In vitro and in vivo assessment of polyherbal topical gel formulation for the treatment of acne vulgaris

Anti-acne herbal formulations are used for the treatment of acne vulgaris with the added advantage of not producing adverse effects unlike synthetic drugs. Phytoconstituents present in methanolic extracts of Camellia sinensis (CSME), Glycyrrhiza glabra (GGME) and Calendula officinalis (COME) have antibacterial and antioxidant properties. Validated HPTLC fingerprinting confirmed the presence of myricetin (CSME), glycyrrhizin (GGME) and kaempferol (COME) in these extracts. Extracts loaded with carbopol® 940 were used for the preparation of herbal (F1-F3) and polyherbal gel (PHF), followed by evaluation for pH, viscosity, spreadability and in vitro antibacterial potential against S. aureus, S. epidermidis and P.acnes. Polyherbal gel formulation indicated antibacterial potential and was further assessed for skin permeation by gamma scintigraphy using hydrophilic radiotracer 99mTc-DTPA and lipophilic radiotracer 99mTc-MIBI. Significant permeation (78.11%) was observed with hydrophilic radiotracer labeled 99mTc-DTPA-PHF and this suggested that the formulation was capable of sustained drug delivery for the treatment of moderate to severe type of acne.

New 2-chloro-7-methylquinoline amine analogues as possible antimycotic agents

A series of N-[(2-chloro-7-methylquinolin-3-yl)methyl]-(substituted)-aniline/butan-1-amine/cyclohexamine derivatives (4a-n) & N-benzyl-1-(2-chloro-7-methylquinolin-3-yl)methanamine (4o) was designed and synthesized based on the structural requirements essential for allylamine / benzylamine antimycotics. Compounds (4a-o) were synthesized by nucleophilic substitution reaction of 2-chloro-3-(chloromethyl)-7- methylquinoline with substituted aromatic/aliphatic primary amine in absolute ethanol in presence of triethylamine. The structures of all new products were confirmed by IR, 1H & 13C-NMR and mass spectral data. The newly synthesized compounds were screened in-vitro for their antifungal activity against Aspergillus niger MTCC 281, Aspergillus flavus MTCC 277, Monascus purpureus MTCC 369 and Penicillium citrinum NCIM 768 by cup plate method. Preliminary screening of compounds (4a-o) revealed that compounds viz. 4a, 4b, 4e, 4g, 4j and 4l showed excellent antifungal activity. Dihalogen and benzyl substituted compounds 4j, 4l & 4o exhibited potent antifungal activity. Replacement of phenyl ring with aliphatic groups like butyl or cyclohexyl causes substantial decrease in antifungal activity and activity decreases when phenyl ring is substituted with electron releasing groups.Colegio de Farmacéuticos de la Provincia de Buenos Aire

ORIENTAL JOURNAL OF CHEMISTRY Synthesis of Benzo[g]quinoxaline-5,10-dione Based Pyridine Derivatives and their Antimycobacterial Activity

ABSTRACT Thirteen new compounds belonging to series 2-amino-6-(5,10-dioxo-2,3-diphenyl-5,10-dihydrobenzo[g]quinoxalin-7-yl)-4-(substituted)phenylpyridine-3-carbonitrile (6a-m) were synthesized by multistep synthetic scheme. The newly synthesized compounds were screened for their antimycobacterial activity by L.J. Slope (Conventional) Method. Compound 6h with 4-N(CH 3 ) 2 group at phenyl ring of above mentioned position has been reported as most active antimycobacterial compound and compound 6k with 4-CH 3 substitution at phenyl above mentioned position has been reported as the least active antimycobacterial compound

Synthesis and pharmacological screening of 4, 6-substituted di-(phenyl) pyrimidin-2-amines

A new series of 4, 6-substituted di-(phenyl) pyrimidin-2-amine (IIa–d) were synthesized by reacting chalcone derivatives with guanidine hydrochloride in the presence of dimethylformamide. The synthesized compounds were characterized by spectral analysis and were screened for anti-inflammatory activity. Two compounds 4-(4-nitrophenyl)-6-phenylpyrimidine-2-amine (IIa) and 4-(4-methoxyphenyl)-6-phenylpyrimidine-2-amine (IIb) showed highly significant reduction in oedema volum

N-[(2-Chloro-6-methylquinolin-3-yl)methyl]aniline

Quinolinyl amines are important organic compounds which possess a variety of pharmacological activities such as antimalarial, antifungal, hypotensive and antidepressant activity

Structural modifications of quinoline-based antimalarial agents: Recent developments

Antimalarial drugs constitute a major part of antiprotozoal drugs and have been in practice for a long time. Antimalarial agents generally belong to the class of quinoline which acts by interfering with heme metabolism. The recent increase in development of chloroquine-resistant strains of Plasmodium falciparum and failure of vaccination program against malaria have fuelled the drug discovery program against this old and widespread disease. Quinoline and its related derivative comprise a class of heterocycles, which has been exploited immensely than any other nucleus for the development of potent antimalarial agents. Various chemical modifications of quinoline have been attempted to achieve analogs with potent antimalarial properties against sensitive as well as resistant strains of Plasmodium sp., together with minimal potential undesirable side effects. This review outlines essentially some of the recent chemical modifications undertaken for the development of potent antimalarial agents based on quinoline

Synthesis and biological evaluation of di- and tri-substituted imidazoles as safer anti-inflammatory-antifungal agents

Purpose: In view of the potential pharmacophoric nature of imidazole nucleus, two series of imidazole derivatives, 2,4-disubstituted-1 H-imidazoles (2a-m) and 1,2,4-trisubstituted-1 H-imidazoles (3a-m), were synthesized with an aim of obtaining dual acting compounds i.e., anti-inflammatory and antifungal agents. Materials and Methods: The title compounds were synthesized from 4-methoxyphenyl glyoxal (1) following multistep synthesis, and their structures were established on the basis of modern analytical techniques (IR, NMR and MS). The synthesized imidazoles were tested for their in vivo anti-inflammatory activity. In addition to that, some compounds were also evaluated for their analgesic and ulcerogenic effects. The compounds were also evaluated for their in vitro antifungal activity. Results: Di- and tri-substituted imidazole derivatives (2a-m and 3a-m) were successfully synthesized. In in vivo anti-inflammatory test, six compounds (2 h, 2 l, 3 g, 3 h, 3 l and 3 m) exhibited good anti-inflammatory activity (49.58 to 58.02% inhibition) with minimal GI irritation (severity index; 0.17 to 0.34). These compounds were also tested for their analgesic activity and showed appreciable protection (40.53 to 49.60% protection) against saline-induced writhing test. Indomethacin was used as standard drug for comparison. In antifungal test, two compounds (3 h and 3 l) displayed appreciable antifungal activity (MIC; 12.5 μg mL -1 ) against the fungal strains tested. Conclusion: Two compounds, 2-(4-nitrophenyl)-4-(4-methoxyphenyl)-1-phenyl-1H-imidazole (3 h) and 2,4-di-(4-methoxyphenyl)-1-phenyl-1H-imidazole (3 l), emerged as lead compounds having dual biological activities; good anti-inflammatory as well as antifungal effect with lesser GI irritation