Posted by admin on Jan 31, 2017 in |
1,2,3-Benzotriazole (BTA) is a heterocyclic compound with three nitrogen atoms. The enormous investigations on derivatives of benzotriazole reveals wide applicability of this molecules for tagging and delivering huge number of heterocyclic nuclei. This molecule has been used for the analytical determination of silver as well as a restrainer in photographic emulsions. The effectiveness of 1,2,3-Benzotriazole (BTA) as drug precursors have been drawing attention for a long period. The derivatives of benzotriazole act as agonists for many biologically active proteins. For instance, corozole and alizapride have the inhibitory properties against different proteins and Benzotriazole esters have been reported to work as mechanism-based inactivators for severe acute respiratory syndrome (SARS) 3CL protease. The various derivatives synthesized by different research workers showed antimicrobial activities such as antibacterial, antifungal, antiviral, anthelmintics, antiprotozoal and antimycobacterial activity. The present article throws light on the different derivatives of benzotriazole and their related biological activity, and is reported chronologically. The chronologic development in the synthesis of its derivatives and related changes in therapeutic activity opens new channels...
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Posted by admin on Dec 31, 2016 in |
Reactive oxygen species (ROS) are inevitable by-products of cellular respiration. These are highly reactive chemical species derived from molecular oxygen (O2). These include the superoxide (O2−) and hydroxyl (HO−) free radicals as well as non-radical molecules such as hydrogen peroxide (H2O2). These act as both toxic and beneficial compounds, since they can be either harmful or helpful to the body. Redox regulation or controlled ROS generation is the net effect of a subtle balance between ROS generation and neutralization or utilization by cellular antioxidant systems. The most deleterious effect of ROS is “oxidative stress”. Oxidative stress plays a major part in the development of chronic and degenerative ailments such as cancer, arthritis, aging, autoimmune disorders, cardiovascular and neurodegenerative diseases. Several mechanism exists to counteract oxidative stress. This review provides a detailed overview of the influence of ROS on human pathophysiology and novel therapeutic strategies followed to treat ROS mediated diseases or...
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Posted by admin on Dec 31, 2016 in |
Mimusops elengi L. is an Indian origin herb used in the Unani and other traditional systems of medicine since long time. It is commonly called by the names Spanish cherry, West Indian Medlar or Bullet wood tree. This plant is frequently cultivated throughout India especially in north India for its ornamental appearance and fragrant flowers. All parts of plant such as leaf, root, fruit, seed, bark, flower of Mimusops elengi were reported for treatment of various human ailments in traditional system of medicine. Pharmacological activities like antimicrobial, antifungal, antioxidant and free radical scavenging, anti-inflammatory analgesic, antipyretic, antiurolithiatic, cytotoxic, diuretic, neuroprotective, anti-amnesic, cognitive enhancing, antihyperglycemic, antihyperlipidemic, hypotensive, antiulcer, anthelmintic, antitumor, wound healing, larvicidal activities have been scientifically evaluated for various parts of this plant. A number of phytochemical constituents have been identified in this plant that may be responsible for its pharmacological activities. So many articles are available on Mimusops elengi L., but from Unani literature the discussion is very limited. This review is an effort to summarize the detailed...
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Posted by admin on Dec 31, 2016 in |
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) in addition with Nucleoside reverse transcriptase inhibitors (NRTIs) and protease inhibitors (PIs) used in the treatment of HIV-1 infection. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) gained exact place in the treatment of HIV-1 infections. Starting from the HEPT and TIBO derivatives, different classes of compounds have been identified as NNRTIs, that is compounds that are specifically inhibitory to HIV-1 replication and targeted at the HIV-1 reverse transcriptase (RT). Two NNRTIs (nevirapine and delavirdine) have been formally licensed for clinical use and several others are (or have been) in preclinical and: or clinical development [tivirapine (TIBO R-86183), loviride (a-APA R89439), thiocarboxanilide UC-781, HEPT derivative MKC-442, quinoxaline HBY 097, DMP 266 (efavirenz), PETT derivatives (trovirdine, PETT-4, PETT-5) and the dichlorophenylthio (pyridyl) imidazole derivative [S-1153]. Several compounds acting as Reverse transcriptase inhibitors was proved to be highly valuable against HIV-1 replication with minimal toxicity. NNRTIs interact with a specific ‘pocket’ site of HIV-1 RT and thus inhibiting the translocation and further elongation of DNA strand. The major drawbacks...
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Posted by admin on Dec 31, 2016 in |
“Acid labile drug” means a drug that is easily destroyed in acidic environment, Stomach is the main site for drug absorption mainly by oral rout. The pH of the stomach is acidic so the absorption of acid labile drugs through stomach is difficult. For this resign the drugs should be formulated as enteric coated or may be administered through parenteral rout. These approaches are effective but they increase the cost of the dosage form. So for making the acid labile drug effective in acidic environment one of the best approach is in-situ buffer formulation. These are the formulation containg agents which immediately buffer the internal environment of the body and increases the stability of acid labile drugs inside the body. This article covers the possible approaches for buffer formulation, formulations could be possible, method of preparation and evaluation of in-situ buffer formulation. The articles the examples of agents can be used as...
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