IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
First View
1

A COMPREHENSIVE REVIEW ON ANTHELMINTIC ACTIVITY OF SOME MEDICINAL PLANTS

Dnyaneshwari Bade*, Vishal Rasve
SAJVPM’S, College of Pharmaceutical Sciences and Research Center, Kada Ashti, Beed MH-414202.

Indian medicinal herbs have long been recognized for their healing properties. The oldest medical system, Ayurveda, advises using treatments based mostly on medicinal herbs to address a wide range of human and animal ailments. The average person can afford and get herbal therapies. The powerful source of many pharmacological activities was medicinal plants. Due to the ability of the plants and its chemical to treat a disease that results in significant financial loss and decreased animal production for livestock owners, one of the plants with anthelmintic action has attracted a lot of interest. Although less effective at curing diseases, crude drugs are generally side effect free. Various in vitro and in vivo techniques have been used to examine medicinal plants for this activity. The crude compounds made from plants are less effective in treating parasite disorders but they are generally free from adverse effects. In undeveloped nations, helminthiasis is historically treated with a wide variety of medicinal plants. In order to treat parasitic infections, plant-derived medications are receiving a lot of attention.This review present the herbal medicines or medicinal plants which are have number of benefits and used as anthelmintic. Ethnobotanical survey, in India the belief that their evaluation will accelerate the discovery of new effective therapeutic agents as anthelmintic.



2

“SYNTHESIS AND MOLECULAR DOCKING STUDIES OF NOVEL PYRROLYL BENZAIMIDAZOLE DERIVATIVES AS ANTICONVULSANT AGENTS.

Channabasappa S. Hallikeri*, DaneshwariKadakol, Shrinivas D. Joshi, Venkatarao H. Kulkarni.
Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical chemistry, S.E.T’s College of Pharmacy, Sangolli Rayanna Nagar, Dharwad 580 002, India.

The various novel pyrrolyl benzamide derivatives were synthesized and molecular docking studies were carried out further few compounds evaluated for anticonvulsant activity against MES and PTZ induced convulsions. Purity of the newly synthesized compounds confirmed by using TLC and structures were confirmed by using IR, NMR, 13C and Mass spectra. Appropriate o-phenylene diamine(1) is treated with para amino-2-chloro benzoic acid (2) in
ethanol and reaction mixture made alkaline by adding 10% sodium hydroxide solution to form substituted benzimidazole-2-chloro aniline(3a-e) which is further stirred with 4-pyrrole-1-yl-benzoic acid(4) and 4-(2, 5-dimethyl-1yl)-benzoic acid (5) by dissolving in a dry DMF in presence of HBTU and DIEA yielded the corresponding final compounds(6a-e) and (7a-e). and o-phenylene diamine (1) is treated with para-amino benzoic acid (8) in ethanol and reaction made alkaline by adding 10% sodium hydroxide solution to form substituted benzimidazole aniline (9a-e) which is further stirred with4-(2, 5-dimethyl-1yl)-benzoic acid (5) by dissolving in a dry DMF in presence of HBTU and DIEA yielded the corresponding final compounds(10a-e). Docking study was performed by Surflex-Dock program that is interfaced with Sybyl-X 2.0. Compounds 7e and 10d showed excellent consensus scoreat 7.17 & 7.26 respectively. Docking study reveals that all the compounds have showed very good docking score against the enzyme. The few newly synthesized compounds were screened for their anticonvulsant activity. Compounds 10a (9.8+0.34) and 10e (11.83+0.44) showed significantly decrease in hind limb extension against MES induced convulsions. Compound 6e (140+2.02) and 10e (160+2) showed protection against PTZ induced convulsions. Simultaneously activity is compared with control and standard group. The newly synthesized novel series of pyrrolyl benzamide derivatives may be developed into potential class of anticonvulsant agents in future.



3

NANOSPONGES: A NOVEL APPROACH OF DRUG DELIVERY SYSTEM: REVIEW

Jijimol T*, Dr. Ann Rose Augusthy, Suhana, Dr. Vipin K V

Department of Pharmaceutics, College of Pharmaceutical Sciences, Government Medical College Kannur, Kerala University of Health Science, Kerala, India.

Recent developments in nanotechnology have paved the way for the creation of novel biomaterials based on the nanoscale with numerous potential uses in the area of nanomedicine. The main issue that medical experts are dealing with is targeted drug delivery to specified areas. These issues could be solved by the newly created colloidal system known as nanosponge. Nanosponges are a brand-new type of colloidal structures made of hypercross-linked polymers and composed of solid nanoparticles with colloidal diameters and nanosized voids. Nanosponges are tiny sponges that are roughly the size of a virus and may hold a range of medications. These tiny sponges can move through the body until they reach the intended target site, where they adhere to the skin and start to release the drug in a controlled and predictable manner. This review attempts to elaborate the advantages, synthesis, characterisation, and applications of nanosponges.




4

“SYNTHESIS AND CHARACTERIZATION OF NEW PYRROLYL OXADIAZOLE AS ANTIMICROBIAL AGENTS”

Vidya Kamatar, Prashanth K. U, Channabasappa S. Hallikeri*, Shrinivas D. Joshi

Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical chemistry, S.E.T’s College of Pharmacy, SangolliRayanna Nagar, Dharwad 580 002, India.

The various novel nitrogen containing heterocyclic compounds were synthesized and are screened for antibacterial and antitubercular activities, purity of newly synthesized compounds confirmed by using TLC and structures for the same compounds were confirmed by using IR, NMR, 13C and Mass spectrum. Pyrrole ring was constructed by reacting benzocaine with 2, 5-dimethoxytetrahydrofuran in presence of glacial acetic acid to obtain ethyl 4-pyrrol-1-ylbenzoate (2) in good yield. Conversion of ethyl 4-pyrrol-1-ylbenzoate (2) into 4-pyrrol-1-yl-benzoic acid hydrazide (3), which was achieved by refluxing ethyl 4-pyrrol-1-ylbenzoate (2) with hydrazine hydrate in ethanol. Then this 4-pyrrol-1-yl-benzoic acid hydrazide (3) treated with appropriate benzaldehyde in presence of TCCA and ethanol to yield compound substituted 2-(4-(1H-pyrrol-1-yl)phenyl)-5-phenyl-1,3,4-oxadiazole 04(a-f).Structures of newly synthesized compounds were confirmed on the basis of physico-chemical and spectral data (IR, 1H &13C-NMR, Mass spectra). All the synthesized compounds were screened for anti-tubercular activity using Microplate Almar Blue Assay (MABA) method. Compounds showed anti-tubercular activity at MIC values between 50 to 3.12 µg/ml when compared with standard drugs Pyrazinamide (3.125 µg/ml) and Streptomycin (6.25 µg/ml).Newly synthesised compounds were also screened for antibacterial activity using broth micro dilution assay method. Compounds showed antibacterial activity at MIC values between 25 to 0.8 µg/ml when compared with standard drugs Ciprofloxacin and Norfloxacin.




5

SYNTHESIS CHARACTERIZATION OFNOVEL SERIES OF PYRROLYL PYRANOPYRAZOLE AS ANTIMICROBIAL AGENTS

Tabasum Killedar, Shweta Medleri, Channabasappa S. Hallikeri*, Shrinivas D. Joshi

Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical chemistry, S.E.T’s College of Pharmacy, SangolliRayanna Nagar, Dharwad 580 002, India.

New series of pyrrolylpyranopyrazole were synthesized by reacting with (one pot synthesis) ethyl acetoacetate in aqueous ethanol (1), hydrazine hydrate (2), substituted aldehydes (3a-g), malononitrile (4) and triethylamine’s base stirring for 5hr the solid precipitate was obtained, it has been filtered and washed with cold water to give 6-amino-3-methyl-4-substituted phenyl-1,3a,4,7a-tetrahydropyrano [2,3-c] pyrazole-5-carbonitrile (5a-g). Further it is reacted with 4- pyrrol-1-yl benzoic acid (6) with substituted pyranopyrazoline presence of HBTU and DIEA which resulting in formation of substituted N-5-cyano-3-methyl-4-substituted phenyl 1,3a,47a-tetrahydropyrano [2,3-c] pyrazol-6-yl)-4-(1H-pyrrol-1-yl) benzamides (7a-g) was obtained. All newly synthesized compounds were confirmed by TLC and melting point. The structure of the all newly synthesized compounds were confirmed by spectral study such as IR, 1H NMR, 13C NMR and Mass spectroscopy. The newly synthesized compounds were screened for their antibacterial and antitubercular activities. Compounds exhibited antitubercular activity in the range of 1.6 to 25 µg/ml (MIC). Compounds showed antibacterial activity in the range of 0.8 to 100 µg/ml (MIC). It was indeed very much encouraging to note that most of the compounds have shown better and significant antibacterial and antitubercular activities.




6

INSIGHTS INTO RESISTANCE AND SENSITIVITY PATTERNS OF VARIOUS UROPATHOGENS AND THEIR MANAGEMENT IN URINARY TRACT INFECTIONS

Jakka Jagadeesh Kumar*, Chinnavaidi Vidhya Sree, Kumbam Reshma, Apoorva Bachu, Dr. Amatul Ali Sameera

Sree Dattha Institute of Pharmacy, Sheriguda, Ibrahimpatnam, R.R-District, Telangana 501510.

AIM AND OBJECTIVE: Theaim of the study was to Insights into resistance and sensitivity patterns of various uropathogens and their management in urinary tract infections RESULTS: The study included 221 UTI patients reports revealed that males accounted for 50.2% and females 49.7%, respectively. Escherichia coli (31.2%) was the most common and Proteus mirabilis (1.35%) was the least often found organism to cause UTIs, with the addition of klebsiella pneumonia (24.8%), and pseudomonas aeruginosa (12.2%) playing their role in causing UTIs. The gram-negative uropathogens accounted for 78.2% which caused more UTIs, followed by Gram-positive bacteria at 18.55% and fungi at 3.16%. Tigecycline (76.9%) was shown to be the most sensitive antibiotic, were as ciprofloxacin (72.3%) was the most frequently seen drug that showed resistance to uropathogens. E. coli was found to be resistant to ciprofloxacin (72.4%), but sensitive to tigecycline (95.6%). Pseudomonas aeruginosa was found to be resistant to trimethoprim/sulfamethoxazole (86.6%, but sensitive to Colistin (83.3%). Klebsiella pneumonia was found to be resistant to ciprofloxacin (67.2%) and sensitive to colistin and tigecycline (85.4%). Enterococcus species were found to be resistant to ciprofloxacin (94.5%), but sensitive to tigecycline (100%). CONCLUSION: According to the study, tigecycline was the most sensitive antibiotic while ciprofloxacin was the most resistant antibiotic. It was also identified that the most common probable causative organism was found to be E. coli.




7

SYNTHESIS AND ANTITUBERCULAR EVALUATION OF CERTAIN PYRROLE DERIVATIVES

Sandhya Chinnamulagund, Ashwini S. Joshi, Chetana, Sravanthi Avunoori, V. H. Kulkarni, Shrinivas D. Joshi*

Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical Chemistry, SET’s College of Pharmacy, Sangolli Rayanna Nagar, Dharwad 580 002, India.

A series of 2-aryl-5-[4-(1H-pyrrol-1-yl)phenyl]-1,3,4-oxadiazole derivatives (VIa-g) have been synthesized in good yields. These compounds were synthesized with an approach to reduce the growing anti-tubercular resistance and to develop more potent and less side effects having antitubercular activity. The reaction of 2,5-dimethoxytetrahydro furan with 4-aminobenzoate (II) in presence of ethanol, which yields ethyl 4-pyrrol-1-yl benzoate (III). This ethyl-4-pyrrol-1-yl benzoate (III) on reaction with hydrazine hydrate produced 4-pyrrol-1-yl benzoic acid hydrazide (IV). This carbohydrazide on treatment with different substituted benzoyl chlorides gave intermediates (Va-g), which on cyclisation with P2O5 in the presence of DMF yielded of 2-aryl-5-[4-(1Hpyrrol-1-yl)phenyl]-1,3,4-oxadiazoles VI(a-g). Structure of newly synthesized pyrrole derivatives were confirmed on the basis of physicochemical and spectral data (IR, 1H-NMR, 13C-NMR and Mass spectra). All the synthesized compounds were screened for their antitubercular activity using Microplate Alamar Blue Assay (MABA) method. Compounds showed anti-tubercular activity at MIC values between 1.6 to 12.5 µg/ml, compounds VIb,VIc and VId showed highest activity of 1.6 µg/ml. Selected compounds were evaluated for anti-bacterial activity against gram positive (S. aureus) and gram negative (E. coli). Compounds showed moderate activity. Physicochemical properties of the selected compounds satisfieds with the Lipinski’s rule of 5.