Structure-activity relationship of pharmacophores and toxicophores: the need for clinical strategy.

Objectives: Sometimes clinical efficacy and potential risk of therapeutic and toxic agents are difficult to predict over a long period of time. Hence there is need for literature search with a view to assessing cause of toxicity and less efficacy of drugs used in clinical practice.

Method: Hence literatures were searched for physicochemical properties, chemical formulas, molecular masses, pH values, ionization, receptor type, agonist and antagonist, therapeutic, toxic and structure-activity relationship of chemical compounds with pharmacophore and toxicophore, with a view to identifying high efficacious and relative low toxic agents.

Biomedical Applications of Polyurethane Hydrogels, Polyurethane Aerogels, and Polyurethane-graphene Nanocomposite Materials.

Background: The emergence of new diseases poses therapeutic challenges in modern medicine. Polyurethane hydrogels that comprise polyol, copolymer and extender could be prepared from diverse chemical compounds with adjuvants such as ascorbic acid and sorbitol, among others. Their mechano-physicochemical properties are functions of their biological activities.

Genetic diversity of canine parvovirus variants circulating in Nigeria.

Canine parvovirus (CPV) is a fast-evolving single-stranded DNA virus that causes severe and fatal gastrointestinal disease in dogs. Lately, several mutations affecting viral protein (VP) capsid resulting in highly pathogenic variants with distinctive immunological and clinicopathological characteristics abound. This study involved screening stools of 44 randomly selected clinical cases of canine gastroenteritis from 4 cities (Ibadan, Jos, Makurdi, and Zaria) in Nigeria for CPV antigen using an on-the-spot immunoassay test kit, as well as, molecular detection of viral nucleic acid by polymerase chain reaction.

Modified formulas for calculation of encephalization: quotient in dogs.

Objective: Dogs are a breed of animals that play important roles in security service, companionship, hunting, guard, work and models of research for application in humans. Intelligence is the key factor to success in life, most especially for dogs that are used for security purposes at the airports, seaports, public places, houses, schools and farms. However, it has been reported that there is correlation between intelligence, body weight, height and craniometry in human.

Comparative therapeutic index, lethal time and safety margin of various toxicants and snake antivenoms using newly derived and old formulas.

Objective: The assessment of clinical efficacy and toxicity is very important in pharmacology and toxicology. The effects of psychostimulants (e.g.

Application of median lethal concentration (LC) of pathogenic microorganisms and their antigens in vaccine development.

Objective: Lack of ideal mathematical models to qualify and quantify both pathogenicity, and virulence is a dreadful setback in development of new antimicrobials and vaccines against resistance pathogenic microorganisms. Hence, the modified arithmetical formula of Reed and Muench has been integrated with other formulas and used to determine bacterial colony forming unit/viral concentration, virulence and immunogenicity.

Results: Microorganisms' antigens tested are Staphylococcus aureus, Streptococcus pneumoniae, Pseudomonas aeruginosa in mice and rat, Edwardsiella ictaluri, Aeromonas hydrophila, Aeromonas veronii in fish, New Castle Disease virus in chicken, Sheep Pox virus, Foot-and-Mouth Disease virus and Hepatitis A virus in vitro, respectively.

Therapeutic effects of root bark extract on bacterially and chemically induced diarrhea in the Wistar albino rat ().

Background: Diarrhea can be caused by pathogenic microorganisms and chemicals. In view of this, Schum and Thonn (Connaraceae) was used to treat diarrhea induced by castor oil or bacteria in Wistar albino rats.

Methods: Qualitative and quantitative analyses of an aqueous root back extract of were made and the acute toxicity, antidiarrhea properties, and in vitro and in vivo antimicrobial activities of the extract were investigated in rats.

Chirality of Central Nervous System (CNS) Acting Drugs: A Formidable Therapeutic Hurdle Against CNS Diseases.

Background: Over fifty percent of drugs being used clinically are chiral and 90% of them are racemates. Unfortunately, they have both adverse and beneficial effects on body systems.

Methods: Because of the erratic effects of chiral compounds on body functional systems, literature search was carried out with a view to identify CNS chiral drugs, their clinical advantages and disadvantages, unique physicochemical properties and structural modifications into safer drugs.

Conversion of Benzimidazoles, Imidazothiazoles and Imidazoles into more Potent Central Nervous System Acting Drugs.

Background: Benzimidazole (albendazole), imidazothiazole (levamisole) and imidazole (euconazole) are used in chemotherapy of helminthosis and mycosis respectively, with central nervous system (CNS) side effects. But only a limited number of azole groups are used clinically in the treatment of CNS diseases, which are on increase and could not be cured permanently. Due to increased incidence of more challenging new CNS diseases, there is a need for the synthesis of more potent CNS drugs.

Chemistry and Effects of Brainstem Acting Drugs.

Background: Brain is the most sensitive organ, whereas brainstem is the most important part of Central Nervous System (CNS). It connects the brain and the spinal cord. However, a myriad of drugs and chemicals affects CNS with severe resultant effects on the brainstem.

Determination of median effective dose (ED) of scorpion antivenom against scorpion envenomation using a newly developed formula.

Background: About 50 species of scorpions cause fatal scorpionism worldwide. Most of these are members of the Buthidae family, and include, among others, , , , , and . Because high doses of scorpion venom and antivenom can cause death and hypersensitive reactions, there is a need to develop a formula that can be used to calculate both lethal and effective doses for scorpion venom and antivenom, respectively, thereby obviating the need for laboratory experiments.

Biomedical Application of Polymers: A Case Study of Non-CNS Drugs Becoming CNS Acting Drugs.

Background: The transport of CNS acting drugs across blood-brain barrier (BBB) is complex and guided by the molecular weight, pH, physicochemical and pathological state of the BBB among others.

Methods: In view of this, literatures were assessed for possible conversion of Non-CNS to CNS acting drugs, whose ability to penetrate CNS can be improved using polymers for biomedical applications.

Results: The findings have shown that compounds with pyridine, pyrrole, carboxamide, pyridone among others can be converted to CNS acting drugs that can be loaded in specialized carrier polymers for transportation across BBB.

Functional Chemical Groups that May Likely Become a Source for the Synthesis of Novel Central Nervous System (CNS) Acting Drugs.

Introduction: Central Nervous System (CNS) disorders are on increase perhaps due to genetic, enviromental, social and dietetic factors. Unfortunately, a large number of CNS drugs have adverse effects such as addiction, tolerance, psychological and physical dependence. In view of this, literature search was carried out with a view to identify functional chemical groups that may serve as lead molecules for synthesis of compounds that may have CNS activity.

The new algorithm for calculation of median lethal dose (LD) and effective dose fifty (ED) of Micrarus fulvius venom and anti-venom in mice.

One million people throughout the world are bitten yearly by poisonous snakes. Of this, one-tenth died and three-tenth suffer some forms of disabilities. In view of this, anti-snake venoms are currently being developed against viper and colubrid snake venoms using mice.

In vivo Piroxicam Metabolites: Possible Source for Synthesis of Central Nervous System (CNS) Acting Depressants.

Background: Piroxicam has been reported to be convertible to Central Nervous System (CNS) acting agents. It has serious depressant effects at high doses.

Objective: In view of this, structures of piroxicam metabolites were assessed for possible conversion to CNS depressants.

Toxico-Neurological Effects of Piroxicam in Monogastric Animals.

Piroxicam is a benzothiazine compound with anti-inflammatory, antipyretic, and analgesic properties. Because of the very high efficacy of piroxicam and its increasing use in the treatment of carcinomas in dogs and cats, there is a need for acute toxicity study of piroxicam in monogastric animals and its potential for causing secondary poisoning in puppies. Piroxicam manufactured by Shanxi Federal Pharmaceutical Co, Ltd.

Piroxicam: Source for Synthesis of Central Nervous System (CNS) Acting Drugs.

Background: The use of central nervous system (CNS) acting drugs in the management of neuro degenerative and psychiatric problems cannot be overemphasized. Therefore, the chemical structure of piroxicam can be modified to yield new CNS stimulants and depressants that can be of great benefit to man and animals.

Methodology: Acetylcholine has Methyl - Oxygen-Oxygen (M-O-O) and Nitrogen (N) functional groups which are structurally related to Sulphur-Oxygen-Oxygen (S-O-O) and Nitrogen (N) of piroxicam that are either methylated or hydrogenated.

Ameliorative properties of aqueous extract of Ficus thonningii on erythrocyte osmotic fragility induced by acetaminophen in Rattus norvegicus.

In vitro antioxidant and erythrocyte protecting activities by aqueous extract of Ficus thonningii leaves on blood cells were studied in acetaminophen treated rats. The extract was safe at limit dose of 5000 mg kg(-1) body weight. The extract demonstrated dose dependent antihemolytic effect at dose levels between 50 and 200 mg kg(-1) body weight.