(1H-Pyrrolo [2,3-b]pyridine)7-Azaindole Derivatives and Their Antiurease, Phosphodiesterase and ẞ-glucuronidase Activity.

A variety of 7-azaindole analogs 1-14 with variable substituents on phenyl ring of phenacyl moiety were synthesized and evaluate for their urease, phosphodiesterase and -glucuronidase Inhibitory potential. Compound 9 (IC50 = 2.19±0.37μM) showed potent urease inhibitory potential than standard thiourea (IC50 = 21.00±0.01μM). However, while compounds 10 (IC50 = 255.11±6.62μM) and 8 (IC50 = 133.3±0.46μM), exhibited moderate urease potential. Moreover, compound 2 (IC50 = 20.83± 0.234μM) showed potent phosphodiesterase inhibitory potential than standard EDTA (IC50 = 274.00+0.007μM). Compound 8 (IC50 192.6±3.53μM) was found to be moderate ẞ-glucuronidase inhibitor, as compare to standard 1,4, lactone D saccharic acid (IC50 = 48.41±1.24μM). Nevertheless, compounds 13 (36.81% inhibition) and 14 (47.11% inhibition) showed less than 50% ẞ-glucuronidase inhibition, therefore they were not further evaluated for their IC50 values. The size of the substituent, electron donating or withdrawing affect of substituents as well as the position of substituent on phenyl affects the activity.

(1H-Pyrrolo [2,3-B] Pyridine) 7-Azaindole as Cholinesterase/ Glycation Inhibitors.

As a part of our program to discover novel analoges of (1H-pyrrolo [2,3-b] pyridine) 7- azaindole having useful biological activities, a variety of 7-azaindole analogs 1-9 with variable substituents on phenyl ring of phenacyl moiety were synthesized and evaluated for their AChE, BChE and antiglycation Inhibitory potential. Compounds 2-5 were found to be AChE inhibitors with IC50 1.34 μM, 11.60 μM, 0.96 μM and 0.97 μM respectively, while compounds 2-5 were also found to be BChE inhibitors with IC50 1.25 μM, 3.93 μM, IC50 9.18μM and 10.20μM respectively. Compounds 2 (IC50 = 1.25±0.019uM) and 3 (IC50 = 3.93±0.36uM), showed potent BChE inhibitory potential than standard Galantamine (IC50 = 8.51±0.02uM). Besides this, compounds 2-9 were evaluated for glycation inhibition activity. Compound 5 (IC50 values 120.6+0.2uM) showed potent antiglycation potential than standard rutin (IC50=294.50+1.5uM). The size of the substituent, electron donating or withdrawing effect of substituents as well as the position of substituent on phenyl effects the activity.

Heterotopic pregnancy: a rare spontaneous case

An 18-years old primigravida, married for the last three months presented at 7 weeks gestational age with complaints of sudden onset of severe pain in lower abdomen and vaginal spotting for the last six hours. Her menstrual cycle was regular. This was a planned spontaneous conception. Her pregnancy test was positive, but there was no ultrasonic evidence available. On examination she was extremely pale and sweating. The blood pressure was 70/40 mmHg, and pulse 120/min. Cervical os was closed with slight brownish vaginal discharge. There was fullness in all fornices and uterus size could not be assessed due to marked tenderness. She was immediately resuscitated with intravenous fluids. Ultrasound revealed ruptured ectopic pregnancy. Her hemoglobin was 5 grams%. On emergency laparotomy, there was 3 liters of fresh and clotted blood in the peritoneal cavity. Both the tubes were intact but right was slightly swollen and bleeding, it seems like tubal abortion. Right salpingectomy was done. Specimen sent for pathologic examination. Both ovaries were normal looking and uterus was bulky. Haemostasis was secured and abdomen was closed. About three weeks postoperatively she presented with persistent nausea and vomiting, on thorough examination ultrasound revealed normal intrauterine gestation of 10 weeks consistent with her LMP. She was followed up regularly for fetal growth, and any other complications. She went into spontaneous labour at term and delivered a live normal male baby of 2.8 kilograms by vaginal route