Hybrids of privileged structures benzothiazoles and pyrrolo[2,1-c] [1,4]benzodiazepin-5-one, and diversity-oriented synthesis of benzothiazoles.

Privileged structures like Benzothiazole and Pyrrolobenzodiazepine offer wonderful opportunity to explore in anti-cancer drug discovery as a mean to counter drug-resistance problem. BT-PBD hybrids and diverse BT derivatives have been synthesized and their in vitro cytotoxic activities were screened against five cancer cell lines have been discussed. The novel compounds showed promising results as compared with the marketed drug etoposide and could well be used in future anti-cancer drug development studies.

Diversity-oriented synthesis of quinolines via Friedländer annulation reaction under mild catalytic conditions.

An efficient and practical method has been manifested for the diversity-oriented synthesis of quinolines via Friedländer annulation reaction for the generation of a wide range of structurally interesting and pharmacologically significant compounds by using ceric ammonium nitrate as a catalyst (10 mol %) at ambient temperature in 45 min. A variety of functional groups are introduced at various positions of the quinoline moiety, and further the diversity of the core skeleton was expanded at R(1) and R(2) positions by the synthesis of various hybrids. Initial screening of the compounds for cytotoxicity against a series of cancer cell lines showed promising results.

Locomotor behavioral response of mosquitofish (Gambusia affinis) to subacute mercury stress monitored by video tracking system.

Locomotor behavior is commonly affected by contaminants, and the pattern of fish swimming is a highly organized species-specific response. In the current study, we examined the locomotor behavioral response of the mosquitofish, Gambusia affinis, which was exposed to a sublethal concentration (LC(5), 20 microg/L) of mercuric chloride (HgCl2) for 28 days and monitored using a computer vision system. The EthoVision video tracking system for automation of behavioral studies at regular intervals revealed abnormal locomotor behavior such as reduction in swimming speed (cm/s) and distance traveled per unit time. The effects of this metal on the gill morphology and bioaccumulation in different body parts were also investigated. High-resolution microscopy studies revealed abnormal gill morphology, with fusion of primary lamellae along with deep lesions and erosions in the secondary lamellae. The bioaccumulation concentrations in head, body, and viscera were determined by cold vapor atomic absorption spectrometric technique at regular intervals. The results indicated that the accumulation of mercury was the highest in viscera followed by head and body, with bioconcentration factors (BCFs) of 3.99, 2.18, and 1.57 and uptake rate constants (k1) of 17.91, 11.02, and 8.13, respectively. These observations indicate that alterations in fish behavior under subacute stress can provide important information useful in predicting the stress.

Toxicity of organophosphates on morphology and locomotor behavior in brine shrimp, Artemia salina.

The acute toxicity and hatching success of four organophosphorus insecticides--acephate (ACEP), chlorpyrifos (CPP), monocrotophos (MCP), and profenofos (PF)--was studied in a short-term bioassay using brine shrimp, Artemia salina. Fifty percent hatchability inhibition concentration and median lethal concentration (LC(50)) values were calculated after probit transformation of the resulting data. Among the insecticides tested, CPP is found to be the most toxic and also to inhibit hatching success of A. salina cysts in a concentration-dependent manner. In addition, the effect of these pesticides on locomotor behavior (swimming speed) and morphologic differences were studied in LC(50)-exposed nauplii after 24 hours. The in vivo effect of these insecticides on acetylcholinesterase (Enzyme commission number (EC 3.1.1.7) activity was also determined in LC(50)-exposed nauplii after 24 hours. Maximum percent decrease in their swimming speed and significant morphologic alterations were noticed in CPP-exposed brine shrimps. The order of toxicity was CPP > PF > MCP > ACEP in all the parameters studied.

Sublethal effects of profenofos on locomotor behavior and gill architecture of the mosquito fish, Gambusia affinis.

Subacute studies of profenofos on mosquito fish, Gambusia affinis, were carried out for 20 days to assess the locomotor behavior and structural integrity of gill in relation to bioaccumulation and targeted enzyme acetylcholinesterase (AChE; EC 3.1.1.7). The sublethal concentration of 0.13 mg/L (1/5 of LC50) altered locomotor behavior such as distance traveled and swimming speed in exposed fish. This could be due to inhibition in the activity of acetylcholinesterase and deformities in the primary and secondary lamella of gill. The bioaccumulation values indicated that the accumulation of profenofos was highest in viscera followed by head and body. The average bioconcentration factor values are 254.83, 6.18, and 2.52 microg/g for viscera, head, and body. The findings revealed that profenofos is highly toxic even at sublethal concentrations to the mosquito fish, Gambusia affinis.

Effect of chlorpyrifos and monocrotophos on locomotor behaviour and acetylcholinesterase activity of subterranean termites, Odontotermes obesus.

The acute toxicity of chlorpyrifos and monocrotophos to subterranean termites, Odontotermes obesus (Rambur), has been studied by a paper contact method. The LC50 values for chlorpyrifos and monocrotophos were 0.046 and 0.148 microg cm(-2), respectively. Chlorpyrifos was 3.22-fold more toxic than monocrotophos. The effect of the pesticides on locomotor behaviour (velocity) and head acetylcholinesterase (AChE: EC 3.1.1.7) activity was estimated in LC50-exposed termites at intervals of 4, 8, 12, 16, 20 and 24 h. Chlorpyrifos- and monocrotophos-treated termites showed, respectively, 97 and 88% reduction in locomotor behaviour (velocity) after 24 h. At all time intervals the chlorpyrifos-treated termites exhibited more AChE inhibition and showed greater distorted behaviour than those exposed to monocrotophos. In vitro studies indicated that the I50 value (50% inhibition) for chlorpyrifos against AChE was 8.75 times that of monocrotophos.