carried out.Results: Antimicrobial studies for the synthesized Pyrazolines revealed that some compounds have showed promising activity.Conclusions: The above results proved that Pyrazolines are found to be interesting lead molecules for further synthesis as Antimicrobial and Antitubercular agents.Keywords: Chalcones, Pyrazolines, Antimicrobial Activity,  Antitubercular Activity