Synthetic heterocyclic compounds have incredible potential against different diseases; pyridines, phenolic compounds and the derivatives of azo moiety have shown excellent antimicrobial, antiviral, antidiabetic, anti-melanogenic, anti-ulcer, anticancer, anti-mycobacterial, anti-inflammatory, DNA binding and chemosensing activities. In the present review, the above-mentioned activities of the nitrogen-containing heterocyclic compounds (pyridines), hydroxyl (phenols) and azo derivatives are discussed with reference to the minimum inhibitory concentration and structure–activity relationship, which clearly indicate that the presence of nitrogen in the phenyl ring; in addition, the hydroxyl substituent and the incorporation of a diazo group is crucial for the improved efficacies of the compounds in probing different diseases. The comparison was made with the reported drugs and new synthetic derivatives that showed recent therapeutic perspectives made in the last five years.

Surra, a vector borne disease caused by Trypanosoma (T.) evansi, affects the health, productivity and working capacity of camels. Since clinical signs are not pathognomonic, diagnosis must be confirmed by laboratory methods. This is a first study on the prevalence of surra in Cholistan Desert, Pakistan using a broad variety of diagnostic tests thereby emphasizing it as a risk for the dromedaries of Pakistan. In a cross sectional study, 1005 dromedary camels from three districts in the Cholistan Desert were sampled to assess the prevalence of trypanosomosis due to T. evansi by means of parasitological (Giemsa stained thin smear), serological (formol gel test, CATT/T. evansi, ELISA/VSG RoTat 1.2, immune trypanolysis) and molecular tests (TBR1/2 PCR and RoTat 1.2 PCR). Kappa was calculated to assess the degree of agreement between different tests whereas chi-square test along with odds ratios and their 95 % confidence intervals were used to study influence of breed, gender, age and locality on disease prevalence. Overall prevalence was 0.7 % with Giemsa stained thin smears (GST), 40.1 % with formol gel test (FGT), 47.7 % with CATT/T. evansi, 44.2 % with ELISA/VSG RoTat 1.2, 39.9 % with immune trypanolysis (TL), 31.9 % with TBR1/2 PCR and 30.5 % with RoTat1.2 PCR. Based on these results, the Cholistan Desert appears to be a high risk area for surra. According to TL and TBR1/2 PCR, camels at Bahawalpur are approximately two times more likely to be infected than those in Bahawalnagar (OR = 1.8; 95 % CI: 1.38-2.42) and Rahim Yar Khan (OR = 1.9; 95 % CI: 1.30-2.75). Test agreement of TL was moderate with CATT/T. evansi (k = 0.43; 95 % CI: 0.378-0.489) and ELISA/VSG RoTat 1.2 (k = 0.54; 95 % CI: 0.489-0.594) and poor with the other tests. Test agreement between TBR1/2 PCR and RoTat1.2 PCR was almost perfect (k = 0.96; 95 % CI: 0.950-0.984). We didn't find evidence for the presence of T. evansi type B in the studied population. Our study supports using antibody detection tests, rather than parasitological and molecular examination, to assess surra prevalence in camels. It also calls for implementation of measures to control surra in the Cholistan Desert.

In the present study, a series of azo derivatives (TR-1 to TR-9) have been synthesised via the diazo-coupling approach between substituted aromatic amines with phenol or naphthol derivatives. The compounds were evaluated for their therapeutic applications against alpha-glucosidase (anti-diabetic) and pathogenic bacterial strains E. coli (gram-negative), S. aureus (gram-positive), S. aureus (gram-positive) drug-resistant strain, P. aeruginosa (gram-negative), P. aeruginosa (gram-negative) drug-resistant strain and P. vulgaris (gram-negative). The IC₅₀ (µg/mL) of TR-1 was found to be most effective (15.70 ± 1.3 µg/mL) compared to the reference drug acarbose (21.59 ± 1.5 µg/mL), hence, it was further selected for the kinetic studies in order to illustrate the mechanism of inhibition. The enzyme inhibitory kinetics and mode of binding for the most active inhibitor (TR-1) was performed which showed that the compound is a non-competitive inhibitor and effectively inhibits the target enzyme by binding to its binuclear active site reversibly.

Objectives: Neurada procumbens L. (Neuradaceae ) is a Cholistani desert plant traditionally employed in fever, inflammations, diabetes and hepatitis. The purpose of this study was to determine the chemical composition, anti-bacterial, antibiofilm and antioxidant activities of various extracts of this important medicinal plant; separately for its aerial and floral parts. Methods: The phytochemical screening (by HPLC analysis), antioxidant (by DPPH assay), antibacterial (by disc diffusion test and MIC) and anti-biofilm potential against seven bacterial strains (E. coli, K. pneumoniae, S. aureus, S. aureus MDR, P. aeruginosa, P. aeruginosa MDR and P. vulgaris) were determined by aqueous, methanol, n-butanol, ethyl acetate, n-hexane and dichloromethane extracts of floral and aerial parts of N. procumbens. Results: The floral MetOH and DCM extracts were found to contain higher polyphenolic contents including 2,3-di methoxy benzoic acid (38.21 µg/mg), chlorogenic acid (26.59 µg/mg) and catechin (14.24 µg/mg) and exhibited a comparatively higher antioxidant (IC ₅₀ < 100 μg/ml) potential in DPPH assay. Moreover, these floral MetOH and DCM extracts were found to be most active (>13.5 mm zone of inhibition and MICs 62.5–125 µg/ml) against P. aeruginosa MDR and S. aureus in anti-bacterial activity. In an anti-biofilm assay, MetOH and DCM floral extracts showed a promising potential (>85 % biofilm inhibition) with IC₅₀ < 150 μg/ml against P. aeruginosa MDR and S. aureus MDR better than moxifloxacin and was further confirmed by light and scanning electron microscopy. Moreover, the floral-MetOH extract of N. procumbens has been found to be safe up to 2 g/kg BW with its lethal dose (LD₅₀) as 3872.98 mg/kg BW in rats. Conclusion: Hence, due to presence of essential medicinal compounds with low toxicity effects, the plant is recommended to be safely employed in various pharmaceutical preparations.

Aslam J, et al. J Vet Sci. 2024 May;25(3):e47. https://doi.org/10.4142/jvs.23258